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 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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
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 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 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 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.
Written by Alan Palmer
Our Alzheimer's disease poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease.
Request copyDownload PDFWritten by J.J. Maguire and A.P. Davenport
Our Cardiovascular poster highlights the key G protein-coupled receptors involved in the regulation of vascular reactivity.
Request copyDownload PDFWritten by Clea Warburton and Zafar Bashir
Our Learning and Memory poster gives an overview of the cellular mechanisms underlying recognition memory and its links to long-term depression.
Request copyDownload PDFWritten by Justin M. Saunders and Javier González-Maeso
Our Schizophrenia poster highlights the targets and pathways representing the most promising strategies to pursue for novel drug development.
Request copyDownload PDF