Active Ingredient History

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Pivalopril (RHC 3659-(S); (S)-N-cyclopentyl-N-(2-methyl-3-pivaloylthiopropionyl) glycine) is an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, the free SH metabolite of pivopril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Pivopril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Pivalopril has been compared to captopril for oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs and antihypertensive activity in rats. In separate groups of conscious normotensive rats, pivalopril (0.03-1.0 mg/kg, orally [p.o.]) produced a dose-related antagonism of angiotensin I (AngI)-induced pressor effects. The ED50 for pivalopriland captopril was 0.1 mg/kg. Pivalopril has being shown to be a potent, orally effective ACE inhibitor and antihypertensive agent.   NCATS

  • SMILES: C[C@H](CS)C(=O)N1CCC[C@H]1C(O)=O
  • InChIKey: FAKRSMQSSFJEIM-RQJHMYQMSA-N
  • Mol. Mass: 217.285
  • ALogP: 0.63
  • ChEMBL Molecule:
More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: Yes
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

Australia

$0.0424 - $74.2892

United States

$0.3498 - $12.1910
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Combination drugs

(2s)-1-[(2s)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid | acepress | acepril | apopril | capoten | captolane | captomex | captopril | (-)-captopril | captoprilum | captopryl | captoril | cesplon | cp | d-2-methyl-3-mercaptopropanoyl-l-proline | d-3-mercapto-2-methylpropanoyl-l-proline | dilabar | ecopace | garranil | hypertil | hyteneze 12.5 | hyteneze 25 | hyteneze 50 | kaplon | l-captopril | lopirin | lopril | noyada | s-captopril | sq14225 | sq 14225 | sq-14225 | tenosbon | tensobon | tensoprel

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