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
Gene Data

Antagonists

Cat No Product Name / Activity
1671 PD 102807
Selective M4 antagonist
0909 Tropicamide
Selective M4 muscarinic antagonist

Modulators

Cat No Product Name / Activity
3141 VU 10010
Selective allosteric potentiator 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

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Alzheimer's

Alzheimer's Poster

Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Learning & Memory

Learning & Memory Poster

Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.

Schizophrenia

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.

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