An investigation into the structural determinants of cannabinoid receptor ligand efficacy

A number of side‐chain analogues of Δ8‐THC were tested in GTPγS binding assay in rat cerebellar membranes. O‐1125, a saturated side‐chain compound stimulated GTPγS binding with an Emax of 165.0%, and an EC50 of 17.4 nM. O‐1236, O‐1237 and O‐1238, three‐enyl derivatives containing a cis carbon‐carbon...

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Veröffentlicht in:	British journal of pharmacology 1999-04, Vol.126 (7), p.1575-1584
Hauptverfasser:	Griffin, Graeme, Wray, Emma J, Rorrer, William K, Crocker, Peter J, Ryan, William J, Saha, Bijali, Razdan, Raj K, Martin, Billy R, Abood, Mary E
Format:	Artikel
Sprache:	eng
Schlagworte:	[35S]‐GTPγS binding agonist Animals antagonist Biological and medical sciences Cannabinoid receptors Dose-Response Relationship, Drug Dronabinol - analogs & derivatives Dronabinol - pharmacology efficacy Guanosine 5'-O-(3-Thiotriphosphate) - metabolism G‐proteins Male Medical sciences Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors partial agonist Pharmacology. Drug treatments Piperidines - pharmacology Pyrazoles - pharmacology Radioligand Assay rat cerebellum Rats Rats, Sprague-Dawley Receptors, Cannabinoid Receptors, Drug - drug effects Receptors, Drug - metabolism Structure-Activity Relationship
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