![Professor Roger Pertwee Professor Roger Pertwee](/img/200x200/staffpages/uploads/pha040/roger-pertwee.jpg?size=4746)
Emeritus Professor
- About
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- 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
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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;
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the discovery of a cannabinoid CB1 receptor allosteric site;
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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;
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the pharmacological characterization of other phytocannabinoids, including cannabidiol, cannabidiolic acid & cannabigerol, and the further pharmacological characterization of THCV;
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the discovery/pharmacological characterization of novel synthetic cannabinoids many of which are widely used by cannabinoid researchers as experimental tools, e.g.
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methanandamide, the first CB1 receptor-selective agonist (with Dr Alexandros Makriyannis);
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two other CB1-selective agonists: ACEA & ACPA (with Dr Cecelia Hillard);
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HU-308, a CB2-selective agonist (with Dr Raphael Mechoulam);
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AM281, a widely-used CB1 receptor antagonist, and AM630, a widely-used CB2 receptor antagonist (with Dr Alexandros Makriyannis);
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CB1 receptor “neutral” antagonists;
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O-1057, the first water-soluble cannabinoid receptor ligand (with Drs Billy Martin and Raj Razdan);
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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
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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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A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus
British Journal of Pharmacology, vol. 134, no. 1, pp. 30-37Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0704223
Cannabinoids and the gastrointestinal tract
Gut, vol. 48, no. 6, pp. 859-867Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1136/gut.48.6.859
Agonist-induced internalization and trafficking of cannabinoid CB1 receptors in hippocampal neurons
Journal of Neuroscience, vol. 21, no. 7, pp. 2425-2433Contributions to Journals: ArticlesCannabinoid receptors and pain
Progress in Neurobiology, vol. 63, no. 5, pp. 569-611Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0301-0082(00)00031-9
Endocannabinoids control spasticity in a multiple sclerosis model.
The FASEB Journal, vol. 15, no. 2, pp. 300-302Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1096/fj.00-0399fje
Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens
British Journal of Pharmacology, vol. 132, no. 3, pp. 631-640Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0703850
Angriffspunkte und Wirkungsmechanismen: Targets and mechanisms of action
Cannabis und Cannabinoide: Pharmakologie Toxicologie und therapeutisches Potential. Grotenhermen, F. (ed.). Huber-Verlag, pp. 93-107Chapters in Books, Reports and Conference Proceedings: ChaptersActions of cannabinoid receptor ligands on rat cultured sensory neurones: implications for antinociception
Neuropharmacology, vol. 40, no. 2, pp. 221-232Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0028-3908(00)00135-0
Activation of type II cannabinoid receptors improves myocardial tolerance to arrhythmogenic effects of coronary occlusion and reperfusion
Bulletin of Experimental Biology and Medicine, vol. 131, pp. 523-525Contributions to Journals: ArticlesAnandamide activates peripheral nociceptors in normal and arthritic rat knee joints
British Journal of Pharmacology, vol. 132, pp. 617-621Contributions to Journals: ArticlesPharmacological actions and therapeutic uses of cannabis and cannabinoids
Anaesthesia, vol. 56, pp. 1059-1068Contributions to Journals: Literature ReviewsInhibition of nitric oxide production in RAW264.7 macrophages by cannabinoids and palmitoylethanolamide
European Journal of Pharmacology, vol. 401, no. 2, pp. 121-130Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0014-2999(00)00437-4
Functional expression of cell surface cannabinoid CB(1) receptors on presynaptic inhibitory terminals in cultured rat hippocampal neurons
Neuroscience, vol. 98, no. 2, pp. 253-262Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0306-4522(00)00120-2
O-1057, a potent water-soluble cannabinoid receptor agonist with antinociceptive properties
British Journal of Pharmacology, vol. 129, no. 8, pp. 1577-1584Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0703245
Cannabinoid receptor ligands: clinical and neuropharmacological considerations, relevant to future drug discovery and development
Expert Opinion on Investigational Drugs, vol. 9, pp. 1553-1571Contributions to Journals: Literature ReviewsCannabinoids and pain modulation in animals and humans.
Proceedings of the 9th World Congress on Pain,. Devor, M., Rowbotham, M., Wiesenfeld-Hallin, Z. (eds.). IASP Press, pp. 915-926Chapters in Books, Reports and Conference Proceedings: ChaptersCannabinoids control spasticity and tremor in a multiple sclerosis model
Nature, vol. 404, pp. 84-87Contributions to Journals: ArticlesComparison of novel cannabinoid partial agonists and SR141716A in the guinea-pig small intestine
British Journal of Pharmacology, vol. 129, pp. 645-652Contributions to Journals: ArticlesFunctional expression of cell surface cannabinoid CB1 receptors on presynaptic inhibitory terminals in cultured rat hippocampal neurons
Neuroscience, vol. 98, pp. 253-262Contributions to Journals: ArticlesNeuropharmacology and therapeutic potential of cannabinoids
Addiction Biology, vol. 5, pp. 37-46Contributions to Journals: Literature ReviewsOverlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity
FEBS Letters, vol. 483, pp. 52-56Contributions to Journals: ArticlesHU-308: A specific agonist for CB2, a peripheral cannabinoid receptor
PNAS, vol. 96, no. 25, pp. 14228-14233Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1073/pnas.96.25.14228
Development of agonists, partial agonists and antagonists in the Delta(8)-tetrahydrocannabinol series
Tetrahedron, vol. 55, no. 49, pp. 13907-13926Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0040-4020(99)00849-2
Structural determinants of the partial agonist-inverse agonist properties of 6'-azidohex-2'-yne-¿8-tetrahydrocannabinol at cannabinoid receptors
British Journal of Pharmacology, vol. 128, no. 3, pp. 735-743Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0702836
Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1)
Journal of Pharmacology and Experimental Therapeutics, vol. 289, no. 3, pp. 1427-1433Contributions to Journals: ArticlesDesign and synthesis of the CB1 selective cannabinoid antagonist AM281
AAPS PharmSci, vol. 1, no. 2, pp. 39-45Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1208/ps010204
Cannabinoid receptors and their ligands in brain and other tissues
Marihuana and Medicine. Nahas, G., Sutin, K., Harvey, D., Agurell, S. (eds.). Humana Press, pp. 177-185Chapters in Books, Reports and Conference Proceedings: ChaptersAgonist inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630
British Journal of Pharmacology, vol. 126, no. 3, pp. 665-672Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0702351
Cannabis and cannabinoids: Pharmacology and rationale for clinical use
Forschende Komplementärmedizin, vol. 6, pp. 12-15Contributions to Journals: ArticlesEvidence for the presence of CB1 cannabinoid receptors on peripheral neurones and for the existence of neuronal non-CB1 cannabinoid receptors
Life Sciences, vol. 65, pp. 597-605Contributions to Journals: ArticlesMedical uses of cannabinoids: the way forward
Addiction, vol. 94, pp. 317-320Contributions to Journals: EditorialsPharmacology of cannabinoid receptor ligands
Current Medicinal Chemistry, vol. 6, pp. 635-664Contributions to Journals: Literature ReviewsPrescribing cannabinoids for multiple sclerosis - Current issues
CNS Drugs, vol. 11, pp. 327-334Contributions to Journals: ArticlesStructure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists
Journal of Medicinal Chemistry, vol. 42, pp. 769-776Contributions to Journals: ArticlesCharacterization of Cannabinoid Receptors in the Spleen and in Mast Cells
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. 376-379Chapters in Books, Reports and Conference Proceedings: ChaptersAdvances in cannabinoid receptor pharmacology
Cannabis. The Genus Cannabis. Brown, D. (ed.). Harwood Academic Publishers, pp. 133-185Chapters in Books, Reports and Conference Proceedings: ChaptersComparison of cannabinoid binding sites in guinea-pig forebrain and small intestine
British Journal of Pharmacology, vol. 125, no. 6, pp. 1345-1351Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0702204
Interactions between synthetic vanilloids and the endogenous cannabinoid system
FEBS Letters, vol. 436, no. 3, pp. 449-454Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0014-5793(98)01175-2
Correlation between cannabinoid mediated effects on paired pulse depression and induction of long term potentiation in the rat hippocampal slice
Neuropharmacology, vol. 37, no. 9, pp. 1123-1130Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0028-3908(98)00096-3
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
Canadian Journal of Physiology and Pharmacology, vol. 76, no. 3, pp. 340-346Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1139/cjpp-76-3-340
Cannabinoid Receptors
The IUPHAR Compendium of Receptor Characterization and Classification: International Union of Pharmacology Committee on Receptor Characterization and Classification. Girdlestone, D. (ed.). IUPHAR Media, pp. 97-104Chapters in Books, Reports and Conference Proceedings: ChaptersCharacterization of cannabinoid receptors in the spleen and in mast cells
Chapters in Books, Reports and Conference Proceedings: Conference ProceedingsThe bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: Insights gained from (E)- and (Z)-naphthylidene indenes
Journal of Medicinal Chemistry, vol. 41, pp. 5177-5187Contributions to Journals: ArticlesEvidence for the presence of CB2-like cannabinoid receptors on peripheral nerve terminals
European Journal of Pharmacology, vol. 339, no. 1, pp. 53-61Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1016/S0014-2999(97)01336-8
Therapeutic Uses of Cannabis
Harwood Academic Publishers, Amsterdam, Netherlands. 142 pagesBooks and Reports: BooksSynthesis and pharmacological comparison of dimethylheptyl and pentyl analogs of anandamide
Journal of Medicinal Chemistry, vol. 40, no. 22, pp. 3626-3634Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1021/jm9702950
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
Journal of Medicinal Chemistry, vol. 40, no. 20, pp. 3312-3318Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1021/jm970136g
Effects of cannabinoid receptor ligands on electrophysiological properties of myenteric neurones of the guinea-pig ileum
British Journal of Pharmacology, vol. 122, no. 2, pp. 330-334Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0701393
Evidence that methyl arachidonyl fluorophosphonate is an irreversible cannabinoid receptor antagonist
British Journal of Pharmacology, vol. 121, no. 8, pp. 1716-1720Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0701303
Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus
British Journal of Pharmacology, vol. 121, no. 8, pp. 1557-1566Contributions to Journals: Articles- [ONLINE] DOI: https://doi.org/10.1038/sj.bjp.0701301