VCP171 是一种有效的腺苷 A1 受体 (A1R) 正变构调节剂 (PAM)。
货号:ajcx23722
CAS:1018830-99-3
分子式:C18H12F3NOS
分子量：347.4
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml,Ethanol: 10 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

VCP171 is a positive allosteric modulator of adenosine A₁receptors (EC₅₀= 15.8 μM in a kinetic assay measuring agonist dissociation).¹. It reduces AMPA receptor-mediated evoked excitatory postsynaptic currents (eEPSCs) in lamina I and lamina II neurons in a rat model of neuropathic pain (EC₅₀s = 1.995 and 0.251 μM, respectively) to a greater extent than in sham control animals (EC₅₀s = 2.512 and 0.631 μM, respectively).²

1.Aurelio, L., Figler, H., Flynn, B.L., et al.5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancersBioorg. Med. Chem.16(3)1319-1327(2008) 2.Imlach, W.L., Bhola, R.F., May, L.T., et al.A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain modelMol. Pharm.88(3)460-468(2015)