AM630 antagonism of cannabinoid-stimulated [35S]GTPγS binding in the mouse brain

Yoshiaki Hosohata, Raymond M. Quock, Keiko Hosohata, Alexandros Makriyannis, Paul Consroe, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

62 Scopus citations


This research was designed to determine the action of the novel aminoalkylindole AM630 (6-iodo-pravadoline) at the cannabinoid receptor by studying its interaction with the cannabinoid receptor agonist WIN 55,212-2 (R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4 -benzoxazin-y1]-(1-naphthalenyl)methanone mesylate) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in mouse brain. WIN 55,212-2 stimulated [35S]GTPγS binding, while AM630 had no effect. AM630 antagonized WIN 55,212-2-induced [35S]GTPγS binding and shifted the WIN 55,212-2 dose-response curve to the right. These results clearly demonstrate that AM630 exerts cannabinoid receptor antagonist properties in the brain.

Original languageEnglish (US)
Pages (from-to)R1-R3
JournalEuropean Journal of Pharmacology
Issue number1
StatePublished - Feb 19 1997


  • AM630
  • Cannabinoid receptor antagonist
  • [S]GTPγS binding

ASJC Scopus subject areas

  • Pharmacology


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