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Professor Roger Pertwee

Professor Roger Pertwee
Professor Roger Pertwee
Professor Roger Pertwee

Emeritus Professor

About
Email Address
rgp@abdn.ac.uk
Office Address

School of Medical Sciences Institute of Medical Sciences University of Aberdeen Foresterhill Aberdeen AB25 2ZD Scotland, UK

School/Department
School of Medicine, Medical Sciences and Nutrition

Biography

Roger Pertwee has three degrees from the University of Oxford: MA (in biochemistry), D.Phil. (in pharmacology) and D.Sc. (in physiological sciences). He is now an Emeritus Professor at the University of Aberdeen, where he is still actively engaged in scientific research. He is also co-chairman of the International Union of Basic and Clinical Pharmacology (IUPHAR) Subcommittee on Cannabinoid Receptors, a co-ordinator of the British Pharmacological Society’s Special Interest Group on Cannabinoids, a co-founder of the International Cannabinoid Research Society (ICRS) <http://icrs.co/> , and an invited scientific advisor on cannabinoid pharmacology/therapeutics to the Beckley Foundation <http://beckleyfoundation.org/about/advisory-boards/>, has had formal cannabinoid pharmacology-related links with several pharmaceutical companies, and currently has such a link with GW Pharmaceuticals. He has served too, twice as President of the ICRS (1997-1998 and 2007-2008), and once as Chairman of the International Association for Cannabinoid Medicines (IACM; 2005-2007), and is also currently ICRS International Secretary, and a member of the IACM Board of Directors <http://www.cannabis-med.org/index.php?tpl=page&id=74&lng=en>. He was the recipient of the 2002 Mechoulam Award “for his outstanding contributions to cannabinoid research”. He was also awarded the 2011 Wellcome Gold Medal by the British Pharmacological Society (BPS) “for outstanding contributions to pharmacology, based mainly on research achievements”, and the 2013 IACM Special Award “for his major contributions to the re-introduction of cannabis as a medicine”, and is an Honorary Fellow of the BPS: this fellowship is awarded to BPS members who have “demonstrated distinction and peer recognition in science, or have given long and valuable service to the Society”. In addition, he was identified by Thomson Reuters in 2005 to be a “Highly Cited Researcher” and hence among “the world's most cited and influential researchers”. He also received (1) a Highly Cited Researcher Award from Thomson Reuters in September 2014 “in recognition of ranking among the top 1% of researchers for most cited documents in their specific field” (see Pertwee in “Archives” at <http://hcr.stateofinnovation.thomsonreuters.com/page/archives> and from Clarivate Analytics in 2018 “in recognition of exceptional research performance demonstrated by production of multiple highly cited papers, those that rank in the top 1% by citations for field and year in Pharmacology and Toxicology” and (2) the 2018 Lifetime Achievement Award from the International Cannabinoid Research Society "for outstanding contributions to cannabinoid research and the ICRS".

Roger Pertwee presented evidence on cannabis in person at the House of Lords to the Science and Technology Committee which published its report on cannabis in 1998. He is the author of numerous review articles on the cannabinoids and is often invited to speak on the pharmacology of cannabinoids at international conferences. He is also interested in the therapeutic potential of cannabinoids. Indeed, he was a contributing author of the British Medical Association book entitled "Therapeutic Uses of Cannabis." and served on the Royal Pharmaceutical Society working party that recommended and helped to design clinical trials with cannabis and THC that were carried out in the UK and funded by the Medical Research Council. Together with Drs Rik Musty and Paul Consroe he also carried out the first large survey of multiple sclerosis patients who self-medicate with cannabis [Eur Neurol (1997) 38: 44]. His contributions to the "medicalization of cannabis" are summarized in a Witness Seminar Transcript (Vol 40), co-authored by Crowther, S.M., Reynolds, L.A. and Tansey, E.M. and published in 2010 by The Wellcome Trust Centre for the History of Medicine at UCL. This book is freely downloadable at <http://www.history.qmul.ac.uk/research/modbiomed/wellcome_witnesses/volume40/index.html>.

Roger Pertwee's research focuses on the pharmacology of cannabinoids. He began his work in this area in 1968 as a post-doc with Professor Sir William Paton at the Department of Pharmacology, Oxford University. He initially worked with cannabis and also with delta-9-tetrahydrocannabinol (THC) and cannabidiol, both of which were extracted from tincture of cannabis, then still a legal medicine in the UK. This research led to the demonstration that cannabidiol is a highly effective inhibitor of hepatic microsomal enzymes and to the development of the "ring immobility test", still widely used as a behavioural bioassay.

After moving to Aberdeen in 1974, Roger Pertwee continued with his cannabinoid research, initially investigating the basis for the hypothermic effect of THC. This work provided evidence that THC lowers the thermoregulatory set point such that animals regulate their core temperature at a lower level than normal by adjusting heat gain and heat loss both autonomically and behaviourally. In other research carried out during this time he found that cannabinoids interact synergistically with benzodiazepines and also identified the globus pallidus as one of the sites at which cannabinoids alter motor function.

