SKF 89976A

製品番号: HY-100228: Data Sheet 取扱説明書
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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.

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SKF 89976A 構造式

CAS 番号 : 85375-85-5

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Other 在庫あり Forms of SKF 89976A:

SKF89976A hydrochloride

Other Forms of SKF 89976A:

SKF89976A hydrochloride 在庫あり

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参考文献
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製品説明

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.

IC₅₀ & Target

IC50: 0.28 μM (GAT-1), 137.34 μM (GAT-2), 202.8 μM (GAT-3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.13 3 Compound: 4, SK and F-89976-A	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	[PMID: 23336362]
HEK293	IC₅₀	0.13 3 Compound: 4, SK and F-89976-A	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	[PMID: 23336362]

体外実験

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 IC₅₀ values of 3514 , 202.13, and 728.8, respectively^[1]. 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^[2]. 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)^[3.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

335.44

分子式

C₂₂H₂₅NO₂

CAS 番号

85375-85-5

SMILES

O=C(C1CN(CC/C=C(C2=CC=CC=C2)/C3=CC=CC=C3)CCC1)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

[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. [Content Brief]

[3]. Barakat L, et al. GAT-1 and reversible GABA transport in Bergmann glia in slices. J Neurophysiol. 2002 Sep;88(3):1407-19. [Content Brief]

細胞実験 ^[1]	CHO cells stably expressing the mouse GAT subtypes, rat serotonin transporter (SERT), rat noradrenaline transporter (NET), and rat dopamine transporter (DAT) are incubated with 10 nM tritium-labeled GABA or monoamines for 10 min in the absence or presence of various concentrations of the GAT inhibitors (e.g., SKF89976A) tested. Values presented for SERT, NET, and DAT are the mean±S.E.M. for 3 experiments, with each being performed in duplicate^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Mice^[1] 5-week-old ddY male mice, weighing 25-30 g at the beginning of the study are used. Mice are administered NNC05-2090, SKF89976A, (S)-SNAP5114, or amitriptyline. NNC05-2090, SKF89976A, and (S)-SNAP5114 are dissolved in DMSO and diluted appropriately with ACSF or saline (the final concentration of DMSO is less than 0.5%). The composition of ACSF (in mM) is 142 mM NaCl, 5 mM KCl, 2 mM CaCl₂, 2 mM MgCl₂, 1.25 mM NaH₂PO₄, 10 mM d-glucose, 10 mM HEPES, and 0.05% fatty acid-free bovine serum albumin (pH 7.4). The intraperitoneal (i.p.) injection of drugs is administered in a volume of 0.1 mL/10 g body weight. When given intravenously (i.v.), solutions are injected into the tail vein in a volume of 0.1 mL/10 g body weight. The head of a mouse is placed into a plastic cap and the body is held with one hand for an intrathecal (i.t.) injection. A 27-gauge needle attached to a Hamilton microsyringe is inserted into the subarachnoid space between the L5 and L6 vertebrae of the conscious mouse and 5 mL of the drug solution is slowly injected. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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. [Content Brief] [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. [Content Brief] [3]. Barakat L, et al. GAT-1 and reversible GABA transport in Bergmann glia in slices. J Neurophysiol. 2002 Sep;88(3):1407-19. [Content Brief]

SKF 89976A Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKF 89976A85375-85-5GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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