Synthesis of thiophene carboxamide derivatives as serotonin 5-HT4 receptor agonists.
New thiophene carboxamide derivatives 3 (a-j) were synthesized as serotonin 5-HT4 receptor agonists. Preliminary results showed that the compounds 3a, 3d, 3e and 3f caused concentration dependent relaxation of carbachol-induced contraction in tunica muscularis mucosae in rat oesophagus.
Monge
A
A
CIFA Centro de Investigatión en Farmacobiología Aplicada, Universidad de Navarra, España.
Palop
J
J
Pérez
S
S
Oset
C
C
Lasheras
B
B
D000818:Animals; D002217:Carbachol / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004947:Esophagus / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D018721:Muscarinic Agonists / Q000494:pharmacology; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
D018721:Muscarinic Agonists; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D013876:Thiophenes; D002217:Carbachol