Opioid research with the mouse isolated vas deferens being carried out in Professor Hans Kosterlitz's laboratory in Aberdeen gave Roger Pertwee the opportunity to establish whether this tissue would also serve as a bioassay for cannabinoids. The mouse vas deferens turned out to be an extremely sensitive quantitative assay for CB1 agonists. He presented some of the initial vas deferens data at a cannabinoid meeting in Palm Beach in 1991 and this led to a collaboration with Professor Raphael Mechoulam who was also at the meeting. As a result, using the mouse vas deferens, Roger Pertwee (with Graeme Griffin) was able to provide the first evidence that anandamide not only binds to cannabinoid receptors (Dr William Devane's data) but also activates these receptors, greatly strengthening the argument that anandamide is an endogenous cannabinoid/endocannabinoid [Science (1992) 258:1946]. Other research in his laboratory, led by Dr Angela Coutts, was directed at mapping out the distribution of cannabinoid receptors in brain and gut using immunohistochemical techniques.

His research has also played major roles in

  • the discovery that ethanolamides that are formed from dietary omega-3 polyunsaturated fatty acids and that seem to be endocannabinoids, have the capacity to inhibit cancer cell growth and proliferation;

  • the discovery of a cannabinoid CB1 receptor allosteric site;

  • the discovery that delta-9-tetrahydrocannabivarin is a plant cannabinoid (phytocannabinoid) - and that this compound is both a cannabinoid CB1 receptor blocker (antagonist) and a cannabinoid CB2 receptor activator (agonist) that has the potential to treat drug dependence, Parkinson’s disease, stroke, obesity and liver diseases, and to reduce health risks associated with liver transplantation;

  • the pharmacological characterization of other phytocannabinoids, including cannabidiol, cannabidiolic acid & cannabigerol, and the further pharmacological characterization of THCV;

  • the discovery/pharmacological characterization of novel synthetic cannabinoids many of which are widely used by cannabinoid researchers as experimental tools, e.g.

  1. methanandamide, the first CB1 receptor-selective agonist (with Dr Alexandros Makriyannis);

  2. two other CB1-selective agonists: ACEA & ACPA (with Dr Cecelia Hillard);

  3. HU-308, a CB2-selective agonist (with Dr Raphael Mechoulam);

  4. AM281, a widely-used CB1 receptor antagonist, and AM630, a widely-used CB2 receptor antagonist (with Dr Alexandros Makriyannis);

  5. CB1 receptor “neutral” antagonists;

  6. O-1057, the first water-soluble cannabinoid receptor ligand (with Drs Billy Martin and Raj Razdan);

  7. novel positive and negative allosteric modulators of the CB1 receptor (with Dr Ganesh Thakur). 

Research now being carried out in Roger Pertwee's laboratory is directed (i) at seeking out further pharmacological actions of phytocannabinoids, (ii) at elucidating the pharmacological actions of other constituents of cannabis, and (iii) at exploring the actions and therapeutic potential of novel synthetic allosteric modulators of cannabinoid receptors. This research, which is being conducted mainly using radioligand binding assays and in vitro bioassays that measure drug effects on cannabinoid receptor signalling (e.g. [35S]GTPgammaS binding assays), is currently supported by the US National Institute on Drug Abuse (part of NIH) and by GW Pharmaceuticals. He is also presently collaborating with colleagues at Aberdeen University in cannabinoid research funded by Diabetes UK and by Medical Research Scotland.

 

Research

Research Overview

Primary research interests:

·       pharmacology and therapeutic potential of plant cannabinoids

·       pharmacology of allosteric sites on cannabinoid receptors

·       novel cannabinoid CB1 and CB2 receptor ligands

·       new pharmacological targets for cannabinoids

·       roles of the endocannabinoid system in health and disease

 

Current Research

Roger Pertwee's current research is directed at seeking out pharmacological actions of phytocannabinoids, and at elucidating the pharmacological actions of other constituents of cannabis. In addition, he is currently following up a discovery made in his laboratory that there is at least one allosteric site on the cannabinoid CB1 receptor, by exploring the actions and therapeutic potential of novel synthetic allosteric modulators of cannabinoid receptors.

 

 

 

 

 

Publications

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  • The psychoactive plant cannabinoid, Δ9-tetrahydrocannabinol, is antagonized by Δ8- and Δ9-tetrahydrocannabivarin in mice in vivo

    Pertwee, R. G., Thomas, A., Stevenson, L. A., Ross, R. A., Varvel, S. A., Lichtman, A. H., Martin, B. R., Razdan, R. K.
    British Journal of Pharmacology, vol. 150, no. 5, pp. 586-594
    Contributions to Journals: Articles

  • Significance of cardiac cannabinoid receptors in regulation of cardiac rhythm, myocardial contractility, and electrophysiologic processes in heart

    Krylatov, A. V., Maslov, L. N., Ermakov, S. Y., Lasukova, O. V., Barzakh, E. I., Crawford, D., Pertwee, R. G.
    Bulletin of Experimental Biology and Medicine, vol. 34, no. 1, pp. 28-35
    Contributions to Journals: Articles

