Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H41ClN4O5.2ClH |
Molecular Weight | 610.013 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CO[C@H]1CN(CCCCCC(=O)O[C@H]2CN3CCC2CC3)CC[C@H]1NC(=O)C4=C(OC)C=C(N)C(Cl)=C4
InChI
InChIKey=ZKVOMYDQQYOJKE-HTKGJVFSSA-N
InChI=1S/C27H41ClN4O5.2ClH/c1-35-23-15-21(29)20(28)14-19(23)27(34)30-22-9-13-31(17-25(22)36-2)10-5-3-4-6-26(33)37-24-16-32-11-7-18(24)8-12-32;;/h14-15,18,22,24-25H,3-13,16-17,29H2,1-2H3,(H,30,34);2*1H/t22-,24+,25+;;/m1../s1
Naronapride (ATI-7505), an orally administered, cisapride analogue and serotonin4 (5HT4) receptor agonist, is being developed by Renexxion for the treatment of multiple gastrointestinal disorders. Sinovant is initially developing naronapride for the treatment of irritable bowel syndrome – constipation (IBS-C), a disease that affects millions of Chinese patients and for which few effective treatment options are available. Naronapride has been evaluated in over 900 subjects in multiple randomized controlled clinical studies and has demonstrated promising results in patients with gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and chronic idiopathic constipation (CIC). Naronapride’s low systemic absorption and high specificity for 5HT4 and D2 receptors is thought to improve its safety and tolerability profile relative to other members of the class.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Metabolism and pharmacokinetics of naronapride (ATI-7505), a serotonin 5-HT(4) receptor agonist for gastrointestinal motility disorders. | 2011 Jul |
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Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders. | 2012 Apr |
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Systematic review with meta-analysis: highly selective 5-HT4 agonists (prucalopride, velusetrag or naronapride) in chronic constipation. | 2014 Feb |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17187586
A randomized, parallel-group, double-blind, placebo-controlled study evaluated effects of 9-day treatment with Naronapride (3, 10 or 20 mg t.i.d.) on scintigraphic GI and colonic transit in healthy volunteers.
Route of Administration:
Oral
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49843901
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898PE2W8US
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WW-118
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CHEMBL2103858
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300000044482
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C175158
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860169-57-9
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DTXSID60235356
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DBSALT002600
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SUBSTANCE RECORD