133040-01-4 Usage
Description
Eprosartan, also known by its brand name Teveten, is a member of the class of imidazoles and thiophenes. It is an angiotensin II receptor antagonist used for the treatment of high blood pressure. Eprosartan is a potent, highly selective, competitive antagonist with no agonist activity. It selectively targets the AT1 subtype receptor and has a duration of action similar to Enalapril, lasting for more than 12 hours. The drug rapidly dissociates from the receptor, but its prolonged duration of action is likely due to slow removal from compartments within tissue, cells, or matrix around the AT1 receptor. Eprosartan is a light-yellow solid and is not bound by bovine serum albumin (BSA).
Uses
Used in Pharmaceutical Industry:
Eprosartan is used as an antihypertensive agent for the treatment of hypertension. It functions as a prototype of the imidazoleacrylic acid angiotensin II receptor antagonists, helping to regulate blood pressure by blocking the effects of angiotensin II, a potent vasoconstrictor.
Used in Research and Development:
Eprosartan (E590100) is utilized as an impurity in the development and testing of new drugs related to hypertension treatment. This application aids in understanding the drug's behavior, side effects, and potential interactions with other substances.
Used in Chemical Synthesis:
Eprosartan serves as a starting point for the synthesis of various related compounds in the imidazoleacrylic acid angiotensin II receptor antagonist class. This application is crucial for the development of new drugs with improved properties or alternative mechanisms of action.
Originator
SmithKline Beecham (UK)
Clinical Use
Angiotensin-II antagonistHypertension
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 impairment with ACE
inhibitors and aliskiren.Ciclosporin: increased risk of hyperkalaemia and
nephrotoxicity.Diuretics: enhanced hypotensive effect;
hyperkalaemia with potassium-sparing diuretics.Epoetin: increased risk of hyperkalaemia;
antagonism of hypotensive effect.Lithium: reduced excretion, possibility of enhanced
lithium toxicity.Potassium salts: increased risk of hyperkalaemia.Tacrolimus: increased risk of hyperkalaemia and
nephrotoxicity.
Metabolism
Following oral and intravenous dosing with [14C]
eprosartan in human subjects, eprosartan was the only
drug-related compound found in the plasma and faeces.
In the urine, approximately 20% of the radioactivity
excreted was an acyl glucuronide of eprosartan with the
remaining 80% being unchanged eprosartanEprosartan is eliminated by both biliary and renal
excretion. Following intravenous [14C] eprosartan,
about 61% of radioactivity is recovered in the faeces and
about 37% in the urine. Following an oral dose of [14C]
eprosartan, about 90% of radioactivity is recovered in the
faeces and about 7% in the urine.
Check Digit Verification of cas no
The CAS Registry Mumber 133040-01-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,0,4 and 0 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 133040-01:
(8*1)+(7*3)+(6*3)+(5*0)+(4*4)+(3*0)+(2*0)+(1*1)=64
64 % 10 = 4
So 133040-01-4 is a valid CAS Registry Number.
InChI:InChI=1/C23H24N2O4S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29)/b18-12+
133040-01-4Relevant articles and documents
1-(Carboxybenzyl)imidazole-5-acrylic Acids: Potent and Selective Angiotensin II Receptor Antagonists
Weinstock, Joseph,Keenan, Richard M.,Samanen, James,Hempel, Judith,Finkelstein, Joseph A.,et al.
, p. 1514 - 1517 (1991)
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COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE
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, (2015/02/05)
To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.
AN IMPROVED PROCESS FOR THE PREPARATION OF PURE EPROSARTANAND ITS PHARMACEUTICAL ACCEPTABLE SALTS
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Page/Page column 7, (2011/05/11)
The present invention relates to an improved process for preparation of pure Eprosartan and its pharmaceutical acceptable salts comprising the steps of: a) treating the Eprosartan with hydrochloric acid; b) suspending the resulted Eprosartan hydrochloride