  • Differential effects of cannabis extracts and pure plant cannabinoids on hippocampal neurones and glia

    Ryan, D., Drysdale, A. J., Pertwee, R. G., Platt, B.
    Neuroscience Letters, vol. 408, no. 3, pp. 236-241
    Contributions to Journals: Articles

  • Effect of sublingual application of cannabinoids on intraocular pressure: A pilot study

    Tomida, I., Azuara-Blanco, A., House, H., Flint, M., Pertwee, R. G., Robson, P. J.
    Journal of Glaucoma, vol. 15, no. 5, pp. 349-353
    Contributions to Journals: Articles

  • In vitro and in vivo pharmacology of synthetic olivetol- or resorcinol-derived cannabinoid receptor ligands

    Cascio, M. G., Bisogno, T., Palazzo, E., Thomas, A. D., van der Stelt, M., Brizzi, A., De Novellis, V., Marabese, I., Ross, R. A., van de Doelen, T., Brizzi, V., Pertwee, R. G., Maione, S., Di Marzo, V.
    British Journal of Pharmacology, vol. 149, no. 4, pp. 431-440
    Contributions to Journals: Articles

  • Cannabinoid-mediated immunosuppression in experimental allergic encephalomyelitis

    Baker, D., Croxford, J. L., Pryce, G., Jackson, S. M., Ledent, C., Marsicano, G., Lutz, B., Giovannoni, G., Pertwee, R. G., Yamamura, T.
    Journal of Neuroimmunology, vol. 178, no. Suppl. 1, pp. 90-91
    Contributions to Journals: Articles

  • Cannabidiol-induced intracellular Ca2+ elevations in hippocampal cells

    Drysdale, A. J., Ryan, D., Pertwee, R. G., Platt, B.
    Neuropharmacology, vol. 50, no. 5, pp. 621-631
    Contributions to Journals: Articles

  • Cannabinoid pharmacology

    Pertwee, R. G.
    British Journal of Pharmacology, vol. 147, no. S1, pp. S163-S171
    Contributions to Journals: Articles

  • First "hybrid" ligands of vanilloid TRPV1 and cannabinoid CB2 receptors and non-polyunsaturated fatty acid-derived CB2-selective ligands

    Appendino, G., Cascio, M. G., Bacchiega, S., Moriello, A. S., Minassi, A., Thomas, A., Ross, R., Pertwee, R., De Petrocellis, L., Di Marzo, V.
    FEBS Letters, vol. 580, pp. 568-574
    Contributions to Journals: Articles

  • Novel compounds that interact with both leukotriene B-4 receptors and vanilloid TRPV1 receptors

    McHugh, D., McMaster, R. S., Pertwee, R. G., Roy, S., Mahadevan, A., Razdan, R. K., Ross, R. A.
    Journal of Pharmacology and Experimental Therapeutics, vol. 316, pp. 955-965
    Contributions to Journals: Articles

  • Role of cannabinoid receptors in the regulation of cardiac contractility during ischemia/reperfusion

    Maslov, L. N., Lasukova, O. V., Krylatov, A. V., Hanus, L. O., Pertwee, R. G., Ivanchuk, I. I., Crowford, D.
    Bulletin of Experimental Biology and Medicine, vol. 142, no. 5, pp. 557-561
    Contributions to Journals: Articles

  • Scopolamine and MK801-induced working memory deficits in rats are not reversed by CBD-rich cannabis extracts

    Fadda, P., Robinson, L., Fratta, W., Pertwee, R. G., Riedel, G.
    Behavioural Brain Research, vol. 168, pp. 307-311
    Contributions to Journals: Articles

  • The pharmacology of cannabinoid receptors and their ligands: an overview

    Pertwee, R. G.
    International Journal of Obesity, vol. 30, no. Supplement 1, pp. S13–S18
    Contributions to Journals: Articles

  • Evidence that the plant cannabinoid ¿9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist

    Thomas, A., Stevenson, L. A., Wease, K., Price, M., Baillie, G., Ross, R. A., Pertwee, R. G.
    British Journal of Pharmacology, vol. 146, no. 7, pp. 917-926
    Contributions to Journals: Articles

  • The bioassay of cannabinoids using the mouse isolated vas deferens

    Thomas, A., Pertwee, R. G.
    Marijuana and Medical Research: Methods and Protocols. Onaivi, E. (ed.). Humana Press, pp. 191-207
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Allosteric modulation of the cannabinoid CB1 receptor

    Price, M. R., Baillie, G. L., Thomas, A., Stevenson, L. A., Easson, M., Goodwin, R., McLean, A., McIntosh, L., Goodwin, G., Walker, G., Westwood, P., Marrs, J., Thomson, F., Cowley, P., Christopoulos, A., Pertwee, R. G., Ross, R. A.
    Molecular Pharmacology, vol. 68, no. 5, pp. 1484-1495
    Contributions to Journals: Articles

  • Cannabidiol as a potential medicine

    Pertwee, R. G.
    Cannabinoids as Therapeutics. Mechoulam, R. (ed.). Birkhaüser Verlag, pp. 47-65
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Sulfonamide cannabinoid agonists and antagonists

