Delving into the Latest Updates on KF-18259 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

5-HT3 receptor

Mechanism

5-HT3 receptor antagonists(Serotonin 3 (5-HT3) receptor antagonists)

Therapeutic Areas

Digestive System DisordersOther Diseases

Active Indication-

Inactive Indication

Irritable Bowel SyndromeNausea and vomiting

Originator Organization

Kyowa Kirin Co., Ltd.

Active Organization-

Inactive Organization

Kyowa Kirin Co., Ltd.

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC22H29ClN2O3

InChIKeyKXESITMAGBVRTM-NKZMMAGSSA-N

CAS Registry139094-48-7

We investigated the effects of KF18259 (endo-(8-methyl-8-aza- bicyclo[3.2.1]oct-3-yl)-1-isobutyl-2-oxo-1,2-dihydro-4-quinolinecarboxyl ate hydrochloride), a novel 5-HT3-receptor antagonist, in a variety of rat models, which are assumed to be mediated via 5-HT3 receptors, in comparison with those of YM060 ((R)-5-[(1-methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydro-1H- benzimidazole hydrochloride), granisetron and ondansetron. KF18259 inhibited wrap-restraint stress-induced defecation. The doses of KF18259 to inhibit wrap-restraint stress-induced defecation were lower than those to inhibit the 5-HT-induced von Bezold-Jarisch reflex and the cisplatin-induced slowing of gastric emptying. In contrast, the doses of YM060, granisetron and ondansetron to inhibit these three responses were similar. Moreover, KF18259 inhibited the wrap-restraint stress-induced propulsive motility of the proximal and distal colon. The effect of KF18259 on the distal colon was as potent as that on defecation and was more potent than that on the proximal colon. These results indicate that KF18259 potently inhibits the distal colonic function. KF18259 may be a useful tool for the discrimination of the 5-HT3-receptors located on the distal colon and other tissues.

100 Deals associated with KF-18259

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