Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H24N2O |
Molecular Weight | 260.3746 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CC(C)=C1NC(=O)CN2CCCCCC2
InChI
InChIKey=RJOUHGWLHPOQSA-UHFFFAOYSA-N
InChI=1S/C16H24N2O/c1-13-8-7-9-14(2)16(13)17-15(19)12-18-10-5-3-4-6-11-18/h7-9H,3-6,10-12H2,1-2H3,(H,17,19)
Pincainide is a new beta-amino anilide with local anesthetic properties. It has been shown to be 3 times more potent than lidocaine as a local anaesthetic on desheathed frog sciatic nerve. It was found to be effective against arrhythmias induced in guinea-pigs by ouabain infusion or by administration of adrenaline and chloroform. Pincainide not only inhibited the influx of Ca 2+ and increased 45Ca efflux, thus reducing the contractile responses induced in rat aorta by noradrenaline and high K +, but it also inhibited other effects related to the noradrenaline-induced release of intracellular Ca 2+ stores. Further studies, however, must be performed in experimental models of arrhythmias before the effectiveness of pincainide as an antiarrhythmic drug can be established.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: GO:0005262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4018127 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Comparison of three beta-amino anilides: IQB-M-81, lidocaine and tocainide, on isolated rat atria. | 1983 Nov 11 |
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Effects of pincainide on contractile responses and 45Ca movements in rat isolated vascular smooth muscle. | 1985 May 8 |
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Expression of the focal adhesion protein PINCH in normal and alkali-injured corneas and the role of PMNs. | 2007 Jun |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/4018127
Pincainide (10(-5) to 10(-2) M) produced a dose-dependent inhibition of noradrenaline (NA) and high K+ -induced contractions. Pincainide (5 X 10(-3) M) inhibited the 45Ca influx stimulated by 10(-6) M NA and increased 45Ca efflux.
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NCI_THESAURUS |
C245
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C47793
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ACTIVE MOIETY