PNU 282987

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PNU-282987 是一种选择性 α7 烟碱型乙酰胆碱受体 (α7 nAChR) 激动剂，Ki 为 26 nM；对 α1β1γδ 和 α3β4 nAChR 无亲和力 (IC50 ≥ 60 μM)。

PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).

PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM.PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM. PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM.

PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit.PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner. Animal Model:Rats Dosage:1, 3 mg/kg Administration:i.v.Result:Significantly reversed amphetamine-induced gating deficit.

PNU-282987 | PNU 282987

Endocrinology/Hormones

AChR

α7 nAChR

Neurological Disease

——

123464-89-1

301.21

C14H18Cl2N2O

>98% (HPLC)

DMSO : ≥ 61 mg/mL 202.52 mM; H2O : 50 mg/mL 166.00 mM

Cl.C1CN2CCC1[C@H](C2)NC(=O)c1ccc(cc1)Cl

Benzamide, N-(3R)-1-azabicyclo(2.2.2)oct-3-yl-4-chloro-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years