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Cat. No. Name Size Price Add Cart
KI2559SR14033310 mg$585
SR14033350 mg$2457

Chemical Characteristic

Product NameSR140333
SynonymsN/A
CAS No.153050-21-6
Molecular Weight 656.12
FormulaC37H45Cl3N2O2
Chemical Name1-[2-[(3S)-3-(3,4-Dichlorophenyl)-1-[2-[3-(1-methylethoxy)phenyl]acetyl]-3-piperidinyl]ethyl]-4-phenyl-1-azoniabicyclo[2.2.2]octane chloride
Smiles[N]12(CCC(CC1)(CC2)c1ccccc1)CC[C@]1(CN(CCC1)C(=O)Cc1cc(ccc1)OC(C)C)c1cc(c(cc1)Cl)Cl Cl
Chemical Structure

Biological activities

SR140333 is a potent, selective and new non-peptide inhibitor of tachykinin NK1 receptors. SR140333 antagonizes the contractions elicited by capsaicin with an IC50 of 0.06 nM.[1] In vitro, SR140333 inhibits substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. In vivo, SR140333 shows antagonism toward substance P-induced hypotension in dogs (ED50 = 3 μg/kg i.v.), bronchoconstriction in guinea-pig (ED50 = 42 μg/kg i.v.) and plasma extravasation in rats (ED50 = 7 μg/kg i.v.).[2]

Protocols

In vitro: SR140333 is dissolved in DMSO.[2]

References

[1] Croci T, et al. In vitro characterization of the non-peptide tachykinin NK1 and NK2-receptor antagonists, SR140333 and SR48968 in different rat and guinea-pig intestinal segments. Life Sci. 1995, 56 (4): 267-275.
[2] Emonds-Alt X, et al. In vitro and in vivo biological activities of SR140333, a novel potent non-peptide tachykinin NK1 receptor antagonist. Eur J Pharmacol. 1993, 250 (3): 403-413.

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