Cannabinoid drugs structure-activity relationships

Makriyannis A, Banijamali A, Van der Schyf C, Jarrell H. The role of cannabinoid stereochemistry and absolute configuration and the orientation of A9-THC in the membrane bilayer. Structure-activity relationships of cannabinoids. In Rapaka RS, Makriyannis A, eds. Interactions of Cannabinoids with Membranes. National Institute on Drug Abuse Research Monograph 79. Rockville, MD US Department of Health and Human Services, 1987. 

Much progress has recently been made in our understanding of structure-activity relationships of cannabinoids. In view of the current interest in the clinical usefulness of these compounds as analgesics, Chapter 5 gives a timely survey of present scientific knowledge of these drugs. 

Melvin LS, MUne GM, Johnson MR, Wilken GH, Howlett AC (1995) Structure-activity relationships defining the ACD-tricyclic cannabinoids cannabinoid receptor binding and analgesic activity. Drug Des Discov 13 155-166... 

Osgood PF, Howes JF, Razdan RK, Pars HG (1978) Drugs derived from cannabinoids. 7. Tachycardia and analgesia structure-activity relationships in 4 9-tetrahydrocannabinol and some synthetic analogues. J Med Chem 21 809-811... 

The best recent reference on the SAR is Structure Activity Relationships of the Cannabinoids edited by R. Rapaka-NIDA Research Monograph 79 (1987) published by the National Institute on Drug Abuse. Especially interesting is the article on nonclassical compounds by Melvin and Johnson. 

Many of these synthetic cannabinoids are used in pharmacological studies involving structure-activity relationships, receptor binding studies, and detailed mechanisms of action of these drugs. Some synthetic cannabinoids have been used for medicinal purposes including rimonabant, nabilone, and dronabinol. Rimonabant is a selective CBl receptor antagonist which was used to treat obesity for some time, but was withdrawn from the market because it showed severe side effects such as severe depression [70]. Rimonabant was the first selective CBl receptor blocker to be approved for use... 

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