M4 Receptors
M4 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gi proteins, generally leading to inhibitory effects. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine in the CNS.
M4 Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 3569 | Xanomeline oxalate |
| Functionally biased muscarinic M4 receptor agonist | |
M4 Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 1671 | PD 102807 |
| Selective M4 antagonist | |
| 0909 | Tropicamide |
| Selective M4 antagonist | |
| 7658 | VU 6028418 hydrochloride |
| Potent and selective M4 mAChR antagonist | |
M4 Receptor Modulators |
|
| Cat. No. | Product Name / Activity |
| 7027 | LY 2033298 |
| Selective positive allosteric modulator of M4 receptors; active in vivo; antipsychotic | |
| 6964 | LY 2119620 |
| Positive allosteric modulator of M2 and M4 receptors | |
| 6932 | VU 0467485 |
| Potent and selective positive allosteric modulator of M4 receptors; orally bioavailable and brain penetrant | |
| 3141 | VU 10010 |
| Selective positive allosteric modulator of M4 receptors | |
| 3383 | VU 152100 |
| Positive allosteric modulator of M4 receptors | |
M4 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gi proteins, generally leading to inhibitory effects. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine in the CNS. M4 receptors are densely populated in the striatum and the lungs.
Activation of the M4 receptor leads to several responses, including the inhibition of adenylyl cyclase. One of the primary roles of M4 receptor activation is the indirect mediation of dopaminergic neurotransmission via its cholinergic activity. M4 activation has shown to inhibit D1-induced locomotor stimulation. Other functions of M4 receptor stimulation include wound healing and hair follicle cycling.
M4 receptors are involved in pathological processes including Parkinson's Disease, Alzheimer's Disease, and have also been implicated in several mood disorders including bipolar disorder and schizophrenia. The targeting of the M4 receptor has been suggested to have therapeutic potential for the treatment of these conditions.
External sources of pharmacological information for M4 Receptors :
Literature for M4 Receptors
Tocris offers the following scientific literature for M4 Receptors to showcase our products. We invite you to request* your copy today!
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