The molecular basis of cannabinoid activity.
Cannabinoids have been known to exhibit a wide variety of biological effects. Over the past fifty years numerous analogs were synthesized in an attempt to understand the structural requirements for each cannabinoid activity. Only recently, however, some important findings have focused new attention on this field of research. These findings include: (a) The development of novel "non-classical" potent cannabinoid analogs which exhibit similar pharmacological profiles with their "classical" counterparts; (b) The demonstration that there are specific cannabinoid binding sites in cell cultures as well as in mammalian brains; (c) Biophysical studies related to the interactions of cannabinoids with membranes which lead to a better understanding of those molecular properties which are required for cannabinoid activity; (d) Detailed and uniform pharmacological testing on a sizeable number of analogs allowing for a more detailed dissection of the cannabinoid effects and respective "structure activity relationships." The newly increased interest in cannabinoid research opens the door for a better understanding and potential treatment in cases of abuse as well as novel therapeutic opportunities through the design and synthesis of pharmacologically more selective analogs.
Makriyannis
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School of Pharmacy, University of Connecticut, Storrs 06269-3136.
Rapaka
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D000818:Animals; D001665:Binding Sites; D002186:Cannabinoids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects; D006801:Humans; D009271:Naltrexone / Q000031:analogs & derivatives / Q000494:pharmacology; D011453:Prostaglandins / Q000378:metabolism; D013329:Structure-Activity Relationship
D002186:Cannabinoids; D011453:Prostaglandins; D009271:Naltrexone; C066758:6-deoxy-6-fluoronaltrexone