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经验公式(希尔记法):
C16H14NO2Cl
化学文摘社编号:
分子量:
287.74
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
SB-366791, ≥98% (HPLC), powder
InChI key
RYAMDQKWNKKFHD-JXMROGBWSA-N
SMILES string
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+
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear
originator
GlaxoSmithKline
Quality Level
Gene Information
human ... TRPV1(7442)
Application
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)
Biochem/physiol Actions
SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.
Vanilloid receptor-1 (TRPV1) antagonist.
Features and Benefits
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Narender R Gavva et al.
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
Elizete Maria Rita Pereira et al.
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
SB366791, a TRPV1 antagonist, potentiates analgesic effects of systemic morphine in a murine model of bone cancer pain
Niiyama Y, et al.
British Journal of Anaesthesia, 102(2), 251-258 (2009)
Mauricio Guzmán et al.
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
Vincent Minville et al.
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
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