    Martin, B. R., Razdan, R. K., Pertwee, R. G.
    Patents: Patents

  • Cannabinoids

    Pertwee, R. G.
    Vol. 168, Springer Verlag, Heidelberg, Germany. 772 pages
    Books and Reports: Books

  • Cannabinoid receptors and their ligands

    Pertwee, R. G.
    Cannabinoids. Pertwee, R. G. (ed.). Springer Verlag, pp. 1-51
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Cannabinoid receptor antagonists SR141716 and SR144528 exhibit properties of partial agonists in experiments on isolated perfused rat heart

    Krylatov, A. V., Maslov, L. N., Lasukova, O. V., Pertwee, R. G.
    Bulletin of Experimental Biology and Medicine, vol. 139, pp. 558-561
    Contributions to Journals: Articles

  • Evidence that (-)-7-hydroxy-4 '-dimethylheptyl-cannabidiol activates a non-CB1, non-CB2, non-TRPV1 target in the mouse vas deferens

    Pertwee, R. G., Thomas, A., Stevenson, L. A., Maor, Y., Mechoulam, R.
    Neuropharmacology, vol. 48, pp. 1139-1146
    Contributions to Journals: Articles

  • Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase

    Vandevoorde, S., Saha, B., Mahadevan, A., Razdan, R. K., Pertwee, R. G., Martin, B. R., Fowler, C. J.
    Biochemical and Biophysical Research Communications, vol. 337, pp. 104-109
    Contributions to Journals: Articles

  • Synthesis of long-chain amide analogs of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716) with unique binding selectivities and pharmacological activities

    Thomas, B. F., Francisco, M. E. Y., Seltzman, H. H., Thomas, J. B., Fix, S. E., Schulz, A. K., Gilliam, A. F., Pertwee, R. G., Stevenson, L. A.
    Bioorganic & Medicinal Chemistry, vol. 13, pp. 5463-5474
    Contributions to Journals: Articles

  • The therapeutic potential of drugs that target cannabinoid receptors or modulate the tissue levels or actions of endocannabinoids

    Pertwee, R. G.
    The AAPS Journal, vol. 7
    Contributions to Journals: Literature Reviews

  • Angriffspunkte und Wirkungsmechanismen

    Pertwee, R. G.
    Cannabis und Cannabinoide: Pharmakologie Toxicologie und therapeutisches Potential. Grotenhermen, F. (ed.). Verlag Hans Huber, pp. 95-113
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • The pharmacology and therapeutic potential of cannabidiol

    Pertwee, R. G.
    Cannabinoids. Di Marzo, V. (ed.). . Kluwer Academic/Plenum Publishers, pp. 32-83
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Receptors and pharmacodynamics: natural and synthetic cannabinoids and endocannabinoids

    Pertwee, R. G.
    The Medicinal Uses of Cannabis and Cannabinoids. Guy, G., Whittle, B., Robson, P. (eds.). Pharmaceutical Press, pp. 103-139
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Cannabinoids and glaucoma

    Tomida, I., Pertwee, R. G., Azuara-Blanco, A.
    British Journal of Ophthalmology, vol. 88, no. 5, pp. 708-713
    Contributions to Journals: Articles

  • Differential effects of THC or CBD-rich cannabis extracts on working memory in rats

    Fadda, P., Robinson, L., Fratta, W., Pertwee, R. G., Riedel, G.
    Neuropharmacology, vol. 47, pp. 1170-1179
    Contributions to Journals: Articles

  • Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol

    Ghafouri, N., Tiger, G., Razdan, R. K., Mahadevan, A., Pertwee, R. G., Martin, B. R., Fowler, C. J.
    British Journal of Pharmacology, vol. 143, pp. 774-784
    Contributions to Journals: Articles

  • Pharmacological and therapeutic targets for Delta(9)-tetrahydrocannabinol and cannabidiol

    Pertwee, R. G.
    Euphytica, vol. 140, pp. 73-82
    Contributions to Journals: Articles

  • Selective cannabinoiod receptor agonist HU-210 decreases pump function of isolated perfused heart: Role of cAMP and cGMP

    Maslov, L. N., Lasukova, O. V., Krylatov, A. V., Uzhachenko, R. V., Pertwee, R.
    Bulletin of Experimental Biology and Medicine, vol. 138, pp. 550-553
    Contributions to Journals: Articles

  • Inverse agonism at cannabinoid receptors

    Pertwee, R. G.
    Inverse Agonism: Proceedings of the Esteve Foundation Symposium X, S'Agaró (Girona), Spain, 2-5 October 2002. Ijzerman, A. (ed.). Elsevier, pp. 75-86
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Cannabinoids

    Pertwee, R. G.
    Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. Munglani, R., Schmidt, W., Bountra, C. (eds.). Marcel Dekker, pp. 683-706
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Effects of delta-9-THC and WIN-55,212-2 on place preference in the water maze in rats

    Robinson, L., Hinder, L., Pertwee, R. G., Riedel, G.
    Psychopharmacology, vol. 166, no. 1, pp. 40-50
    Contributions to Journals: Articles

