Nelonicline

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

Nelonicline (ABT-126) 是一种有效的选择性 α7 烟碱受体 (nAChR) 部分激动剂，用于治疗精神分裂症认知障碍。

Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia.Alzheimer Disease Phase 2 Clinical.

Nelonicline is an agonist that binds with high affinity to α7 nAChRs in human brain (Ki= 12.3 nM) and activates currents in Xenopus oocytes expressing recombinant human α7 nAChRs (EC50=2 μM; intrinsic activity of 74% relative to acetylcholine). Nelonicline does bind to α3β4* nAChRs in human IMR-32 neuroblastoma cells (Ki=60 nM), but has only 12% efficacy at 100,000 nM in a calcium flux assay in these cell. Like some other α7 nAChR agonists, Nelonicline is also a 5-HT3 receptor antagonist, but it has >10-fold lower affinity for this receptor than for α7 nAChRs (Ki of 140 nM).

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ABT-126 | ABT126

Membrane Transporter/Ion Channel

nAChR

nAChR

Neurological Disease

Alzheimer Disease

1026134-63-3

312.431

C18H20N2OS

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (39.88 mM)

C1(C(S2)=NN=C2O[C@@H]3[C@H]4C[C@H]5C[C@@H]3CN(C4)C5)=CC=CC=C1

2-(((5S,7S)-adamantan-2-yl)oxy)-5-phenyl-1,3,4-thiadiazole

(-20℃)

With Ice Pack

≥ 2 years