Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.3.1.107 (DAT)
 1,471 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

To obtain gastroprokinetic agents with more potent and selective activity than metoclopramide and cisapride, a series of N-(4-benzyl-2-morpholinylmethyl)benzamides were designed and prepared. Their synthesis and structure-activity relationships were described. As a result, mosapride was selected as a promising candidate for potent gastroprokinetic activity with selective 5-HT4 receptor agonistic activity. As an extension to this project, the novel benzamide and the carboxamide derivatives having 1-benzyl-4-methylhexahydro-1,4-diazepine ring in the amine moiety were prepared and evaluated for 5-HT3 receptor antagonistic activity. DAT-582 was identified as an antiemetic agent in cancer chemotherapy. The asymmetric synthesis of DAT-582 and the SAR studies were briefly reviewed. In further modifications of the N-(1-benzyl-4-methylhexahydro-1,4-diazepin-6-yl)benzamides, the novel nicotinamides with 1-ethyl-4-methylhexahydro-1,4-diazepin ring were found to have potent 5-HT3 and dopamine D2 and D3 receptor antagonistic activities and to show weak central nervous system depression and extrapyramidal syndrome. After extensive SARs, AS-8112 was selected as a broad antiemetic agent.
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PMID:Nitrogen-containing heteroalicycles with serotonin receptor binding affinity: development of gastroprokinetic and antiemetic agents. 991 93