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216776-73-7

216776-73-7 Structure

216776-73-7 Structure
IdentificationBack Directory
[Name]

Methanone, [(2R)-2-(3,4-dichlorophenyl)-2-[2-[(2S)-2-oxidospiro[benzo[c]thiophene-1(3H),4'-piperidin]-1'-yl]ethyl]-4-morpholinyl](3,4,5-trimethoxyphenyl)-, hydrochloride (1:1)
[CAS]

216776-73-7
[Synonyms]

CS-003 HCl
Methanone, [(2R)-2-(3,4-dichlorophenyl)-2-[2-[(2S)-2-oxidospiro[benzo[c]thiophene-1(3H),4'-piperidin]-1'-yl]ethyl]-4-morpholinyl](3,4,5-trimethoxyphenyl)-, hydrochloride (1:1)
[Molecular Formula]

C34H39Cl3N2O6S
[MOL File]

216776-73-7.mol
[Molecular Weight]

710.1
Hazard InformationBack Directory
[Uses]

CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists[1].
[References]

[1] Novel triple neurokinin receptor antagonist CS-003 strongly inhibits neurokinin related responses DOI:10.1016/j.ejphar.2008.02.056
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