Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H26ClNO4.ClH |
Molecular Weight | 440.36 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCOC(=O)COC1=CC2=C(CC[C@@H](C2)NC[C@H](O)C3=CC=CC(Cl)=C3)C=C1
InChI
InChIKey=NQIZCDQCNYCVAS-RQBPZYBGSA-N
InChI=1S/C22H26ClNO4.ClH/c1-2-27-22(26)14-28-20-9-7-15-6-8-19(11-17(15)12-20)24-13-21(25)16-4-3-5-18(23)10-16;/h3-5,7,9-10,12,19,21,24-25H,2,6,8,11,13-14H2,1H3;1H/t19-,21-;/m0./s1
DescriptionSources: http://adisinsight.springer.com/drugs/800001600Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/1976401 | https://www.ncbi.nlm.nih.gov/pubmed/14584972
Sources: http://adisinsight.springer.com/drugs/800001600
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/1976401 | https://www.ncbi.nlm.nih.gov/pubmed/14584972
Amibegron (SR 58611A or SR 58611) is a highly selective agonist for atypical beta3-adrenoceptors. It stimulates neuronal activity in a specific area of the prefrontal cortex and also inhibits intestinal motility. Amibegron was in phase III trials worldwide for the treatment of depression and generalised anxiety disorder but development of the product was discontinued in 2008. Amibegron has been tested for its potential as a treatment for irritable bowel syndrome.
Originator
Approval Year
Sample Use Guides
This eight week double-blind phase III trial compared the efficacy of paroxetine with two fixed doses of amibegron (175mg or 350mg q12) in treating the symptoms of depression (NCT00385307).
In 24 healthy obese volunteers, amibegron 60 and 180 mg/day tid for 6 days and a single dose on day 7 was safe and well tolerated.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7957612
Amibegron (SR 58611A or SR 58611) increased cyclic AMP levels in membrane homogenates from rat interscapular brown adipose tissue with an EC50 of 20 nM. This compound also stimulated glycerol release from the brown fat cells, with an EC50 of 11 nM.
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NCI_THESAURUS |
C48149
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121888
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CHEMBL1193948
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DBSALT002941
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C97276
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N910CJ679E
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100000175016
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UU-12
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ACTIVE MOIETY
SUBSTANCE RECORD