l-SKF89976A hydrochloride
N-(4,4-Diphenyl-3-butenyl)nipecotic acid hydrochloride
CAS: 85375-15-1
Molecular Formula: C22H26ClNO2
l-SKF89976A hydrochloride - Names and Identifiers
| Name | N-(4,4-Diphenyl-3-butenyl)nipecotic acid hydrochloride |
| Synonyms | skf-89976a SKF89976AHCl SKF 89976A HYDROCHLORIDE l-SKF89976A hydrochloride d,l-SKF89976A hydrochloride N-(4,4-Diphenyl-3-butenyl)nipecotic acid hydrochloride 4-(3-Carboxypiperidine)-1,1-diphenyl-1-butene hydrochloride 1-(4,4-DIPHENYL-3-BUTENYL)-3-PIPERIDINECARBOXYLIC ACID HYDROCHLORIDE 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride 1-(4,4-Diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride 1-(4,4-Diphenyl-3-buten-1-yl)-3-piperidinecarboxylic acid hydrochloride 1-(4,4-diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride |
| CAS | 85375-15-1 |
| InChI | InChI=1/C22H25NO2.ClH/c24-22(25)20-13-7-15-23(17-20)16-8-14-21(18-9-3-1-4-10-18)19-11-5-2-6-12-19;/h1-6,9-12,14,20H,7-8,13,15-17H2,(H,24,25);1H |
l-SKF89976A hydrochloride - Physico-chemical Properties
| Molecular Formula | C22H26ClNO2 |
| Molar Mass | 371.9 |
| Boling Point | 531.4°C at 760 mmHg |
| Flash Point | 275.2°C |
| Solubility | DMSO: 20mg/mL, soluble |
| Vapor Presure | 4.04E-12mmHg at 25°C |
| Appearance | solid |
| Color | white |
| Storage Condition | Inert atmosphere,2-8°C |
| In vitro study | SKF89976A has a weak antiallodynic action. SKF89976A weakly inhibits serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in chinese hamster ovary (CHO) cells stably expressing each transporter using a substrate uptake assay, with IC 50 values of 3514 , 202.13, and 728.8, respectively. SKF89976A is a GABA-transport blocker. GABA (1 mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10 μM) and SKF89976A (100 μM), but is unaffected by 100 μM picrotoxin. 100 μM SKF 89976-A is known to block the transport of GABA into cells, completely eliminated the GABA-elicited current in a reversible fashion. SKF89976A is a nontransportable blockers of GAT-1. SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA. SKF89976A (100 μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n=19). Intracellular perfusion of 20 μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n=4). |
| In vivo study | SKF89976A produces a weak antiallodynic response when administered i.v. (0.3 mg/kg). The i.t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice. |
l-SKF89976A hydrochloride - Risk and Safety
| WGK Germany | 3 |
| RTECS | TM6241000 |
l-SKF89976A hydrochloride - Reference Information
| biological activity | SKF89976A hydrochloride is a selective GABA transporter GAT-1 inhibitor, which acts on GAT-1,GAT-2 and GAT-3 in CHO cells, with IC50 of 0.28 μM,137.34 μM and 202.8 μM respectively. |
| target | IC50: 0.28 μM (GAT-1), 137.34 μM (GAT-2), 202.8 μM (GAT-3) |
| in vitro study | SKF89976A has a weak antiallodynic action. SKF89976A weakly inhibits serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in chinese hamster Ovary (CHO) cells stable expressing each transporter using a substrate take assessment, with IC 50 values of 3514 , 202.13, and 728.8, respectively. SKF89976A is a GABA-transport blocker. GABA (1 mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10 μ M) and SKF89976A (100 μ M), but is unaffected by 100 μ M picrotoxin. 100 μ M SKF 89976-A is known to block the transport of GABA into cells, completely eliminated the GABA-elicited current in a reversible fashion. SKF89976A is a nontransportable blockers of GAT-1. SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA. SKF89976A (100 μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n = 19). Intracellular perfusion of 20 μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n = 4). |
| in vivo study | SKF89976A produces a weak antiallodynic response when administered I. v. (0.3 mg/kg). the I. t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice. |
Last Update：2024-04-09 20:52:54
