57149-07-2 Usage
Description
Naftopidil dihydrochloride, also known as Naftopidil, is a potent postsynaptic-selective alpha-1 adrenergic receptor antagonist. It was launched in Japan for the treatment of dysuria associated with benign prostatic hypertrophy (BPH). Naftopidil is an off-white solid with a slightly higher affinity for the human prostatic alpha-adrenoceptor than for the aortic alpha-adrenoceptor. It also exhibits a 5-HT1A agonistic effect, weak calcium antagonistic activity, and no alpha-2 or beta-adrenoreceptor affinity. In experiments with rats or rabbits, Naftopidil has been shown to be more potent and selective for the urodynamic effect than the hypotensive effect. The major routes of metabolism for Naftopidil are aromatic or aliphatic hydroxylation, producing metabolites with a profile similar to the parent compound. It is available under the brand names Avishot and Flivas.
Uses
Used in Pharmaceutical Industry:
Naftopidil dihydrochloride is used as an antihypertensive agent for the treatment of high blood pressure. It functions as an alpha-blocker, helping to relax blood vessels and improve blood flow, thus reducing blood pressure.
Used in Urology:
Naftopidil dihydrochloride is used as a treatment for dysuria associated with benign prostatic hypertrophy (BPH). It acts as an alpha-1 adrenergic receptor antagonist, which helps to relax the muscles in the prostate and bladder neck, improving urine flow and reducing symptoms of BPH.
Used in Cardiovascular Applications:
Naftopidil dihydrochloride is used as a 5HT1A agonist, which can help in the treatment of certain cardiovascular conditions by modulating the serotonin receptors in the heart and blood vessels.
Used in Research and Development:
Naftopidil dihydrochloride is used as a research compound for studying the effects of alpha-1 adrenergic receptor antagonists on various physiological processes and for the development of new drugs with similar mechanisms of action.
Biological Activity
An α 1 -adrenoceptor antagonist with only weak antagonism at post-junctional α 2 receptors; a potent, persistent antihypertensive and vasodilator.
Check Digit Verification of cas no
The CAS Registry Mumber 57149-07-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,7,1,4 and 9 respectively; the second part has 2 digits, 0 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 57149-07:
(7*5)+(6*7)+(5*1)+(4*4)+(3*9)+(2*0)+(1*7)=132
132 % 10 = 2
So 57149-07-2 is a valid CAS Registry Number.
InChI:InChI=1/C24H28N2O3.2ClH/c1-28-24-11-5-4-10-22(24)26-15-13-25(14-16-26)17-20(27)18-29-23-12-6-8-19-7-2-3-9-21(19)23;;/h2-12,20,27H,13-18H2,1H3;2*1H
57149-07-2Relevant articles and documents
NAFTOPIDIL MONOHYDROCHLORIDE DIHYDRATE AND USE THEREOF FOR PREPARATION OF NAFTOPIDIL
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Paragraph 0030-0034, (2021/07/27)
PROBLEM TO BE SOLVED: To provide an intermediate that is useful for the preparation of naftopidil (Naftopidil, (2RS)-1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalene-1-yloxy)propan-2-ol), and a method for preparing naftopidil using the same. SOLUTION: By freeing naftopidil monohydrochloride dihydrate, naftopidil can be obtained in high yield and high purity. In particular, a purity of 99.99% can be achieved without repeating purification operation such as recrystallization multiple times. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2021,JPOandINPIT
New anticancer agent
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Paragraph 0064-0066, (2017/04/03)
PROBLEM TO BE SOLVED: To provide a compound having excellent anticancer activity equal to or greater than that of naftopidil.SOLUTION: This invention relates to a compound represented by formula (I), where the definition of each symbol is as described in
THERAPY FOR COMPLICATIONS OF DIABETES
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, (2009/07/02)
A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
