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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 5 mg/mL, clear
起源
GlaxoSmithKline
SMILES 字串
COc1cccc(NC(=O)\C=C\c2ccc(Cl)cc2)c1
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 密鑰
RYAMDQKWNKKFHD-JXMROGBWSA-N
基因資訊
human ... TRPV1(7442)
應用
SB-366791 has been used as a transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist:
- to infer the in vitro and in vivo pharmacology of (E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide (AMG 9810)
- to study its effects on sodium hydrogen sulfide (NaHS) or capsaicin-induced contractile activity
- to study the inhibitory potency of phoneutria toxin (PnTx3-5) (native and recombinant) on various responses mediated by transient receptor potential cation channel subfamily V member 1 (TRPV1)
生化/生理作用
SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.
Vanilloid receptor-1 (TRPV1) antagonist.
特點和優勢
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
Journal of translational medicine, 17(1), 346-346 (2019-10-24)
Tibial fracture is associated with inflammatory reaction leading to severe pain syndrome. Bradykinin receptor activation is involved in inflammatory reactions, but has never been investigated in fracture pain. This study aims at defining the role of B1 and B2-kinin receptors
Neuropharmacology, 162, 107826-107826 (2019-10-28)
Capsaicin, an agonist of TRPV1, evokes intracellular [Ca2+] transients and glutamate release from perfused trigeminal ganglion. The spider toxin PnTx3-5, native or recombinant is more potent than the selective TRPV1 blocker SB-366791 with IC50 of 47 ± 0.18 nM, 45 ± 1.18 nM and 390 ± 5.1 nM in
Immunology, 161(2), 148-161 (2020-07-24)
Dry eye disease (DED) is a highly prevalent ocular surface disorder with neuroimmune pathophysiology. Tear hyperosmolarity (THO), a frequent finding in affected patients, is considered a key element in DED pathogenesis, yet existing animal models are based on subjecting the
The Journal of pharmacology and experimental therapeutics, 313(1), 474-484 (2004-12-24)
The vanilloid receptor 1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel expressed by peripheral sensory neurons. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Here, we describe the in vitro and in vivo
SB366791, a TRPV1 antagonist, potentiates analgesic effects of systemic morphine in a murine model of bone cancer pain
British Journal of Anaesthesia, 102(2), 251-258 (2009)
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