Professor Roger Pertwee

Professor Roger Pertwee

Emeritus Professor

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Professor Roger Pertwee
Professor Roger Pertwee

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

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

Publications 

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  • Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity

    Brizzi, A., Aiello, F., Boccella, S., Cascio, M. G., De Petrocellis, L., Frosini, M., Gado, F., Ligresti, A., Luongo, L., Marini, P., Mugnaini, C., Pessina, F., Corelli, F., Maione, S., Manera, C., Pertwee, R. G., Di Marzo, V.

    Bioorganic and Medicinal Chemistry, vol. 28, no. 11, 115513

    Contributions to Journals: Articles

  • Anticancer effects of n-3 EPA and DHA and their endocannabinoid derivatives on breast cancer cell growth and invasion

    Brown, I., Lee, J., Sneddon, A. A., Cascio, M. G., Pertwee, R. G., Wahle, K. W., Rotondo, D., Heys, S. D.

    Prostaglandins, Leukotrienes and Essential Fatty Acids, vol. 156, pp. 102024

    Contributions to Journals: Articles

  • Disease associated polymorphisms within the conserved ECR1 enhancer differentially regulate the tissue specific activity of the cannabinoid‐1 receptor gene promoter; implications for cannabinoid pharmacogenetics

    Hay, E. A., Cowie, P., McEwan, A. R., Ross, R., Pertwee, R. G., MacKenzie, A.

    Human Mutation, vol. 41, no. 1, pp. 291-298

    Contributions to Journals: Articles

  • Fatty acid suppression of glial activation prevents central neuropathic pain after spinal cord injury

    Georgieva, M., Wei, Y., Dumitrascuta, M., Pertwee, R., Finnerup, N. B., Huang, W.

    Pain, vol. 160, no. 12, pp. 2724-2742

    Contributions to Journals: Articles

  • Disruption of an enhancer associated with addictive behaviour within the cannabinoid receptor-1 gene suggests a possible role in alcohol intake, cannabinoid response and anxiety-related behaviour

    Hay, E. A., McEwan, A., Wilson, D., Barrett, P., D'Agostino, G., Pertwee, R. G., MacKenzie, A.

    Psychoneuroendocrinology, vol. 109, pp. 104407

    Contributions to Journals: Articles

  • A synthetic analogue of cannabidiolic acid that acts like a positive allosteric modulator at 5-HT1A receptors

    Alcina, A. G., Stevenson, L. A., Haj, C., Smoum, R., Mechoulam, R., Hislop, J. N., Pertwee, R. G.

    British-Pharmacology-Society Meeting (Pharmacology), pp. 3011-3012

    Contributions to Journals: Abstracts

  • Identification of the First Synthetic Allosteric Modulator of the CB2 Receptors and Evidence of Its Efficacy for Neuropathic Pain Relief

    Gado, F., Di Cesare Mannelli, L., Lucarini, E., Bertini, S., Cappelli, E., Digiacomo, M., Stevenson, L. A., Macchia, M., Tuccinardi, T., Ghelardini, C., Pertwee, R. G., Manera, C.

    Journal of Medicinal Chemistry, vol. 62, no. 1, pp. 276-287

    Contributions to Journals: Articles

  • Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or Dependence

    Slivicki, R. A., Xu, Z., Kulkarni, P. M., Pertwee, R. G., Mackie, K., Thakur, G. A., Hohmann, A. G.

    Biological Psychiatry, vol. 84, no. 10, pp. 722-733

    Contributions to Journals: Articles

  • Synthesis, radio-synthesis and in vitro evaluation of terminally fluorinated derivatives of HU-210 and HU-211 as novel candidate PET tracers

    Zanato, C., Pelagalli, A., Marwick, K. F. M., Piras, M., Dall'Angelo, S., Spinaci, A., Pertwee, R. G., Wyllie, D. J. A., Hardingham, G. E., Zanda, M.

    Organic & Biomolecular Chemistry, vol. 15, no. 9, pp. 2086-2096

    Contributions to Journals: Articles

  • The pharmacology and therapeutic potential of plant cannabinoids

    Cascio, M. G., Pertwee, R. G., Marini, P.

