| Identification | Back Directory | [Name]
SK&F 89976-A | [CAS]
85375-85-5 | [Synonyms]
SKF-89976
1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid | [Molecular Formula]
C22H25NO2 | [MDL Number]
MFCD01321071 | [MOL File]
85375-85-5.mol | [Molecular Weight]
335.44 |
| Hazard Information | Back Directory | [Description]
SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo. | [Uses]
SKF89976A is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively. | [Definition]
ChEBI: 1-(4,4-diphenylbut-3-enyl)-3-piperidinecarboxylic acid is a diarylmethane. | [in vivo]
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[1]. | [References]
[1] 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. DOI:10.1254/jphs.13146fp
[2] Kreitzer MA, et al. Glutamate modulation of GABA transport in retinal horizontal cells of the skate. J Physiol. 2003 Feb 1;546(Pt 3):717-31. DOI:10.1113/jphysiol.2002.034421
[3] Barakat L, et al. GAT-1 and reversible GABA transport in Bergmann glia in slices. J Neurophysiol. 2002 Sep;88(3):1407-19. DOI:10.1152/jn.2002.88.3.1407 |
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