  • Lugares y mecanismos de acción

    Pertwee, R. G.
    Cannabis y Cannabinoides: Farmacología, toxicología y potencial terapéutico. Varo, R., Russo, E., Grotenhermen, F. (eds.). Haworth Press, pp. 95-113
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'

    Papahatjis, D. P., Nikas, S. P., Kourouli, T., Chari, R., Xu, W., Pertwee, R. G., Makriyannis, A.
    Journal of Medicinal Chemistry, vol. 46, pp. 3221-3229
    Contributions to Journals: Articles

  • Cannabinoids and multiple sclerosis

    Pertwee, R. G.
    Pharmacology & Therapeutics, vol. 95, no. 2, pp. 165-174
    Contributions to Journals: Articles

  • Localisation of cannabinoid CB1 receptor-immunoreactivity in the guinea-pig and rat myenteric plexus

    Coutts, A. A., Irving, A. J., Mackie, K., Pertwee, R. G., Anavi-Goffer, S.
    Journal of Comparative Neurology, vol. 448, no. 4, pp. 410-422
    Contributions to Journals: Articles

  • Pharmacological characterization of the anandamide cyclooxygenase metabolite

    Ross, R. A., Craib, S., Stevenson, L. A., Pertwee, R. G., Henderson, A., Toole, J., Ellington, H. C.
    Journal of Pharmacology and Experimental Therapeutics, vol. 301, no. 3, pp. 900-907
    Contributions to Journals: Articles

  • Functions of cannabinoid receptors in the hippocampus

    Davies, S. N., Pertwee, R. G., Riedel, G.
    Neuropharmacology, vol. 42, no. 8, pp. 993-1007
    Contributions to Journals: Articles

  • Sites and Mechanisms of Action

    Pertwee, R. G.
    Cannabis and Cannabinoids: Pharmacology Toxicology and Therapeutic Potential. Grotenhermen, F., Russo, E. (eds.). Haworth Press, pp. 73-87, 15 pages
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • New developments in the pharmacology of cannabinoids

    Pertwee, R. G.
    Trends in Drug Research III: Proceedings of the 13th Noordwijkerhout-Camerino Symposium. van der Goot, H. (ed.). Elsevier Science, pp. 249-258
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Cannabinoid receptors and their ligands

    Pertwee, R. G., Ross, R.
    Prostaglandins, Leukotrienes and Essential Fatty Acids, vol. 66, no. 2-3, pp. 101-121
    Contributions to Journals: Articles

  • Activation of cannabinoid receptors decreases the area of ischemic myocardial necrosis

    Ugdyzhekova, D. S., Krylatov, A. V., Bernatskaya, N. A., Maslov, L. N., Mechoulam, R., Pertwee, R. G.
    Bulletin of Experimental Biology and Medicine, vol. 133, pp. 125-126
    Contributions to Journals: Articles

  • Endogenous cannabinoids improve myocardial resistance to arrhythmogenic effects of coronary occlusion and reperfusion: a possible mechanism

    Krylatov, A. V., Uzhachenko, R. V., Maslov, L. N., Bernatskaya, N. A., Makriyannis, A., Mechoulam, R., Pertwee, R. G., Sal'nikova, O. M., Stefano, J. B., Lishmanov, Y. B.
    Bulletin of Experimental Biology and Medicine, vol. 133, pp. 122-124
    Contributions to Journals: Articles

  • International Union of Pharmacology.: XXVII. Classification of cannabinoid receptors

    Howlett, A. C., Barth, F., Bonner, T. I., Cabral, G., Casellas, P., Devane, W. A., Felder, C. C., Herkenham, M., Mackie, K., Martin, B. R., Mechoulam, R., Pertwee, R. G.
    Pharmacological Reviews, vol. 54, no. 2, pp. 161-202
    Contributions to Journals: Literature Reviews

  • Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB1 receptor antagonist N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716)

    Francisco, M. E. Y., Seltzman, H. H., Gilliam, A. F., Mitchell, R. A., Rider, S. L., Pertwee, R. G., Stevenson, L. A., Thomas, B. F.
    Journal of Medicinal Chemistry, vol. 45, pp. 2708-2719
    Contributions to Journals: Articles

  • The endogenous cannabinoid anandamide activates vanilloid receptors in the rat hippocampal slice

    Al-Hayani, A., Wease, K., Ross, R. A., Pertwee, R. G., Davies, S. N.
    Neuropharmacology, vol. 41, no. 8, pp. 1000-1005
    Contributions to Journals: Articles

  • A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus

    Craib, S., Ellington, H. C., Pertwee, R. G., Ross, R. A.
    British Journal of Pharmacology, vol. 134, no. 1, pp. 30-37
    Contributions to Journals: Articles

  • Cannabinoids and the gastrointestinal tract

    Pertwee, R. G.
    Gut, vol. 48, no. 6, pp. 859-867
    Contributions to Journals: Articles

  • Agonist-induced internalization and trafficking of cannabinoid CB1 receptors in hippocampal neurons

    Coutts, A. A., Anavi-Goffer, S., Ross, R. A., MacEwan, D. J., Mackie, K., Pertwee, R. G., Irving, A. J.
    Journal of Neuroscience, vol. 21, no. 7, pp. 2425-2433
    Contributions to Journals: Articles

  • Cannabinoid receptors and pain

    Pertwee, R. G.
    Progress in Neurobiology, vol. 63, no. 5, pp. 569-611
    Contributions to Journals: Articles

  • Endocannabinoids control spasticity in a multiple sclerosis model.

