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Category:
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Transporters Neurotransmitter TransportersGABA Transporters
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Cat.No.
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Product Name
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1081 |
SKF 89976A hydrochloride
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Price and Availability
Click here for full price details of
SKF 89976A hydrochloride
Other Information:
Sold with the permission of GlaxoSmithKline
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Chemical Name:
1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid
hydrochloride |
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Biological Activity:
A potent GABA uptake inhibitor,
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). Inhibits transport current
competitively (Ki = 7 μM)
and transmitter-gated current non-competitively (Ki = 0.03 nM). Able
to pass the blood-brain barrier after systemic administration and is active in
vivo.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Ali et
al (1985) Orally active and potent
inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653. Murali Dhar
(1996) On the bioactive conformation of the GABA uptake inhibitor SK&F
89976-A. Bioorg.Med.Chem.Lett. 6 1535. Krause and
Schwarz (2005) Identification and selective inhibition of the channel mode
of the neuronal GABA transporter 1. Mol.Pharmacol. 68 1728.
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or by Research Area
Keywords: SKF 89976A Hydrochloride, Neurotransmitter Transporters, Potent GABA Uptake Inhibitor. Penetrates Blood Brain Barrier, SKF89976A Hydrochloride, Tocris Bioscience
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