M1 Receptors

M1 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gq proteins. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS).

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3689 Cevimeline hydrochloride
Selective M1 agonist
1384 McN-A 343
Selective M1 muscarinic agonist
3569 Xanomeline oxalate
Functionally selective M1 agonist

Antagonists

Cat No Product Name / Activity
2853 Biperiden hydrochloride
Muscarinic receptor antagonist; some selectivity for M1
0469 Nitrocaramiphen hydrochloride
Muscarinic antagonist, M1 > M2
1071 Pirenzepine dihydrochloride
Selective M1 muscarinic antagonist
1122 Telenzepine dihydrochloride
Potent, selective M1 antagonist
3727 VU 0255035
Highly selective muscarinic M1 antagonist

Modulators

Cat No Product Name / Activity
4295 VU 0357017 hydrochloride
Positive allosteric modulator of M1 receptors

M1 receptors are members of the G-protein-coupled receptor (GPCR) family which are found mostly bound to Gq proteins. They are one of five muscarinic receptors that act to control the metabotropic functions of acetylcholine (ACh) in the central nervous system (CNS). M1 receptors are most densely populated in the neuronal cells of the cerebral cortex and hippocampus. Activation of the M1 receptor leads to several responses, including the upregulation of phospholipase C, the activation of ion channels such as K+ and Cl- and the inhibition of cAMP production. M1 receptor agonism can also lead to secretion (from the salivary gland, or stomach) and bronchoconstriction. Overall, M1 receptors are involved in numerous processes including the control of seizures, regulation the force of cardiac muscle contraction and most importantly mediating cognitive processes such as memory and learning.

M1 receptors are a well-known therapeutic target in the treatment of Alzheimer's Disease. Activation of the M1 receptor by selective agonists increases the secretion of non-toxic α-amyloid peptide and decreases harmful β-amyloid secretion from amyloid precursor proteins.

External sources of pharmacological information for M1 Receptors :

Literature for M1 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 highlights the targets and pathways representing the most promising strategies to pursue for novel drug development.

M1 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human CHRM1 NM_000738 P11229
Mouse Chrm1 NM_001112697 P12657
Rat Chrm1 NM_080773 P08482