Synthesis and pharmacological activity of metabolites of the 5-HT(4) receptor antagonist SB-207266.
Three metabolites of N-[(1-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]-oxazino[3,2_a]indole-10-carboxamide (SB-207266) (1) were synthesised and their pharmacological activity determined.
Fedouloff
M
M
Department of Synthetic Chemistry, Smithkline Beecham Pharmaceuticals, New Frontiers Science Park, Essex CM19 5AW, Harlow, UK. Michael_fedouloff@sbphrd.com
Hossner
F
F
Voyle
M
M
Ranson
J
J
Powles
J
J
Riley
G
G
Sanger
G
G
D000818:Animals; D006168:Guinea Pigs; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000378:metabolism*; D044422:Receptors, Serotonin, 5-HT4; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism
D007211:Indoles; D010880:Piperidines; D011985:Receptors, Serotonin; C096919:SB 207266; D012702:Serotonin Antagonists; D044422:Receptors, Serotonin, 5-HT4