184845-18-9

184845-18-9 structure

Name: NNC 05-2090 hydrochloride
Chemical Name: 1-[3-(9H-Carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-4-piperidinol hydrochloride (1:1)
CAS Number: 184845-18-9
Molecular Formula: C₂₇H₃₁ClN₂O₂
Molecular Weight: 451.000
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2018-06-14 15:01:51
Modify Date: 2024-01-09 17:51:04
NNC05-2090 (hydrochloride) is a GABA uptake inhibitor. NNC05-2090 is a betaine/GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM. NNC05-2090 can be used for the research of epilepsy and neurological disease[1][2].

Name	1-[3-(9H-Carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-4-piperidinol hydrochloride (1:1)
Synonyms	1-[3-(9H-Carbazol-9-yl)propyl]-4-(2-methoxyphenyl)piperidin-4-ol hydrochloride (1:1) 4-Piperidinol, 1-[3-(9H-carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-, hydrochloride (1:1) 1-[3-(9H-Carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-4-piperidinol hydrochloride (1:1)

Description	NNC05-2090 (hydrochloride) is a GABA uptake inhibitor. NNC05-2090 is a betaine/GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM. NNC05-2090 can be used for the research of epilepsy and neurological disease[1][2].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> GABA Receptor
In Vitro	NNC05-2090 hydrochloride 与 prazosin 和 spiperone 结合的 IC50 值分别为 266 nM 和 1632 nM[1]。 NNC05-2090 hydrochloride (0.1-100 μM) 抑制大鼠皮层突触小体 [3H]GABA 的摄取，IC50 值为 4.4 μM[1]。 NNC05-2090 hydrochloride (0.1-100 μM) 下丘突触小体中抑制 [3H]GABA 的摄取 IC50 值为 2.5 μM[1]。 NNC05-2090 hydrochloride 抑制血清素、去甲肾上腺素、多巴胺转运蛋白和 BGT-1 的 IC50 值分别为 5.29，7.91，4.08 和 10.6 μM[1]。 NNC05-2090 hydrochloride 抑制 GAT-1，GAT-2 和 GAT-3 的 IC50 分别为 29.62，45.29 和 22.51 μM[1]。
In Vivo	NNC05-2090 hydrochloride (腹腔注射) 剂量依赖性地保护小鼠的最大电击 (MES) ED50 值为 73 μmol/kg，并对 DBA/2 小鼠的强直性和阵挛性抽搐的 ED50 值为 19 μmol/kg 和 26 μmol/kg[1]. NNC05-2090 hydrochloride (0.01，0.1，0.3 mg/kg；腹腔注射或鞘内注射，1 次) 可逆转部分坐骨神经结扎小鼠的机械性异常痛。 Animal Model: Partial sciatic nerve ligation (PSL) mice with mechanical allodynia[2] Dosage: 0.01, 0.1 and 0.3 mg/kg Administration: Intraperitoneal injection or intrathecal injection; 0.1 mg/kg, once Result: Dose-dependently reversed mechanical allodynia in PSL model mice by both intraperitoneal injection and intrathecal injection.
References	[1]. Dalby NO, 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. [2]. Jinzenji A, et al. Antiallodynic action of 1-(3-(9H-Carbazol-9-yl)-1-propyl)-4-(2-methyoxyphenyl)-4-piperidinol (NNC05-2090), a betaine/GABA transporter inhibitor. J Pharmacol Sci. 2014;125(2):217-26.

Molecular Formula	C₂₇H₃₁ClN₂O₂
Molecular Weight	451.000
Exact Mass	450.207397

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