SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Authors :: Forbes IT
Douglas S
Gribble AD
Ife RJ
Lightfoot AP
Garner AE
Riley GJ
Jeffrey P
Stevens AJ
Stean TO
Thomas DR
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Nov 18; Vol. 12 (22), pp. 3341-4.
Publication Year :: 2002
Abstract: A focused SAR study around the previously reported selective 5-HT(7) receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improved pharmacokinetic profile. Replacement of the phenolic group in SB-269970-A with an indole moiety, and replacement of the piperidinyl 4-methyl group with a heterocyclic ring system proved to be the key changes leading to the identification of SB-656104-A.

Subjects :: Animals
Blood-Brain Barrier
Heterocyclic Compounds
Indoles
Phenols chemical synthesis
Phenols pharmacology
Protein Binding
Pyrrolidines chemical synthesis
Pyrrolidines pharmacology
Rats
Serotonin Antagonists pharmacology
Structure-Activity Relationship
Sulfonamides pharmacokinetics
Phenols pharmacokinetics
Pyrrolidines pharmacokinetics
Receptors, Serotonin chemistry
Serotonin Antagonists chemical synthesis
Serotonin Antagonists pharmacokinetics

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