    Baker, D., Pryce, G., Croxford, J. L., Brown, P., Pertwee, R. G., Makriyannis, A., Khanolkar, A., Fezza, F., Bisogno, T., Di Marzo, V.
    The FASEB Journal, vol. 15, no. 2, pp. 300-302
    Contributions to Journals: Articles

  • Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens

    Ross, R. A., Gibson, T. M., Brockie, H. C., Leslie, M., Pashmi, G., Craib, S., Di Marzo, V., Pertwee, R. G.
    British Journal of Pharmacology, vol. 132, no. 3, pp. 631-640
    Contributions to Journals: Articles

  • Angriffspunkte und Wirkungsmechanismen: Targets and mechanisms of action

    Pertwee, R. G.
    Cannabis und Cannabinoide: Pharmakologie Toxicologie und therapeutisches Potential. Grotenhermen, F. (ed.). Huber-Verlag, pp. 93-107
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Actions of cannabinoid receptor ligands on rat cultured sensory neurones: implications for antinociception

    Ross, R. A., Coutts, A. A., McFarlane, S. M., Anavi-Goffer, S., Irving, A. J., Pertwee, R. G., MacEwan, D. J., Scott, R. H.
    Neuropharmacology, vol. 40, no. 2, pp. 221-232
    Contributions to Journals: Articles

  • Activation of type II cannabinoid receptors improves myocardial tolerance to arrhythmogenic effects of coronary occlusion and reperfusion

    Krylatov, A. V., Ugdyshekova, D. S., Bernatskaya, N. A., Maslov, L. N., Mekhoulam, R., Pertwee, R. G., Stephano, G. B.
    Bulletin of Experimental Biology and Medicine, vol. 131, pp. 523-525
    Contributions to Journals: Articles

  • Anandamide activates peripheral nociceptors in normal and arthritic rat knee joints

    Gauldie, S. D., McQueen, D. S., Pertwee, R., Chessell, I. P.
    British Journal of Pharmacology, vol. 132, pp. 617-621
    Contributions to Journals: Articles

  • Pharmacological actions and therapeutic uses of cannabis and cannabinoids

    Kumar, R. N., Chambers, W. A., Pertwee, R. G.
    Anaesthesia, vol. 56, pp. 1059-1068
    Contributions to Journals: Literature Reviews

  • Inhibition of nitric oxide production in RAW264.7 macrophages by cannabinoids and palmitoylethanolamide

    Ross, R. A., Brockie, H. C., Pertwee, R. G.
    European Journal of Pharmacology, vol. 401, no. 2, pp. 121-130
    Contributions to Journals: Articles

  • Functional expression of cell surface cannabinoid CB(1) receptors on presynaptic inhibitory terminals in cultured rat hippocampal neurons

    Irving, A. J., Coutts, A. A., Harvey, J., Rae, M. G., Mackie, K., Bewick, G. S., Pertwee, R. G.
    Neuroscience, vol. 98, no. 2, pp. 253-262
    Contributions to Journals: Articles

  • O-1057, a potent water-soluble cannabinoid receptor agonist with antinociceptive properties

    Pertwee, R. G., Gibson, T. M., Stevenson, L. A., Ross, R. A., Banner, W. K., Saha, B., Razdan, R. K., Martin, B. R.
    British Journal of Pharmacology, vol. 129, no. 8, pp. 1577-1584
    Contributions to Journals: Articles

  • Cannabinoid receptor ligands: clinical and neuropharmacological considerations, relevant to future drug discovery and development

    Pertwee, R. G.
    Expert Opinion on Investigational Drugs, vol. 9, pp. 1553-1571
    Contributions to Journals: Literature Reviews

  • Cannabinoids and pain modulation in animals and humans.

    Holdcroft, A., Hargreaves, K., Rice, A., Pertwee, R. G.
    Proceedings of the 9th World Congress on Pain,. Devor, M., Rowbotham, M., Wiesenfeld-Hallin, Z. (eds.). IASP Press, pp. 915-926
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Cannabinoids control spasticity and tremor in a multiple sclerosis model

    Baker, D., Pryce, G., Croxford, J. L., Brown, P., Pertwee, R. G., Huffman, J. W., Layward, L.
    Nature, vol. 404, pp. 84-87
    Contributions to Journals: Articles

  • Comparison of novel cannabinoid partial agonists and SR141716A in the guinea-pig small intestine

    Coutts, A. A., Brewster, N., Ingram, T., Razdan, R. K., Pertwee, R. G.
    British Journal of Pharmacology, vol. 129, pp. 645-652
    Contributions to Journals: Articles

  • Functional expression of cell surface cannabinoid CB1 receptors on presynaptic inhibitory terminals in cultured rat hippocampal neurons