    Cannabis sativa L. - Botany and Biotechnology. Chandra, S., Lata, H., ElSohly, M. (eds.). Springer, Biomedicine & Life Sciences, pp. 207-225, 19 pages

    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe

    Laprairie, R. B., Kulkarni, A. R., Kulkarni, P. M., Hurst, D. P., Lynch, D., Reggio, P. H., Janero, D. R., Pertwee, R. G., Stevenson, L. A., Kelly, M. E. M., Denovan-Wright, E. M., Thakur, G. A.

    ACS Chemical Neuroscience, vol. 7, no. 6, pp. 776-798

    Contributions to Journals: Articles

  • The Displacement Binding Assay Using Human Cannabinoid CB2 Receptor-Transfected Cells

    Cascio, M. G., Marini, P., Pertwee, R. G.

    Endocannabinoid Signaling. Maccarrone, M. (ed.). Springer Science+Business Media, pp. 57-63, 7 pages

    Chapters in Books, Reports and Conference Proceedings: Chapters

  • Effect of cannabis on glutamate signalling in the brain: A systematic review of human and animal evidence

    Colizzi, M., McGuire, P., Pertwee, R. G., Bhattacharyya, S.

    Neuroscience & Biobehavioral Reviews, vol. 64, pp. 359-381

    Contributions to Journals: Literature Reviews

  • Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s)

    Kulkarni, P. M., Kulkarni, A. R., Korde, A., Tichkule, R. B., Laprairie, R. B., Denovan-Wright, E. M., Zhou, H., Janero, D. R., Zvonok, N., Makriyannis, A., Cascio, M. G., Pertwee, R. G., Thakur, G. A.

    Journal of Medicinal Chemistry, vol. 59, no. 1, pp. 44-60

    Contributions to Journals: Articles

  • The Cyclic AMP Assay Using Human Cannabinoid CB2 Receptor-Transfected Cells

    Marini, P., Cascio, M. G., Pertwee, R. G.

    Endocannabinoid Signaling. Maccarrone, M. (ed.). Springer Science+Business Media, pp. 85-93, 9 pages

    Chapters in Books, Reports and Conference Proceedings: Chapters

  • CB2 cannabinoid receptor agonist enantiomers HU-433 and HU-308: An inverse relationship between binding affinity and biological potency

    Smoum, R., Baraghithy, S., Chourasia, M., Breuer, A., Mussai, N., Attar-Namdar, M., Kogan, N. M., Raphael, B., Bolognini, D., Cascio, M. G., Marini, P., Pertwee, R. G., Shurki, A., Mechoulam, R., Bab, I.

    PNAS, vol. 112, no. 28, pp. 8774-8779

    Contributions to Journals: Articles

  • Modulation of food consumption and sleep-wake cycle in mice by the neutral CB1 antagonist ABD459

    Goonawardena, A. V., Plano, A., Robinson, L., Ross, R., Greig, I., Pertwee, R. G., Hampson, R. E., Platt, B., Riedel, G.

    Behavioural Pharmacology, vol. 26, no. 3, pp. 289-303

    Contributions to Journals: Articles

  • Are cannabidiol and Delta(9)-tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review

    McPartland, J. M., Duncan, M., Di Marzo, V., Pertwee, R. G.

    British Journal of Pharmacology, vol. 172, no. 3, pp. 737-753

    Contributions to Journals: Literature Reviews

  • Early phytocannabinoid chemistry to endocannabinoids and beyond

    Mechoulam, R., Hanus, L. O., Pertwee, R., Howlett, A. C.

    Nature reviews neuroscience, vol. 15, no. 11, pp. 757-764

    Contributions to Journals: Articles

  • Pyrazoles with a "click" 4-[N-(4-fluorobutyl)-1,2,3-triazole] substituent in position 3 are nanomolar CB1 receptor ligands

    Distinto, R., Zanato, C., Montanari, S., Cascio, M. G., Lazzari, P., Pertwee, R., Zanda, M.

    Journal of Fluorine Chemistry, vol. 167, pp. 184-191

    Contributions to Journals: Articles

  • Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist

    Brizzi, A., Aiello, F., Marini, P., Cascio, M. G., Corelli, F., Brizzi, V., De Petrocellis, L., Ligresti, A., Luongo, L., Lamponi, S., Maione, S., Pertwee, R. G., Di Marzo, V.

    Behavioral and Brain Sciences, vol. 22, no. 17, pp. 4770-4783

    Contributions to Journals: Articles

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