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.
CB1 Receptor Agonists |
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|---|---|
| Cat. No. | Product Name / Activity |
| 1319 | ACEA |
| Potent and highly selective CB1 agonist | |
CB1 Receptor Inverse Agonists |
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| Cat. No. | Product Name / Activity |
| 1115 | AM 281 |
| Potent and selective CB1 inverse agonist | |
| 3791 | Hemopressin (human, mouse) |
| Selective CB1 inverse agonist | |
| 2387 | LY 320135 |
| Selective CB1 inverse agonist | |
| 0923 | SR 141716A |
| Selective CB1 inverse agonist | |
| 7131 | TM 38837 |
| Highly potent CB1 inverse agonist; peripherally restricted | |
CB1 Receptor Antagonists |
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| 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 | |
| 6763 | AVE 1625 |
| Potent and selective CB1 receptor 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 |
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| 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
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
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.
Our Cannabinoid review gives an overview of the pharmacological ligands used to study the cannabinoid CB1 and CB2 receptors.
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Written by Prof David Nutt, this poster summarizes the brain circuits and neurotransmitter systems that are affected by the main classes of addictive drugs.
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