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 Receptor Agonists |
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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 | |
M1 Receptor Antagonists |
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Cat. No. | Product Name / Activity |
2853 | Biperiden hydrochloride |
Muscarinic receptor antagonist; some selectivity for M1 | |
1071 | Pirenzepine dihydrochloride |
Selective M1 antagonist | |
1122 | Telenzepine dihydrochloride |
Potent, selective M1 antagonist | |
3727 | VU 0255035 |
Highly selective M1 antagonist | |
M1 Receptor Modulators |
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Cat. No. | Product Name / Activity |
6872 | BQCA |
Positive allosteric modulator of M1 receptors | |
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.
Tocris offers the following scientific literature for M1 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 (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.
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 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.