product name Zaltoprofen
Description: Zaltoprofen is an inhibitor of Cox-1 and Cox-2 for treatment of arthritis. It binds to specific sites on the protein of the bradykinin B2 receptor. 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.
References: Neuropharmacology. 2005 Jun;48(7):1035-42; Int J Mol Med. 2002 Apr;9(4):369-72.
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)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19408684
| 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. Kinase Assay: Cell Assay: |
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| 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. |
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| Formulation & Dosage | |
| References | Neuropharmacology. 2005 Jun;48(7):1035-42; Int J Mol Med. 2002 Apr;9(4):369-72. |
