| Description | NNC 05-2090 hydrochloride is a betaine/GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM.NNC 05-2090 hydrochloride can be used for the study of epilepsy and neurological disorders. |
| In vitro | NNC05-2090 hydrochloride binds to prazosin and spiperone with IC50 values of 266 nM and 1632 nM, respectively.[1]NNC05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in rat cortical synaptosomes with an IC50 value of 4.4 μM.[1]NNC05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in inferior colliculus synaptosomes with an IC50 value of 2.5 μM.[1]NNC05-2090 hydrochloride inhibits serotonin, norepinephrine, dopamine transporter, and BGT-1 with IC50 values of 5.29, 7.91, 4.08, and 10.6 μM respectively.[1]NNC05-2090 hydrochloride inhibits GAT-1, GAT-2 and GAT-3 with IC50s of 29.62, 45.29 and 22.51 μM respectively.[1] |
| In vivo | NNC05-2090 hydrochloride (i.p.; PSL mice) dose-dependently protects mice from maximal electric shock (MES) ED50 of 73 μmol/kg and against tonic and clonic convulsions in DBA/2 mice with an ED50 of 19 μmol /kg and 26 μmol/kg.[1] NNC05-2090 hydrochloride (0.01, 0.1, 0.3 mg/kg; intraperitoneal or intrathecal injection; once) can dose-dependently reverse mechanical allodynia in PSL model mice by both intraperitoneal injection and intrathecal injection.[2] |
| molecular weight | 451 |
| Molecular formula | C27H31ClN2O2 |
| CAS | 184845-18-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 5.64 mg/mL DMSO: 50 mg/mL (110.86 mM) |
| 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-Epilepsy Res. 1997;28(1):51-6 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):217-226. |