CAS NO: | 74711-43-6 |
规格: | ≥98% |
包装 | 价格(元) |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
5g | 电议 |
10g | 电议 |
Molecular Weight (MW) | 298.36 |
---|---|
Formula | C17H14O3S |
CAS No. | 74711-43-6 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 60 mg/mL (201.1 mM) |
Water: <1 mg/mL | |
Ethanol: 31 mg/mL (103.9 mM) | |
Other info | Chemical Name: 10,11-Dihydro-alpha-methyl-10-oxodibenzo(b,f)thiepin-2-acetic acid InChi Key: MUXFZBHBYYYLTH-UHFFFAOYSA-N InChi Code: InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20) SMILES: O=C(O)C(C)C1=CC=C(C(C2)=C1)SC3=CC=CC=C3C2=O |
Synonyms | CN 100; CN-100; CN100 |
In Vitro | In vitro activity: Zaltoprofen binds to specific sites on the protein of the bradykinin B2 receptor, hence we have examined the effect of zaltoprofen on bradykinin-induced responses of adult DRG neurons to investigate possible interaction sites. Zaltoprofen most potently inhibits bradykinin-enhancement of capsaicin-induced Ca2+ uptake into DRG neurons. Zaltoprofen also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and the slow bradykinin-induced onset of substance P release from DRG neurons. Zaltoprofen produces an analgesic action on bradykinin-induced nociceptive responses by blocking the B(2) receptor-mediated pathway in the primary sensory neurons. Zaltoprofen completely inhibits the bradykinin-induced increase of [Ca(2+)](i), which is inhibited by B(2) antagonist D-Arg-[Hyp(3), Thi(5,8), D-Phe(7)]-bradykinin, but not by B(1) antagonist. Zaltoprofen at 1nmol shows strong analgesic action on BK (i.pl.)-induced nociceptive flexor responses, whereas loxoprofen or its active metabolite loxoprofen-SRS does not. Zaltoprofen also inhibits the nociception induced by [Tyr8]-BK, a specific agonist of B2-type BK receptor, but does not affect the nociception by [Lys-des-Arg9]-BK, a specific agonist of B1-type BK receptor. Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) causes potent inhibition of cyclooxygenase-2 with fewer side effects on the gastrointestinal tract. |
---|---|
In Vivo | Zaltoprofen improves the loss in body weight in both Con A-treated mice and carbon tetrachloride-treated rats. Zaltoprofen (10 mg/kg) administrated at 8 h after Con A treatment is found to inhibit the Con A-induced reduction in body weight. Zaltoprofen (10 mg/kg) combined with Con A results in four times greater food intake than that in mice treated with only Con A. |
Animal model | Mice and rats |
Formulation & Dosage | 10 mg/kg |
References | Neuropharmacology. 2005 Jun;48(7):1035-42; Int J Mol Med. 2002 Apr;9(4):369-72. |