|1-苯基-3,3-双(吡啶-4-基甲基)吲哚啉-2-酮二盐酸盐|CsnPharm

CAS No.: 113168-57-3

1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride Catalog No. CSN20023

Synonyms: Linopirdine Dihydrochloride;DuP-996 Dihydrochloride;DuP-996 2HCl

Linopirdine 2HCl is a blocker of KV7 (KCNQ) voltage-gated potassium channels which blocks KV7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM), and is a putative cognition-enhancing drug.

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描述Linopirdine 2HCl (Linopirdine [DuP 996, 3, 3-bis(4-pyridinylmethyl)-1-phenylindolin-2-one]), a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue and improves performance in animal models of learning and memory. Linopirdine was found to block voltage-gated, calcium-activated and leak K+ currents in a dose-dependent manner. Linopirdine was most selective for IM with an IC50 of 2.4 +/- 0.4 microM, followed by IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC50 of 16.3 +/- 2.4 microM. Linopirdine selectively blocks IM at concentrations [3]. In addition, linopirdine blocked responses of recombinant alpha9alpha10 nicotinic cholinergic receptors (nAChRs) in a concentration-dependent manner with an IC(50) of 5.2 microM. Block by linopirdine was readily reversible, voltage independent, and surmountable at high concentrations of ACh, thus suggestive of a competitive type of interaction with the receptor^[4]. Linopirdine (0.1 and 1 mg/kg) ameliorated the scopolamine-induced deficit, but at doses ranging from 0.01-1 mg/kg, it did not affect passive avoidance retention in normal (untreated) mice. Linopirdine (0.01 and 0.1, but not 1 mg/kg) ameliorated the atropine deficit. In addition, linopirdine (0.1 mg/kg) ameliorated the deficit in cognition-impaired aged rats (23-24 mo), but did not affect unimpaired aged rats. In terms of neurochemical action, linopirdine (1, 10, and 100 microM) produced a concentration-dependent increase in K(+)-evoked ACh overflow from superfused rat hippocampal slices. Also, linopirdine (10 microM) similarly increased ACh release in young control rats and cognition-impaired and nonimpaired aged rats^[5].
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计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1534 mL
- 10.7669 mL
- 21.5338 mL
- 5 mM
- 0.4307 mL
- 2.1534 mL
- 4.3068 mL
- 10 mM
- 0.2153 mL
- 1.0767 mL
- 2.1534 mL

技术信息

CAS号	113168-57-3	储存条件	粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C26H23Cl2N3O	运输	蓝冰
分子量	464.39	别名	Linopirdine Dihydrochloride;DuP-996 Dihydrochloride;DuP-996 2HCl

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1-Phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one dihydrochloride Catalog No. CSN20023

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