SB-366791

The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin. TRPV1 is present in primary sensory neurons and in both central and peripheral sensory nerve terminals and plays a role in thermal and mechanical hyperalgesia. SB-366791 is a selective TRPV1 antagonist that is widely used in pain research. In cultured trigeminal ganglion neurons, SB-366791 inhibits capsaicin-evoked Ca2+ influx with an IC50 value of 0.7 µM. A 1 nmol injection of SB-366791 in mouse paw reduces capsaicin-induced nociceptive responses in a model of pain. Intrathecal pretreatment of 10 µl SB-366791 in rats suppresses tolerance to the analgesic effects of chronic morphine administration. Co-administration of morphine and SB-366791 at 0.1 mg/kg has potent analgesic effects in a mouse model of bone cancer pain.Formal Name: 3-(4-chlorophenyl)-N-(3-methoxyphenyl)-2-propenamide. CAS Number: 472981-92-3. Molecular Formula: C16H14ClNO2. Formula Weight: 287.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml, DMSO: 10 mg/ml. lambdamax: 297 nm. SMILES: ClC1=CC=C(/C=C/C(NC2=CC(OC)=CC=C2)=O)C=C1. InChi Code: InChI=1S/C16H14ClNO2/c1-20-15-4-2-3-14(11-15)18-16(19)10-7-12-5-8-13(17)9-6-12/h2-11H,1H3,(H,18,19)/b10-7+. InChi Key: RYAMDQKWNKKFHD-JXMROGBWSA-N.