Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.
نویسندگان
چکیده
Pyrrolizidine benzamide (+/-)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT(4) agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (+/-)-2 has an EC(50) of 449 nM in the TMM assay, as compared to 23 nM for SC-53116, and 66 nM for the racemate of SC-53116.
منابع مشابه
5-CT or DOI augments TRH analog-induced gastric acid secretion at the dorsal vagal complex.
Serotonin (5-HT) interacts with thyrotropin-releasing hormone (TRH) at the dorsal vagal complex (DVC) to augment TRH-induced stimulation of gastric acid secretion. To investigate the 5-HT receptor family involved in the augmentation response, prototypical 5-HT receptor-selective agonists (146 pmol) were coinjected with the TRH analog RX-77368 (RX; 12 pmol) into the rat DVC in a 30-nl volume. Th...
متن کاملPyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.
A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT(4) and 5-HT(3) receptor binding, 5-HT(4) receptor agonism in the rat tunica muscularis mucosae (TMM) assay, and for 5-HT(3) receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT(4) receptor, including benzami...
متن کاملEvidence for involvement of central 5-HT(4) receptors in cholinergic function associated with cognitive processes: behavioral, electrophysiological, and neurochemical studies.
The possible involvement of 5-HT(4) receptors in cognitive function was investigated with a view toward modulating the cholinergic neuronal system. For this purpose, behavioral, electrophysiological, and neurochemical studies were performed in rats. The behavioral study, using a passive avoidance test, demonstrated that the 5-HT(4) receptor agonist SC 53116 (10 microg/rat i.c.v.) had an amelior...
متن کاملAzaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.
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.
متن کامل5-HT induces duodenal mucosal bicarbonate secretion via cAMP- and Ca -dependent signaling pathways and 5-HT4 receptors in mice
Tuo, Bi-Guang, Zachary Sellers, Petra Paulus, Kim E. Barrett, and Jon I. Isenberg. 5-HT induces duodenal mucosal bicarbonate secretion via cAMPand Ca -dependent signaling pathways and 5-HT4 receptors in mice. Am J Physiol Gastrointest Liver Physiol 286: G444–G451, 2004. First published October 23, 2003; 10.1152/ ajpgi.00105.2003.—In previous studies, we have found that 5-hydroxytryptamine (5-HT...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 14 12 شماره
صفحات -
تاریخ انتشار 2004