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Bioactivity |
SB-366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist (IC50=5.7 nM). SB-366791 can be used for the research of inflammation[1][2]. |
In Vivo |
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)[1]. |
Name |
SB-366791 |
CAS |
472981-92-3 |
Formula |
C16H14ClNO2 |
Molar Mass |
287.74 |
Appearance |
Solid |
Transport |
Room temperature in continental US; may vary elsewhere. |
Storage |
Powder |
-20°C |
3 years |
|
4°C |
2 years |
In solvent |
-80°C |
6 months |
|
-20°C |
1 month |
|
Reference |
[1]. Lappin SC, et al. TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Eur J Pharmacol. 2006;540(1-3):73-81. [2]. Gunthorpe MJ, et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist [published correction appears in Neuropharmacology. 2004 May;46(6):905]. Neuropharmacology. 2004;46(1):133-149. |