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

doi:10.1016/S0014-2999(97)00047-2

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 journal › Article › peer-review

64 Scopus citations

Abstract

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 language	English (US)
Pages (from-to)	R1-R3
Journal	European Journal of Pharmacology
Volume	321
Issue number	1
DOIs	https://doi.org/10.1016/S0014-2999(97)00047-2
State	Published - Feb 19 1997

Keywords

AM630
Cannabinoid receptor antagonist
[S]GTPγS binding

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/S0014-2999(97)00047-2

Cite this

@article{eaa3258b3dff4931ace6b2deb57e6f85,

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

abstract = "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.",

keywords = "AM630, Cannabinoid receptor antagonist, [S]GTPγS binding",

author = "Yoshiaki Hosohata and Quock, \{Raymond M.\} and Keiko Hosohata and Alexandros Makriyannis and Paul Consroe and Roeske, \{William R.\} and Yamamura, \{Henry I.\}",

note = "Funding Information: This research was supported in part by grants from the Arizona Disease Control Research Commission and N.I.D.A.",

year = "1997",

month = feb,

day = "19",

doi = "10.1016/S0014-2999(97)00047-2",

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AU - Hosohata, Yoshiaki

AU - Quock, Raymond M.

AU - Hosohata, Keiko

AU - Makriyannis, Alexandros

AU - Consroe, Paul

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: This research was supported in part by grants from the Arizona Disease Control Research Commission and N.I.D.A.

PY - 1997/2/19

Y1 - 1997/2/19

N2 - 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.

AB - 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.

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KW - [S]GTPγS binding

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