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

@article{Hosohata1997AM630AO,
  title={AM630 antagonism of cannabinoid-stimulated [35S]GTP$\gamma$S binding in the mouse brain},
  author={Yoshiaki Hosohata and Raymond M. Quock and Keiko Hosohata and Alexandros Makriyannis and Paul F. Consroe and William R. Roeske and Henry I. Yamamura},
  journal={European Journal of Pharmacology},
  year={1997},
  volume={321}
}
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-y]-(1-naphthalenyl)methanone mesylate) on guanosine-5'-O-(3-[35S]thio) triphosphate ([35S]GTP gamma S) binding in mouse brain. WIN 55,212-2 stimulated [35S]GTP gamma S binding, while AM630 had no… Expand
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References

SHOWING 1-7 OF 7 REFERENCES
Cannabinoid receptor stimulation of guanosine-5'-O-(3-[35S]thio)triphosphate binding in rat brain membranes.
TLDR
Results demonstrate that [35S]GTP gamma S binding in the presence of excess GDP is an effective measure of cannabinoid receptor coupling to G-proteins in brain membranes. Expand
AM630, a competitive cannabinoid receptor antagonist.
TLDR
Differences in dissociation constant imply that the mouse vas deferens may contain more than one type of cannabinoid receptor, and that the receptors for which AM630 has the highest affinity may not be CB1 cannabinoid receptors. Expand
In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5'-[gamma-[35S]thio]-triphosphate binding.
  • L. Sim, D. Selley, S. Childers
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1995
TLDR
This technique provides a method of functional neuroanatomy that identifies changes in the activation of G proteins by specific receptors and suggests that variations in coupling efficiency may exist between different receptors in various brain regions. Expand
Further evidence for the presence of cannabinoid CB1 receptors in guinea‐pig small intestine
TLDR
The results support the hypothesis that guinea‐pig small intestine contains prejunctional cannabinoid CB1 receptors through which cannabinoids act to inhibit electrically‐evoked contractions by reducing release of the contractile transmitter, acetylcholine. Expand
Evidence for the presence of cannabinoid CB1 receptors in mouse urinary bladder
TLDR
The hypothesis that mouse urinary bladder contains prejunctional CB1 cannabinoid receptors which can mediate inhibition of electrically‐evoked contractions, probably by reducing contractile transmitter release is supported. Expand
SR141716A, a potent and selective antagonist of the brain cannabinoid receptor
TLDR
SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor and should prove to be a powerful tool for investigating the in vivo functions of the anandamide/cannabinoid system. Expand
Manual of Pharmacologic Calculations: With Computer Programs
Manual of Pharmacologic Calculations with Computer Programs. By R. J. Tallarida and R. B. Murray. New York, Heidelberg and Berlin, Springer‐Verlag, 1981. ix, 150 p. 24·5 cm. Unpriced.