AM630 is an inverse agonist at the human cannabinoid CB1 receptor

Robert S. Landsman; Alexandros Makriyannis; Hongfeng Deng; Paul Consroe; William R. Roeske; Henry I. Yamamura

doi:10.1016/S0024-3205(97)01187-9

AM630 is an inverse agonist at the human cannabinoid CB₁ receptor

Robert S. Landsman, Alexandros Makriyannis, Hongfeng Deng, Paul Consroe, William R. Roeske, Henry I. Yamamura

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

53 Scopus citations

Abstract

The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB₁ receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [³⁵S]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [³⁵S]GTPγS binding 77.9% with an EC₅₀ value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [³⁵S]GTPγS binding by 20.9% with an EC₅₀ value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

Original language	English (US)
Pages (from-to)	PL109-PL113
Journal	Life Sciences
Volume	62
Issue number	9
DOIs	https://doi.org/10.1016/S0024-3205(97)01187-9
State	Published - Jan 23 1998

Keywords

AM630
CHO cells
GTPγS
Human cannabinoid CB receptor
Inverse agonism
Inverse agonist
Negative intrinsic activity
WIN 55,212-2

ASJC Scopus subject areas

General Biochemistry, Genetics and Molecular Biology
Pharmacology, Toxicology and Pharmaceutics(all)

Access to Document

10.1016/S0024-3205(97)01187-9

Cite this

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title = "AM630 is an inverse agonist at the human cannabinoid CB1 receptor",

abstract = "The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [35S]GTPγS binding 77.9% with an EC50 value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [35S]GTPγS binding by 20.9% with an EC50 value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.",

keywords = "AM630, CHO cells, GTPγS, Human cannabinoid CB receptor, Inverse agonism, Inverse agonist, Negative intrinsic activity, WIN 55,212-2",

author = "Landsman, {Robert S.} and Alexandros Makriyannis and Hongfeng Deng and Paul Consroe and Roeske, {William R.} and Yamamura, {Henry I.}",

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T1 - AM630 is an inverse agonist at the human cannabinoid CB1 receptor

AU - Landsman, Robert S.

AU - Makriyannis, Alexandros

AU - Deng, Hongfeng

AU - Consroe, Paul

AU - Roeske, William R.

AU - Yamamura, Henry I.

PY - 1998/1/23

Y1 - 1998/1/23

N2 - The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [35S]GTPγS binding 77.9% with an EC50 value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [35S]GTPγS binding by 20.9% with an EC50 value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

AB - The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPγS binding to cell membranes was determined. WIN 55,212-2 (100 μM) stimulated basal [35S]GTPγS binding 77.9% with an EC50 value of 0.36 μM. Conversely, AM630 (100 μM) inhibited basal [35S]GTPγS binding by 20.9% with an EC50 value of 0.90 μM. These results show that WIN 55,212-2 is an agonist and AM630 is an inverse agonist in this system.

KW - AM630

KW - CHO cells

KW - GTPγS

KW - Human cannabinoid CB receptor

KW - Inverse agonism

KW - Inverse agonist

KW - Negative intrinsic activity

KW - WIN 55,212-2

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