Isonipecotic acid

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Chemical Structure| 498-94-2 同义名 : 异哌啶酸 ;4-Piperidinecarboxylic acid; 4-Carboxypiperidine; Hexahydroisonicotinic acid
CAS号 : 498-94-2
货号 : A111595
分子式 : C6H11NO2
纯度 : 98%
分子量 : 129.16
MDL号 : MFCD00006004
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 100 mg/mL(774.25 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Isonipecotic acid was less potent than its unsaturated analogue isoguvacine as a GABA-mimetic and as an inhibitor of GABA binding[2]. The depolarizing action of all 4 analogues muscimol, isonipecotic acid, isoguvacine and N-methyl isoguvacine could be selectively antagonized by bicuculline methochloride and isopropyl bicyclophosphate. The potency of isoguvacine was 0.23 +/- 0.026 and isonipecotic acid 0.011 +/- 0.0028[3]. Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032[4]. The most significant activity was demonstrated by the p-nitrophenyl esters of nipecotic and isonipecotic acids against bicuculline-induced seizures[5]. In vivo tests revealed statistically significant antinociceptive properties of isonipecotic acid (10 and 30 mg/kg), R-nipecotic acid (30 and 100 mg/kg) and S-nipecotic acid (100 mg/kg) in mice[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.74mL

1.55mL

0.77mL

38.71mL

7.74mL

3.87mL

77.42mL

15.48mL

7.74mL
参考文献

[1]Krogsgaard-Larsen P, Frølund B, Frydenvang K. GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr Pharm Des. 2000 Aug;6(12):1193-209. doi: 10.2174/1381612003399608. PMID: 10903390.

[2]Falch E, Jacobsen P, Krogsgaard-Larsen P, Curtis DR. GABA-mimetic activity and effects on diazepam binding of aminosulphonic acids structurally related to piperidine-4-sulphonic acid. J Neurochem. 1985;44(1):68‐75

[3]Bowery NG, Collins JF, Hudson AL, Neal MJ. Isoguvacine, isonipecotic acid, muscimol and N-methyl isoguvacine on the GABA receptor in rat sympathetic ganglia. Experientia. 1978;34(9):1193‐1195

[4]Fan J, Fahr B, Stockett D, et al. Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio. Bioorg Med Chem Lett. 2008;18(23):6236-6239

[5]Crider AM, Tita TT, Wood JD, Hinko CN. Esters of nipecotic and isonipecotic acids as potential anticonvulsants. J Pharm Sci. 1982;71(11):1214‐1219

[6]Nowaczyk A, Fijałkowski Ł, Zaręba P, Sałat K. Docking and pharmacodynamic studies on hGAT1 inhibition activity in the presence of selected neuronal and astrocytic inhibitors. Part I. J Mol Graph Model. 2018;85:171‐181