82586-52-5 Usage
Description
Moexipril hydrochloride is a novel ACE inhibitor first marketed in the U.S.A. for
the treatment of hypertension as a monotherapy and as a second-line therapy in
combination with diuretics or calcium antagonists. Like other ACE inhibitors, moexipril
is a prodrug that is converted in the liver to its diacid moexiprilat which is the active
agent. Moexipril displays a higher in vitro inhibitory potency to ACE than enalapril
although its effectiveness in reduction of blood pressure in hypertensive patients is
similar to that seen with enalapril. It is orally active with a rapid onset and prolonged
duration of action. Excellent tolerability has been reported. Moexipril is distinguished
by its lower cost than other marketed ACE inhibitors.
Chemical Properties
Crystalline Solid
Uses
Different sources of media describe the Uses of 82586-52-5 differently. You can refer to the following data:
1. Angiotensin converting enzyme (ACE) inhibitor; dimethoxy analog of quinapril
2. Moexipril HCl is a potent orally active non-sulfhydryl angiotensin converting enzyme inhibitor (ACE) with IC50 of 0.041 μM, which is used for the treatment of hypertension and congestive heart failure
Therapeutic Function
Antihypertensive
Hazard
Moderately toxic by ingestion.
Biological Activity
Angiotensin-converting enzyme (ACE) inhibitor that is hydrolyzed in the liver to the active metabolite moexiprilat (IC 50 values are 2.1 and 2700 nM for moexiprilat and moexipril respectively). Antihypertensive; decreases mean blood pressure in the spontaneous hypertensive rat (SHR). Also blocks degradation of bradykinin into inactive metabolites.
Clinical Use
Angiotensin-converting enzyme inhibitor:
Hypertension
Drug interactions
Potentially hazardous interactions with other drugs Anaesthetics: enhanced hypotensive effect.
Analgesics: antagonism of hypotensive effect and
increased risk of renal impairment with NSAIDs;
hyperkalaemia with ketorolac and other NSAIDs.
Antihypertensives: increased risk of hyperkalaemia,
hypotension and renal failure with ARB’S and
aliskiren.
Bee venom extract: possible severe anaphylactoid
reactions when used together.
Ciclosporin: increased risk of hyperkalaemia and
nephrotoxicity.
Cytotoxics: increased risk of angioedema with
everolimus.
Diuretics: enhanced hypotensive effect;
hyperkalaemia with potassium-sparing diuretics.
ESAs: increased risk of hyperkalaemia; antagonism
of hypotensive effect.
Gold: flushing and hypotension with sodium
aurothiomalate.
Lithium: reduced excretion (possibility of enhanced
lithium toxicity).
Potassium salts: increased risk of hyperkalaemia.
Tacrolimus: increased risk of hyperkalaemia and
nephrotoxicity.
Metabolism
Moexipril is a prodrug that is converted to an active
metabolite, moexiprilat in the gastrointestinal mucosa and
liver.
Moexipril is excreted mainly in the urine as moexiprilat,
unchanged drug, and other metabolites; some moexiprilat
may also be excreted in the faeces.
Check Digit Verification of cas no
The CAS Registry Mumber 82586-52-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,2,5,8 and 6 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 82586-52:
(7*8)+(6*2)+(5*5)+(4*8)+(3*6)+(2*5)+(1*2)=155
155 % 10 = 5
So 82586-52-5 is a valid CAS Registry Number.
InChI:InChI=1/C27H34N2O7.ClH/c1-5-36-27(33)21(12-11-18-9-7-6-8-10-18)28-17(2)25(30)29-16-20-15-24(35-4)23(34-3)14-19(20)13-22(29)26(31)32;/h6-10,14-15,17,21-22,28H,5,11-13,16H2,1-4H3,(H,31,32);1H/t17-,21-,22-;/m0./s1
82586-52-5Relevant articles and documents
Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types
Klutchko,Blankley,Fleming,Hinkley,Werner,Nordin,Holmes,Hoefle,Cohen,Essenburg
, p. 1953 - 1961 (2007/10/02)
-
SUBSTITUTED ACYL DERIVATIVES OF 1,2,3,4-TETRAHYDROISOQUINOLINE-3-CARBOXYLIC ACIDS
-
, (2008/06/13)
Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof are produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and when desired hydrolyzing or removing protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.
