1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE
1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE Basic information
- Product Name:
- 1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE
- Synonyms:
-
- 1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE
- NNC 05-2090 HYDROCHLORIDE
- NNC 05-2090HCl
- 4-Piperidinol, 1-[3-(9H-carbazol-9-yl)propyl]-4-(2-methoxyphenyl)-
- NNC 05-2090, GABA uptake inhibitor
- CAS:
- 184845-43-0
- MF:
- C27H30N2O2
- MW:
- 414.54
- Mol File:
- 184845-43-0.mol
1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE Chemical Properties
- Boiling point:
- 623.5±55.0 °C(Predicted)
- Density
- 1.17±0.1 g/cm3(Predicted)
- storage temp.
- Desiccate at RT
- pka
- 14.13±0.20(Predicted)
1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDE Usage And Synthesis
Uses
NNC 05-2090 Hydrochloride is a GABA uptake inhibitor displaying selectivity for BGT-1 (mGAT-2) transporters.
Biological Activity
GABA uptake inhibitor that displays moderate selectivity for BGT-1 (mGAT-2) transporters (K i values are 1.4, 15, 19 and 41 μ M for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively). Anticonvulsive; inhibits sound-induced tonic and clonic convulsions in DBA/2 mice. Also displays affinity at α 1 - and D 2 -receptors (IC 50 values are 266 and 1632 nM respectively).
in vivo
NNC 05-2090 (intraperitoneal injection) dose-dependently protects against maximal electroshock (MES) in mice with an ED50 values of 73 μmol/kg, and shows ED50 values against tonic and clonic convulsions in DBA/2 mice of 19 and 26 μmol /kg, respectively[1]. NNC 05-2090 (0.01, 0.1 and 0.3 mg/kg; i.p. or i.,t., once) reverses mechanical allodynia in (partial sciatic nerve ligation) PSL model mice[3].
1-[3-(9H-CARBAZOL-9-YL)PROPYL]-4-(2-METHOXYPHENYL)-4-PIPERIDINOL HYDROCHLORIDESupplier
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