NS 1738

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

NS 1738 是含 α7 的神经元烟碱乙酰胆碱受体 (nAChR) 的正变构调节剂。

NS 1738 is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs).

NS 1738 acts by increasing the peak amplitude of acetylcholine (ACh)-evoked currents at all concentrations; thus, it increased the maximal efficacy of ACh. Plotting peak current amplitude against the logarithm of the NS 1738 concentration used for preincubation reveals a sigmoidal concentration-response relationship that is well fit by the Hill equation (EC50=3.4 μM). Under similar experimental conditions, NS 1738 shows comparable efficacy and potency at the rat α7 nAChR (EC50=3.9 μM).

To estimate the ability of NS 1738 to permeate the blood-brain barrier, rats are administered 10 mg/kg NS 1738 intraperitoneally. Peak brain concentrations are measured approximately 30 min after injection, and they amount to ~80 ng/mL (~200 nM) at this dose. The ratio between the amount of compound entering the brain and that in plasma is AUCbrain /AUCplasma=0.50. The half-life in plasma is estimated to 42 min. Incubation of NS1738 with isolated liver microsomes in vitro indicates that approximately 60 and 75% of NS 1738 is metabolized via the cytochrome P450 system in mouse and rat, respectively, within 1 h. Adult rats administered NS 1738 at 10 and 30 mg/kg i.p. immediately following the initial exposure to a juvenile rat (T1) display significant decreases in the investigative duration of a subsequent exposure to the same juvenile (T2) 2 h later (T2/T1 ratio of 0.69±0.13 and 0.61±0.07, respectively).

NSC 213859

Endocrinology/Hormones

AChR

nAChR

——

——

501684-93-1

365.14

C14H9Cl2F3N2O2

>98% (HPLC)

DMSO:300 mg/mL (821.63 mM)

O=C(Nc1cc(Cl)ccc1O)Nc1cc(C(F)(F)F)ccc1Cl

3-(5-chloro-2-hydroxyphenyl)-1-[2-chloro-5-(trifluoromethyl)phenyl]urea

(-20℃)

With Ice Pack

≥ 2 years