CB1 Receptors

The CB1 receptor, also known as the central cannabinoid receptor, is a member of the cannabinoid receptor group of G-protein-coupled receptors that also includes CB2 and GPR55. CB1 receptors are found mainly in the terminals of central and peripheral neurons.

Products
Background
Literature (2)
Gene Data

CB1 Receptor Agonists

Cat. No. Product Name / Activity
1319 ACEA
Potent and highly selective CB1 agonist

CB1 Receptor Inverse Agonists

Cat. No. Product Name / Activity
3791 Hemopressin (human, mouse)
Selective CB1 inverse agonist
0923 SR 141716A
Selective CB1 inverse agonist
7131 TM 38837
Highly potent CB1 inverse agonist; peripherally restricted

CB1 Receptor Antagonists

Cat. No. Product Name / Activity
1117 AM 251
Potent CB1 antagonist; also GPR55 agonist
6193 AM 4113
High affinity and selective CB1 antagonist
5443 AM 6545
High affinity and selective CB1 antagonist
4236 CP 945598 hydrochloride
CB1 antagonist
5746 NESS 0327
Ultra-high affinity and selective CB1 antagonist

CB1 Receptor Modulators

Cat. No. Product Name / Activity
2957 Org 27569
Potent allosteric modulator of CB1 receptors
5321 PSNCBAM-1
Negative allosteric modulator of CB1 receptors

Other

Cat. No. Product Name / Activity
2540 Tocrifluor T1117
Fluorescent cannabinoid ligand; fluorescent form of AM 251 (Cat. No. 1117)

The CB1 receptor, also known as the central cannabinoid receptor, is a member of the cannabinoid receptor group of G-protein-coupled receptors that also includes CB2 and GPR55. CB1 receptors are found mainly in the terminals of central and peripheral neurons, where they usually mediate inhibition of neurotransmitter release. They can also be present on some non-neuronal cells, including immune cells.

CB1 receptor antagonists are drugs that bind to the CB1 receptor and prevent its activation by endogenous cannabinoid receptor agonists (known as endocannabinoids). Some CB1 cannabinoidergic compounds, such as SR 141716A (Rimonabant), can produce inverse cannabimimetic effects when administered alone, they are known as CB1 receptor inverse agonists. CB1 receptor competitive antagonists, that lack any detectable ability to induce signs of inverse agonism, have also been developed.

The endocannabinoid system (endocannabinoids and their associated receptor proteins) is highly relevant in the control of metabolism and energy balance. Hyperactivity of the endocannabinoid system is associated with obesity; several CB1 receptor antagonists and inverse agonists have been developed in an attempt to reduce endocannabinoid signaling. Animal studies have shown that both food intake and body weight can be significantly reduced by blocking the CB1 receptor.

External sources of pharmacological information for CB1 Receptors :

Literature for CB1 Receptors

Tocris offers the following scientific literature for CB1 Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.

CB1 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human CNR1 NM_033181 P21554
Mouse Cnr1 NM_007726 P47746
Rat Cnr1 NM_012784 P20272