76144-81-5 Usage
Description
Mildronate is a cardiac and neuroprotective drug that was first developed by the Latvia Institute of Organic Synthesis and Grindeks in the former Soviet Union in 1989. It is a structural analog of carnitine and can inhibit carnitine-dependent fatty acid oxidation by competing with carnitine for γ-trimethylaminobutyrate hydroxylase. Mildronate was added to the WADA list of banned substances in 2016 due to evidence of its use by athletes to enhance performance.
Uses
Used in Cardiology:
Mildronate is used as a treatment for angina, myocardial infarction, and chronic heart failure. It helps improve cardiac function and reduce the severity of symptoms associated with these conditions.
Used in Neuroprotection:
Mildronate is used as a neuroprotective agent to protect the brain and nervous system from damage caused by various factors, such as ischemia, oxidative stress, and excitotoxicity.
Used in Pharmaceutical Compositions:
Mildronate is used as a component in novel pharmaceutical compositions based on reverse transcriptase inhibitors. This combination can enhance the therapeutic effects of the drug and provide additional benefits for patients with specific conditions.
Pharmacology
Mildronate is efficient in the treatment of heart is chemia and its
consequences. Extensive evaluation of pharmacological activities of
mildronate revealed its beneficial effect on cerebral circulation
disorders and central nervous system (CNS) functions. The drug is used
in neurological clinics for the treatment of brain circulation
disorders. It appears to improve patients’ mood; they become more
active, their motor dysfunction decreases, and asthenia, dizziness and
nausea become less pronounced. Since the brain does not utilize fatty
acids as fuel other mechanisms of action of mildronate in CNS should be
considered. Several reports indicate the possible existence of an
alternative, non-carnitine dependent mechanism of action of mildronate.
Our recent findings suggest that CNS effects of mildronate could be
mediated by stimulation of the nitric oxide production in the vascular
endothelium by modification of the ? butyrobetaine and its esters pools.
Side effects
Possible side effects of Mildronate treatment were an allergic reaction , weakness , headache , and discomfort in the epigastrium. According to the manufacturer of Mildronate GX, the commercial pharmaceutical product of meldonium, there are some rare adverse effects, including allergic reactions (redness and itchy skin, urticaria, rash, and/or angioedema), dyspepsia, tachycardia, and change (increase or decrease) in blood pressure.
Clinical claims and research
Mildronate (Grindeks, Latvia), an inhibitor of l-carnitine biosynthesis pathway via the inhibition of γ-butyrobetaine dioxygenase, is used for the treatment of myocardial ischemia in Eastern Europe and has shown a neuroprotective effect in several stroke models. Mildronate treatment improves functional recovery following middle cerebral artery occlusion in rats even though the infarct size did not decrease (Svalbe et al 2011). Analysis of cerebellar tissue extracts revealed significant decrease of concentration of l-carnitine and increase of γ-butyrobetaine. Russian studies have reported efficacy of the mildronate in treatment of patients with ischemic stroke. A randomized, double-blind, placebo-controlled phase II clinical trial in ischemic stroke patients is ongoing at the Xijing Hospital in China (ClinicalTrials. gov Identifier: NCT01800357).
Mode of action
Mildronate is a cardioprotective drug, the main mechanism of action of Mildronate is based on carnitine biosynthesis inhibition aimed to prevent accumulation of cytotoxic intermediate products of fatty acid beta-oxidation in ischemic tissues and to block this highly oxygen-consuming process.
Check Digit Verification of cas no
The CAS Registry Mumber 76144-81-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,6,1,4 and 4 respectively; the second part has 2 digits, 8 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 76144-81:
(7*7)+(6*6)+(5*1)+(4*4)+(3*4)+(2*8)+(1*1)=135
135 % 10 = 5
So 76144-81-5 is a valid CAS Registry Number.
InChI:InChI=1/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5?,6-,7-,8?/m1/s1
76144-81-5Relevant articles and documents
Preparation method for mildronate and key intermediate of mildronate
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Paragraph 0021, (2018/02/04)
The invention discloses a preparation method for a drug mildronate for treating heart failure and a key intermediate of the mildronate; the preparation method comprises the following steps: carrying out a reaction of a compound I and a compound II to obtain the intermediate III, and carrying out hydrogenolysis of the compound III, to obtain the mildronate. By the preparation method, the novel key intermediate III is obtained, and the yield and quality of the mildronate can be obviously improved.
CARBONIC AND SULPHURIC ACID SALTS OF 3-(2,2,2-TRIMETHYLHYDRAZINIUM)PROPIONATE ESTERS AND THEIR USE FOR 3-(2,2,2-TRIMETHYLHYDRAZINIUM)PROPIONATE DIHYDRATE PREPARATION
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Page/Page column 8, (2009/10/18)
The present invention relates to carbonic and sulphuric salts of 3-(2,2,2-trimethylhydrazinium)propionate esters and their use for the preparation of 3- (2,2,2-trimethylhydrazinium)propionate dihydrate.
METHOD FOR PRODUCING 3-(2,2,2-TRIMETHYLHYDRAZINIUM)PROPIONATE DIHYDRATE
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Page/Page column 7, (2008/06/13)
A method for producing 3-(2,2,2-trimethylhydrazinium)propionate dihydrate by saponification of salts of 3-(2,2,2-trimethylhydrazinium)propionate esters with subsequent purification step using saturation with carbon dioxide or sulphur dioxide in alcoholic solution.
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