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Chemical Compound Review:

AC1NSKBE 4-[6-methoxy-2-(4- methoxyphenyl)benzofuran...

Synonyms: CHEMBL411481, SureCN3736014, CTK8E8959, KB-188548, LY-320135, ...

Felder, C.C. et al., Holland, M. et al., Muthian, S. et al.

Muthian, Rademacher, Roelke, Gross, Hillard,

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Disease relevance of LY320135

4. The inhibitory effect of methanandamide on cyclic AMP accumulation was prevented by incubation of the arteries with pertussis toxin and was significantly reduced by LY320135, a selective CB1 antagonist, but not by SR 144528, a CB2-selective antagonist [1].

High impact information on LY320135

A second CB1 receptor antagonist, LY320135 (6 mg/kg), also significantly improved neurological function [2].
LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor [3].

Anatomical context of LY320135

The Ki values for LY320135 at the CB1 and CB2 receptors, transfected and stably expressed in cell lines, were 224 nM and > 10 microM, respectively [3].

References

Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Holland, M., John Challiss, R.A., Standen, N.B., Boyle, J.P. Br. J. Pharmacol. (1999) [Pubmed]
Anandamide content is increased and CB1 cannabinoid receptor blockade is protective during transient, focal cerebral ischemia. Muthian, S., Rademacher, D.J., Roelke, C.T., Gross, G.J., Hillard, C.J. Neuroscience (2004) [Pubmed]
LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. Felder, C.C., Joyce, K.E., Briley, E.M., Glass, M., Mackie, K.P., Fahey, K.J., Cullinan, G.J., Hunden, D.C., Johnson, D.W., Chaney, M.O., Koppel, G.A., Brownstein, M. J. Pharmacol. Exp. Ther. (1998) [Pubmed]

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