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.

Products
Background
Literature (1)
Gene Data

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
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
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!

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


Alzheimer's Disease Poster

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.

M4 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human CHRM4 NM_000741 P08173
Mouse Chrm4 NM_007699 P32211
Rat Chrm4 NM_031547 P08485