SB366791

Research use only, not for human use.

SB-366791 is a new and selective cinnamide TRPV1 antagonist.

SB-366791is a potent and selective TRPV1 antagonist. SB-366791 inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. SB-366791 decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers.

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SB-366791 (30 μM) inhibits the frequency of miniature excitatory postsynaptic currents (EPSCs). SB-366791 (30 μM) reduces the frequency of spontaneous EPSCs in the spinal cord slices from FCA-treated rats. SB-366791(30 μM) inhibits the amplitude of C-fibre evoked EPSCs. SB-366791 has also been used in vivo to assess the potential analgesic action of the inhibition of TRPV1, and significantly inhibits capsaicin-induced hypothermia, eye wiping movements and vasodilatation in the knee joint. SB-366791 inhibits glutamatergic transmission via an apparently pre-synaptic mechanism(s).

SB-366791 | SB 366791 | SB366791

Others

Other Targets

TRPV1

Cancer

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472981-92-3

287.74

C16H14ClNO2

>98% (HPLC)

DMSO : ≥ 39 mg/mL 135.54 mM; H2O : < 0.1 mg/mL

COC1=CC=CC(=C1)NC(=O)/C=C/C2=CC=C(C=C2)Cl

3-(4-chlorophenyl)-N-(3-methoxyphenyl)-2-propenamide

(-20℃)

With Ice Pack

≥ 2 years