    Irving, A. J., Coutts, A. A., Harvey, J., Rae, M. G., Mackie, K., Bewick, G. S., Pertwee, R. G.
    Neuroscience, vol. 98, pp. 253-262
    Contributions to Journals: Articles

  • Neuropharmacology and therapeutic potential of cannabinoids

    Pertwee, R. G.
    Addiction Biology, vol. 5, pp. 37-46
    Contributions to Journals: Literature Reviews

  • Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity

    De Petrocellis, L., Bisogno, T., Davis, J. B., Pertwee, R. G., Di Marzo, V.
    FEBS Letters, vol. 483, pp. 52-56
    Contributions to Journals: Articles

  • HU-308: A specific agonist for CB2, a peripheral cannabinoid receptor

    Hanus, L., Breuer, A., Tchilibon, S., Shiloah, S., Goldenberg, D., Horowitz, M., Pertwee, R. G., Ross, R. A., Mechoulam, R., Fride, E.
    PNAS, vol. 96, no. 25, pp. 14228-14233
    Contributions to Journals: Articles

  • Development of agonists, partial agonists and antagonists in the Delta(8)-tetrahydrocannabinol series

    Crocker, P. J., Saha, B., Ryan, W. J., Wiley, J. L., Martin, B. R., Ross, R. A., Pertwee, R. G., Razdan, R. K.
    Tetrahedron, vol. 55, no. 49, pp. 13907-13926
    Contributions to Journals: Articles

  • Structural determinants of the partial agonist-inverse agonist properties of 6'-azidohex-2'-yne-¿8-tetrahydrocannabinol at cannabinoid receptors

    Ross, R. A., Gibson, T. M., Stevenson, L. A., Saha, B., Crocker, P., Razdan, R. K., Pertwee, R. G.
    British Journal of Pharmacology, vol. 128, no. 3, pp. 735-743
    Contributions to Journals: Articles

  • Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1)

    Hillard, C. J., Manna, S., Greenberg, M. J., Dicamelli, R., Ross, R. A., Stevenson, L. A., Murphy, V., Pertwee, R. G., Campbell, W. B.
    Journal of Pharmacology and Experimental Therapeutics, vol. 289, no. 3, pp. 1427-1433
    Contributions to Journals: Articles

  • Design and synthesis of the CB1 selective cannabinoid antagonist AM281

    Lan, R. X., Lu, Q., Fan, P. S., Gatley, J., Volkow, N. D., Fernando, S. R., Pertwee, R. G., Makriyannis, A.
    AAPS PharmSci, vol. 1, no. 2, pp. 39-45
    Contributions to Journals: Articles

  • Cannabinoid receptors and their ligands in brain and other tissues

    Pertwee, R. G.
    Marihuana and Medicine. Nahas, G., Sutin, K., Harvey, D., Agurell, S. (eds.). Humana Press, pp. 177-185
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Agonist inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630

    Ross, R. A., Brockie, H. C., Stevenson, L. A., Murphy, V. L., Templeton, F., Makriyannis, A., Pertwee, R. G.
    British Journal of Pharmacology, vol. 126, no. 3, pp. 665-672
    Contributions to Journals: Articles

  • Cannabis and cannabinoids: Pharmacology and rationale for clinical use

    Pertwee, R. G.
    Forschende Komplementärmedizin, vol. 6, pp. 12-15
    Contributions to Journals: Articles

  • Evidence for the presence of CB1 cannabinoid receptors on peripheral neurones and for the existence of neuronal non-CB1 cannabinoid receptors

    Pertwee, R. G.
    Life Sciences, vol. 65, pp. 597-605
    Contributions to Journals: Articles

  • Medical uses of cannabinoids: the way forward

    Pertwee, R. G.
    Addiction, vol. 94, pp. 317-320
    Contributions to Journals: Editorials

  • Pharmacology of cannabinoid receptor ligands

    Pertwee, R. G.
    Current Medicinal Chemistry, vol. 6, pp. 635-664
    Contributions to Journals: Literature Reviews

  • Prescribing cannabinoids for multiple sclerosis - Current issues

    Pertwee, R. G.
    CNS Drugs, vol. 11, pp. 327-334
    Contributions to Journals: Articles

  • Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists

    Lan, R. X., Liu, Q., Fan, P. S., Lin, S. Y., Fernando, S. R., McCallion, D., Pertwee, R., Makriyannis, A.
    Journal of Medicinal Chemistry, vol. 42, pp. 769-776
    Contributions to Journals: Articles

  • Characterization of Cannabinoid Receptors in the Spleen and in Mast Cells

    Ross, R. A., Murphy, V., McKay, N., Ashford, M., Pertwee, R. G.
    Essential Fatty Acids and Eicosanoids: Proceedings of the 4th Int. Congress on Fatty Acids and Eicosanoids, Edinburgh. Riemersma, R., Armstrong, R., Kelly, R., Wilson, R. (eds.). AOCS Press, pp. 376-379
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Advances in cannabinoid receptor pharmacology

