Product Feature - Cannabinoid Receptors

Two types of cannabinoid receptor have so far been identified. These are the CB₁ receptor, cloned in 1990, and the CB₂ receptor, cloned in 1993, both of which are members of the superfamily of G-protein-coupled receptors. The cloning of these receptors prompted the development of mice from which cannabinoid CB₁ and/or CB₂ receptors have been genetically deleted and these transgenic animals, particularly CB₁ knockout mice, are now widely used to explore physiological and pathological functions of cannabinoid receptors.

Extract taken from Tocris' new review on cannabinoid receptors written by a leading researcher in the field, Roger Pertwee.

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Key cannabinoid receptor compounds now available from Tocris include:

Potent CB₁ and CB₂ agonist
0949 l CP 55,940
Considerably more potent than Δ⁹-THC in both behavioural tests and receptor binding assays. Displays high and roughly equal affinity for both central and peripheral cannabinoid receptors.
Related Products: WIN 55,212-2 HU 210 Anandamide

Potent, selective CB₁ antagonist/inverse agonist
1117 l AM 251
Displays a K_i value of 7.49 nM at CB₁ receptors and is 306-fold selective over CB₂ receptors.
Related Products: AM 281 ACEA

CB₂ selective antagonist/inverse agonist
1115 l AM 630
165-fold selective over CB₁ receptors. Behaves as a weak partial/inverse agonist at CB₁ receptors.
Related Products: JWH 133 JTE 907 JWH 015

View all Cannabinoid Receptor Related Products.

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Cannabinoid Receptor Ligands

More Cannabinoid Receptor Compounds

GPR55, a new cannabinoid receptor?

Roger Pertwee reviews the evidence for GPR55; a proposed new CB receptor. (more)