Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C12H12F3N |
| Molecular Weight | 227.2256 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CC=C2[C@H]3C[C@H](CNC3)C2=C1
InChI
InChIKey=RNOBTWYQAWEZHH-JGVFFNPUSA-N
InChI=1S/C12H12F3N/c13-12(14,15)9-1-2-10-7-3-8(6-16-5-7)11(10)4-9/h1-2,4,7-8,16H,3,5-6H2/t7-,8+/m0/s1
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor partial agonist developed by Pfizer. The compound has antidepressant-like activity in animal models and was investigated in a phase 2 trial as an augmentation to other antidepressant therapy in patients with Major Depressive Disorder. However, CP-601927 ultimately lacked efficacy as an adjuvant in these patients because of insufficient activity of α4β2 at therapeutic doses.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Species differences in the biotransformation of an alpha 4 beta 2 nicotinic acetylcholine receptor partial agonist: the effects of distinct glucuronide metabolites on overall compound disposition. | 2010 Feb |
|
| Toxicity study in juvenile rats with the α4β2 nicotinic acetylcholine receptor partial agonist CP-601,927. | 2011 Aug |
|
| Therapeutic doses of antidepressants are projected not to inhibit human α4β2 nicotinic acetylcholine receptors. | 2013 Sep |
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1448551-01-6
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11498153
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357425-02-6
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CHEMBL3707250
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DB12244
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VI5LR1EU47
Created by
admin on Sat Dec 16 10:06:01 GMT 2023 , Edited by admin on Sat Dec 16 10:06:01 GMT 2023
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ACTIVE MOIETY
