Δ9-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain

Thomas H. Burkey; Raymond M. Quock; Paul Consroe; William R. Roeske; Henry I. Yamamura

doi:10.1016/S0014-2999(97)00146-5

Δ⁹-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain

Thomas H. Burkey, Raymond M. Quock, Paul Consroe, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journal › Article › peer-review

57 Scopus citations

Abstract

We measured the ability of the cannabinoid agonists Δ⁹-tetrahydrocannabinol and R(+)-[2,3,-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]l-1,4-benzoxazin-yl]-(1-naphthalenyl) methanone mesylate (WIN 55,212-2) to stimulate guanosine 5'-O-(3-[³⁵S]thio)triphosphate ([³⁵S]GTPγS) binding in mouse brain membranes. Δ⁹-Tetrahydrocannabinol stimulated [³⁵S]GTPγS binding by about 25% as compared to WIN 55,212-2. This is the first report demonstrating that Δ⁹-tetrahydrocannabinol acts as a partial agonist in stimulating [³⁵S]GTPγS binding in the mouse brain.

Original language	English (US)
Pages (from-to)	R3-R4
Journal	European Journal of Pharmacology
Volume	323
Issue number	2-3
DOIs	https://doi.org/10.1016/S0014-2999(97)00146-5
State	Published - Apr 4 1997

Keywords

Brain, mouse
G-protein
Δ-Tetrahydrocannabinol

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/S0014-2999(97)00146-5

Cite this

@article{59d23c70f0c94033bf4d8448503b46ae,

title = "Δ9-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain",

abstract = "We measured the ability of the cannabinoid agonists Δ9-tetrahydrocannabinol and R(+)-[2,3,-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]l-1,4-benzoxazin-yl]-(1-naphthalenyl) methanone mesylate (WIN 55,212-2) to stimulate guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in mouse brain membranes. Δ9-Tetrahydrocannabinol stimulated [35S]GTPγS binding by about 25% as compared to WIN 55,212-2. This is the first report demonstrating that Δ9-tetrahydrocannabinol acts as a partial agonist in stimulating [35S]GTPγS binding in the mouse brain.",

keywords = "Brain, mouse, G-protein, Δ-Tetrahydrocannabinol",

author = "Burkey, {Thomas H.} and Quock, {Raymond M.} 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 the National Institute of Drug Abuse.",

year = "1997",

month = apr,

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doi = "10.1016/S0014-2999(97)00146-5",

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AU - Burkey, Thomas H.

AU - Quock, Raymond M.

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 the National Institute of Drug Abuse.

PY - 1997/4/4

Y1 - 1997/4/4

N2 - We measured the ability of the cannabinoid agonists Δ9-tetrahydrocannabinol and R(+)-[2,3,-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]l-1,4-benzoxazin-yl]-(1-naphthalenyl) methanone mesylate (WIN 55,212-2) to stimulate guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in mouse brain membranes. Δ9-Tetrahydrocannabinol stimulated [35S]GTPγS binding by about 25% as compared to WIN 55,212-2. This is the first report demonstrating that Δ9-tetrahydrocannabinol acts as a partial agonist in stimulating [35S]GTPγS binding in the mouse brain.

AB - We measured the ability of the cannabinoid agonists Δ9-tetrahydrocannabinol and R(+)-[2,3,-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo [1,2,3-de]l-1,4-benzoxazin-yl]-(1-naphthalenyl) methanone mesylate (WIN 55,212-2) to stimulate guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding in mouse brain membranes. Δ9-Tetrahydrocannabinol stimulated [35S]GTPγS binding by about 25% as compared to WIN 55,212-2. This is the first report demonstrating that Δ9-tetrahydrocannabinol acts as a partial agonist in stimulating [35S]GTPγS binding in the mouse brain.

KW - Brain, mouse

KW - G-protein

KW - Δ-Tetrahydrocannabinol

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