    Pertwee, R. G.
    Cannabis. The Genus Cannabis. Brown, D. (ed.). Harwood Academic Publishers, pp. 133-185
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Comparison of cannabinoid binding sites in guinea-pig forebrain and small intestine

    Ross, R. A., Brockie, H. C., Fernando, S. R., Saha, B., Razdan, R. K., Pertwee, R. G.
    British Journal of Pharmacology, vol. 125, no. 6, pp. 1345-1351
    Contributions to Journals: Articles

  • Interactions between synthetic vanilloids and the endogenous cannabinoid system

    Di Marzo, V., Bisogno, T., Melck, D., Ross, R. A., Brockie, H., Stevenson, L. A., Pertwee, R. G., De Petrocellis, L.
    FEBS Letters, vol. 436, no. 3, pp. 449-454
    Contributions to Journals: Articles

  • Correlation between cannabinoid mediated effects on paired pulse depression and induction of long term potentiation in the rat hippocampal slice

    Paton, G. S., Pertwee, R. G., Davies, S. N.
    Neuropharmacology, vol. 37, no. 9, pp. 1123-1130
    Contributions to Journals: Articles

  • Evidence that cannabinoid-induced inhibition of electrically evoked contractions of the myenteric plexus: longitudinal muscle preparation of guinea-pig small intestine can be modulated by Ca2+ and camp

    Coutts, A. A., Pertwee, R. G.
    Canadian Journal of Physiology and Pharmacology, vol. 76, no. 3, pp. 340-346
    Contributions to Journals: Articles

  • Cannabinoid Receptors

    Howlett, A., Bonner, T., Cabral, G., Casellas, P., Devane, W., Felder, C., Herkenham, M., Martin, B., Mechoulam, R., Pertwee, R. G.
    The IUPHAR Compendium of Receptor Characterization and Classification: International Union of Pharmacology Committee on Receptor Characterization and Classification. Girdlestone, D. (ed.). IUPHAR Media, pp. 97-104
    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Characterization of cannabinoid receptors in the spleen and in mast cells

    Ross, R. A., Murphy, V. L., McKay, N. G., Ashford, M. L. J., Pertwee, R. G.
    Chapters in Books, Reports and Conference Proceedings: Conference Proceedings

  • The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: Insights gained from (E)- and (Z)-naphthylidene indenes

    Reggio, P. H., Basu-Dutt, S., Barnett-Norris, J., Castro, M. T., Hurst, D. P., Seltzman, H. H., Roche, M. J., Gilliam, A. F., Thomas, B. F., Stevenson, L. A., Pertwee, R. G., Abood, M. E.
    Journal of Medicinal Chemistry, vol. 41, pp. 5177-5187
    Contributions to Journals: Articles

  • Evidence for the presence of CB2-like cannabinoid receptors on peripheral nerve terminals

    Griffin, G., Fernando, S. R., Ross, R. A., McKay, G., Ashford, M. L. J., Shire, D., Huffman, J. W., Yu, S., Lainton, J. A. H., Pertwee, R. G.
    European Journal of Pharmacology, vol. 339, no. 1, pp. 53-61
    Contributions to Journals: Articles

  • Therapeutic Uses of Cannabis

    Ashton, C., Holdcroft, A., Mars, S., Moffat, A., Pertwee, R. G., Wall, P.
    Harwood Academic Publishers, Amsterdam, Netherlands. 142 pages
    Books and Reports: Books

  • Synthesis and pharmacological comparison of dimethylheptyl and pentyl analogs of anandamide

    Seltzman, H. H., Fleming, D. N., Thomas, B. F., Gilliam, A. F., McCallion, D. S., Pertwee, R. G., Compton, D. R., Martin, B. R.
    Journal of Medicinal Chemistry, vol. 40, no. 22, pp. 3626-3634
    Contributions to Journals: Articles

  • Importance of the C-1 substituent in classical cannabinoids to CB2 receptor selectivity: Synthesis and characterization of a series of O,2-propano-Delta(8)-tetrahydrocannabinol analogs

    Reggio, P. H., Wang, T., Brown, A. E., Fleming, D. N., Seltzman, H. H., Griffin, G., Pertwee, R. G., Compton, D. R., Abood, M. E., Martin, R.
    Journal of Medicinal Chemistry, vol. 40, no. 20, pp. 3312-3318
    Contributions to Journals: Articles

  • Effects of cannabinoid receptor ligands on electrophysiological properties of myenteric neurones of the guinea-pig ileum

    LopezRedondo, F., Lees, G., Pertwee, R. G.
    British Journal of Pharmacology, vol. 122, no. 2, pp. 330-334
    Contributions to Journals: Articles

  • Evidence that methyl arachidonyl fluorophosphonate is an irreversible cannabinoid receptor antagonist

    Fernando, S. R., Pertwee, R. G.
    British Journal of Pharmacology, vol. 121, no. 8, pp. 1716-1720
    Contributions to Journals: Articles

  • Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus

    Coutts, A. A., Pertwee, R. G.
    British Journal of Pharmacology, vol. 121, no. 8, pp. 1557-1566
    Contributions to Journals: Articles
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