Agonist-antagonist characterization of 6'-cyanohex-2'-yne-delta 8-tetrahydrocannabinol in two isolated tissue preparations.

European Journal of Pharmacology
R G PertweeB R Martin

Abstract

This investigation was directed at characterizing some of the pharmacological properties of 6'-cyanohex-2'-yne-delta 8-tetrahydrocannabinol (O-823), a compound with high affinity for cannabinoid binding sites (Ki = 0.77 nM). In mouse vasa deferentia, O-823 behaved as a potent partial cannabinoid CB1 receptor agonist (EC50 = 0.015 nM). In the guinea-pig myenteric plexus preparation, it antagonized WIN 55.212-2 [(R)-(+)-[2,3-dihydro-5-methyl-3-[(4-morpholino)methyl]pyrrolo-[1,2,3-de ]-1, 4-benzoxazin-6-yl](1-naphthyl)methanone] and CP 55.940 [(-)-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4-(3-hydroxypropyl ) cyclohexan-1-ol] with Kd values of 0.65 and 0.27 nM, respectively. After in vivo delta 9-tetrahydrocannabinol pretreatment. the sensitivity of vasa deferentia to O-823-induced inhibition of electrically evoked contractions was reduced by 127-fold. 3.162 nM O-823 was inhibitory in unpretreated vasa deferentia but antagonized CP 55,940 in pretreated tissues (Kd = 0.26 nM). O-823 is probably an antagonist in the myenteric plexus preparation and delta 9-tetrahydro-cannabinol pretreated vasa deferentia but a partial agonist in unpretreated vasa deferentia because the first two of these preparations contain fewer receptors than th...Continue Reading

References

Mar 1, 1986·Pharmacological Reviews·L E Hollister
Jan 1, 1994·Pharmacology, Biochemistry, and Behavior·F Rodríguez de FonsecaJ A Ramos
Aug 1, 1996·British Journal of Pharmacology·R G PertweeA A Coutts

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Citations

Mar 23, 2004·European Journal of Pharmacology·Adèle ThomasRoger G Pertwee
Nov 27, 2002·European Journal of Pharmacology·Roger G PertweeAdèle Thomas
Feb 5, 1998·European Journal of Pharmacology·G GriffinR G Pertwee
Jan 1, 1997·Pharmacology & Therapeutics·R G Pertwee
Nov 8, 2001·Trends in Pharmacological Sciences·E Schlicker, M Kathmann
May 14, 1999·British Journal of Pharmacology·G GriffinM E Abood
Oct 12, 1999·British Journal of Pharmacology·G GriffinM E Abood
Jul 26, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Hester van DiepenMartin C Michel
Jan 20, 2017·ACS Chemical Neuroscience·Robert B LaprairieGanesh A Thakur
Jan 1, 2000·Addiction Biology·R G Pertwee
Aug 23, 2007·Chemistry & Biodiversity·Eric Stern, Didier M Lambert

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