Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H28ClN5O |
Molecular Weight | 377.912 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CN1CCC(CNC(=O)C2=CC(Cl)=C(N)N3C=C(C)N=C23)CC1
InChI
InChIKey=ISKHMDNIWXPUGR-UHFFFAOYSA-N
InChI=1S/C19H28ClN5O/c1-12(2)10-24-6-4-14(5-7-24)9-22-19(26)15-8-16(20)17(21)25-11-13(3)23-18(15)25/h8,11-12,14H,4-7,9-10,21H2,1-3H3,(H,22,26)
Molecular Formula | C19H28ClN5O |
Molecular Weight | 377.912 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18198343
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18198343
CJ-033466 is experimental drug, which acts as selective 5-HT4 serotonin receptor partial agonist. It was originally synthesized at Pfizer Laboratories, and it was specifically exemplified in Pfizer patent applications (WO2003035649 and WO2004026869). In animal tests, it stimulated gastrointestinal motility with 30 times the potency of cisapride. CJ-033,466 does not affect D2 and other 5-HT receptors, and it is a potential therapy for gastroparesis patients.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1875 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18198343 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18198343
CJ-033,466 was administered orally to beagle dogs at 0.03 mg/kg
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18198343
Human 5-HT4d was transfected to HEK293 cells. To evaluate functional effect of the drug, Intracellular cAMP production was measured by fluorimetry. EC50 of CJ-033466 was 0.927 nM, Emax 54% compared to 5-HT.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:24:53 GMT 2023
by
admin
on
Sat Dec 16 08:24:53 GMT 2023
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Record UNII |
9KUW8W70PJ
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Record Status |
Validated (UNII)
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Record Version |
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519148-48-2
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CJ-033466
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9KUW8W70PJ
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10429706
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