Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750

Aazaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a– d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC- 54750 is a potent 5-HT 4 agonist and 5-HT 3 antagonist with in vivo efficacy in gastroparesis models and also inhibits cisplatin-indu...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (22), p.5509-5512
Hauptverfasser:	Becker, Daniel P., Flynn, Daniel L., Shone, Robert L., Gullikson, Gary
Format:	Artikel
Sprache:	eng
Schlagworte:	5-HT3 5-HT4 Adamantane - analogs & derivatives Adamantane - chemical synthesis Adamantane - chemistry Adamantane - pharmacology Animals Aza Compounds - chemical synthesis Aza Compounds - pharmacology Azaadamantane Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Biological and medical sciences Cisplatin - antagonists & inhibitors Cisplatin - chemistry Digestive system Dogs Gastrointestinal Agents - chemical synthesis Gastrointestinal Agents - pharmacology Gastrointestinal Motility - drug effects Medical sciences Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Prokinetic Rats Serotonin Serotonin 5-HT3 Receptor Antagonists Serotonin 5-HT4 Receptor Agonists Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - pharmacology Serotoninergic system Vomiting - chemically induced
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Zusammenfassung:	Aazaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a– d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC- 54750 is a potent 5-HT 4 agonist and 5-HT 3 antagonist with in vivo efficacy in gastroparesis models and also inhibits cisplatin-induced emesis. Azaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a– d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC-54750 is a potent 5-HT 4 agonist and 5-HT 3 antagonist with in vivo efficacy in gastroparesis models and also inhibits cisplatin-induced emesis.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.09.005