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NNC 05-2090

Names

[ CAS No. ]:
184845-43-0

[ Name ]:
NNC 05-2090

[Synonym ]:
NNC 05-2090 hydrochloride

Biological Activity

[Description]:

NNC 05-2090 is a potent inhibitor of mGAT2, with a Ki of 1.4 μM. Anticonvulsant properties[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vitro]

NNC 05-2090呈剂量依赖性,对DBA/2小鼠的声诱发强直和阵挛惊厥有抑制作用,其ED50值为19 μmol/kg[2]。 NNC 05-2090呈剂量依赖性,在最大电休克(MES)实验中拮抗强直后肢扩展反应,其ED50值为73 mmol/kg[2]。 NNC 05-2090在最高剂量(72-242 mmol/kg)明显(P<0.05)降低了全身性癫痫的严重程度(癫痫分级为3-5级),并且在这些剂量下NNC 05-2090也显著缩短了后放电持续时间(P<0.05)[2]。

[References]

[1]. C Thomsen, et al. 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br J Pharmacol. 1997 Mar;120(6):983-5.  

[2]. N O Dalby, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 1997 Jul;28(1):51-61.  

Chemical & Physical Properties

[ Boiling Point ]:
643.1ºC at 760 mmHg

[ Molecular Formula ]:
C27H30N2O2

[ Molecular Weight ]:
414.54

[ Flash Point ]:
342.7ºC

[ Exact Mass ]:
450.20700

[ PSA ]:
37.63000

[ LogP ]:
5.91670

[ Vapour Pressure ]:
2.04E-17mmHg at 25°C


Related Compounds