Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H24N2O2 |
Molecular Weight | 312.4061 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]12CN(CC(=O)N1CCC3=C2C=CC=C3)C(=O)C4CCCCC4
InChI
InChIKey=FSVJFNAIGNNGKK-QGZVFWFLSA-N
InChI=1S/C19H24N2O2/c22-18-13-20(19(23)15-7-2-1-3-8-15)12-17-16-9-5-4-6-14(16)10-11-21(17)18/h4-6,9,15,17H,1-3,7-8,10-13H2/t17-/m1/s1
Praziquantel, (+)- is the dextrorotated (+) isomer of Praziquantel. Praziquantel (PZQ) is the drug of choice against schistosomiasis. Since exposure of schistosomes to the drug is associated with calcium influx and muscular contraction, calcium channels have been suggested as the target. It is a specific pharmacological effect seen exclusively with the active levo-R(-)stereo isomer of the drug. Praziquantel, (+)- apparently contributes little to the therapeutic efficacy of Praziquantel. In vivo, single 400-mg/kg oral doses of Praziquantel, (-)- and Praziquantel, (+)- achieved worm burden reductions of 100 and 19%, respectively. Moreover, worms treated in vivo with Praziquantel, (+)- displayed an only transient hepatic shift and returned to the mesenteric veins within 24 h.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3397 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24821110 |
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Target ID: CHEMBL340 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24821110 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24982093
400 or 800 mg/kg
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27445457
(S)-Praziquantel showed higher toxicity against L-02 cell line (IC50 =80.4±1.9 μM and 106±2.0 μM, respectively) than (R)-Praziquantel.
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88027IXB7M
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admin on Sat Dec 16 09:12:01 GMT 2023 , Edited by admin on Sat Dec 16 09:12:01 GMT 2023
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57452-97-8
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admin on Sat Dec 16 09:12:01 GMT 2023 , Edited by admin on Sat Dec 16 09:12:01 GMT 2023
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1917817
Created by
admin on Sat Dec 16 09:12:01 GMT 2023 , Edited by admin on Sat Dec 16 09:12:01 GMT 2023
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SUBSTANCE RECORD