Selective positive allosteric modulator of M4 receptors; active in vivo; antipsychotic
| Cas No. | 886047-13-8 |
| 别名 | 3-氨基-5-氯-N-环丙基-6-甲氧基-4-甲基噻吩并[2,3-B]吡啶-2-羧酰胺 |
| Canonical SMILES | NC1=C(C(NC2CC2)=O)SC3=NC(OC)=C(Cl)C(C)=C31 |
| 分子式 | C13H14ClN3O2S |
| 分子量 | 311.79 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Selective positive allosteric modulator of M4 receptor (KB = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold. Exhibits no effect at hM1/3/5 receptors and a small effect at hM2 (KB = 1 μM α = 3.7). Potentiates other full and partial orthosteric agonists, including Carbachol, Oxotremorine-M, and McN-A343. Does not affect binding of antagonist NMS. Active in vivo. Antipsychotic. α indicates the degree of allosteric enhancement when both orthosteric and allosteric sites are occupied (derived from the allosteric ternary complex model). Leach et al (2010) Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology 35 855 PMID:19940843 |Huynh et al (2015) Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004. ACS Chem. Neurosci. 6 838 PMID:25857219 |Chan et al (2008) Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia Proc.Natl.Acad.Sci.U.S.A. 105 10978 PMID:18678919 |
