RS 67506
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RS 67506
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CAS No:
168986-61-6
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Formula:
C18H28ClN3O4S.ClH
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Chemical Name:
RS 67506
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Synonyms:
Methanesulfonamide,N-[2-[4-[3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl]-1-piperidinyl]ethyl]-,hydrochloride (1:1);Methanesulfonamide,N-[2-[4-[3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl]-1-piperidinyl]ethyl]-,monohydrochloride;RS 67506
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CAS No:
Description
ChEBI: A hydrochloride salt obtained by mixing equimolar amounts of RS 39604 with hydrochloric acid. A potent and selective 5-HT4 antagonist, with a pKi of 9.1 at 5-HT4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A, 2C, 3 and D1, D2, M1, M2, AT1, B1 and alpha1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.
Drug Information
1-(4-amino-5-chloro-2-methoxyphenyl)-3-(1-(2-methyl sulphonylamino)ethyl-4-piperidinyl)-1-propanone hydrochloride
RS 67506 Use and Manufacturing
A potent and selective 5-HT 4 partial agonist, with a pK i of 8.8 at 5-HT 4 sites in guinea pig striatum, but < 6.0 at several other receptors including 5-HT 1A, 1D, 2A, 2C , D 1 , D 2 and M 1-3 . It is active in vivo and has an intrinsic activity compared to 5-HT of 0.6.
Computed Properties
Molecular Weight:454.4
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:9
Exact Mass:453.1255830
Monoisotopic Mass:453.1255830
Topological Polar Surface Area:110
Heavy Atom Count:28
Complexity:576
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes