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VU 0152100
- VU 152100
- Soluble in DMSO
- MF: C18H19N3O2S
- MW: 341.43
Description
VU 0152100 is a selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (CHRM4, M4 mAChR). It enhances receptor responses to endogenous acetylcholine without acting as a conventional orthosteric agonist.
Selective potentiation of M4 signaling enables investigation of cholinergic control of dopaminergic circuits and other CNS pathways while reducing interference from related muscarinic receptor subtypes. VU 0152100 is therefore a useful probe for M4 receptor allostery and therapeutic mechanism studies.
Key Features
- Selective M4 muscarinic receptor PAM
- Potentiates acetylcholine-dependent M4 signaling
- Acts through an allosteric rather than orthosteric binding mechanism
- Useful for studying cholinergic regulation of CNS circuitry
Applications
- M4 receptor pharmacology and allosteric modulation
- Muscarinic acetylcholine signaling studies
- Cholinergic–dopaminergic circuit research
- CNS drug-discovery and receptor-selectivity assays
More Information
| Parent CAS No. | 409351-28-6 |
|---|---|
| Chemical Name | 3-Amino-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxylic acid 4-methoxy-benzylamide |
| SMILES | C1C(C)=C2C(N)=C(C(NCC3C=CC(OC)=CC=3)=O)SC2=NC=1C |
| MFCD | MFCD02742972 |
| InChi | InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22) |
| InChiKey | MDNWGCQSCGNTKH-UHFFFAOYSA-N |
| CID | 864492 |
| Short Description | PAM of M4 mAChR |
References
- AE Brady et al. Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Ratss. J. Pharmacol. Exp. Ther. 2008, 327(3), 941–953.
- CM Jones. M4 Positive Allosteric Modulators For The Treatment Of Schizophrenia. Grant 1R01MH086601-01 from National Institute Of Mental Health.
- P Jeffrey Conn et al. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends in Pharmacological Sciences 2009, 30(3), 148-155.
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