82586-52-5 Usage
Uses
Used in Pharmaceutical Industry:
Moexipril hydrochloride is used as an ACE inhibitor for the treatment of hypertension and congestive heart failure. It is a potent, orally active non-sulfhydryl ACE inhibitor with an IC50 of 0.041 μM, offering a more cost-effective alternative to other marketed ACE inhibitors.
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 academic research and scientific papers
N-SUBSTITUTED AMINO ACIDS AS INTERMEDIATES IN THE PREPARATION OF ACYL DERIVATIVES OF 1,2,3,4-TETRAHYDROISOQUINOLINE-3-CARBOXYLIC ACIDS
-
, (2008/06/13)
N-substituted amino acids are described which when coupled with 1,2,3, 4-tetrahydroisoquinolines result in substituted acyl derivatives of 1,2,3, 4-tetrahydroisoquinoline-3-carboxylic acids as anti-hypertensive agents. The novel intermediates are in turn prepared by reacting an amino acid such as alanine with 2-bromo-4-phenyl butanoic acid or an ester thereof.
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.
