75438-57-2 Usage
Description
Different sources of media describe the Description of 75438-57-2 differently. You can refer to the following data:
1. Moxonidine, also known as Physiotens, is a highly selective imidazoline receptor agonist-Ⅰ by excitement ventrolateral medulla nucleus (RVLM)-Ⅰ type imidazoline receptor in the peripheral sympathetic nerve activity decreased. This receptor subtype is found in both the rostral ventro-lateral pressor and ventromedial depressor areas of the medulla oblongata.
Moxonidine therefore causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.
It is a new type of antihypertensive drug, commonly used in the treatment of essential hypertension. Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. In contrast, clonidine binds to both receptors with equal affinity.
It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure.
2. Moxonidine, which is structurally related to clonidine, is a new centrally acting
antihypertensive that acts as a stronger agonist at imidazole receptors and a weaker
agonist at α2-adrenergic receptors than clonidine. It is also reported to have less side
effects and a much reduced potential to produce a rebound in blood pressure on
withdrawal. Clinically, moxonidine appears to have comparable antihypertensive
efficacy with the ACE inhibitors and calcium antagonists.
Physical and Chemical Properties
ensity: 1.52g/cm3, boiling point:? 364.7 °C at 760 mmHg, flash point: 174.3 °C, crystallization, melting point: 217-219 degrees Celsius.
Application
By stimulating the central presynaptic alpha 2-receptor and onset, and its antihypertensive effect of ACE inhibitors, calcium antagonists nifedipine and captopril similar. Treatment of essential hypertension.
The intervention of renal interstitial fibrosis can protect the kidney.
Preparation
5-amino-4,6-dichloro-2-methyl pyrimidine and 1-acetyl-2-imidazolin-2-one. The product, reacting with sodium methanol can produce moxonidine.
Precautions
There may be dry mouth, fatigue and headache at the beginning of treatment, occasional dizziness, insomnia, and weakness in the legs and so on.
Sick sinus syndrome, the sinus node and atrioventricular Ⅱ-Ⅲ degree block, resting bradycardia (50 beats/min), unstable angina, severe liver disease, progressive renal dysfunction, angioedema patients should not use it.
References
https://en.wikipedia.org/wiki/Moxonidine
Chemical Properties
White Solid
Originator
Beiersdorf (Germany)
Uses
Different sources of media describe the Uses of 75438-57-2 differently. You can refer to the following data:
1. Moxonidine is an antihypertensive agent.
2. Antihypertensive;Imidazoline receptor agonist
Brand name
Cynt (Lilly); Nucynt (Lilly); Norcynt (Lilly);Physiotens.
Biological Activity
Mixed I 1 imidazoline receptor and α 2 -adrenergic agonist; displays 40-fold higher affinity for I 1 receptors versus α 2 -adrenoceptors. Centrally acting antihypertensive agent.
Clinical Use
Antihypertensive agent (centrally acting agonist at I1
receptor, imidazoline and alpha2
adrenoceptors)
Drug interactions
Potentially hazardous interactions with other drugs
None known
Metabolism
10-20% metabolised, predominantly to
4,5-dehydromoxonidine and to an aminomethanamidine
derivative both of which are much less active than
moxonidine.
Moxonidine and its metabolites are almost entirely
eliminated via the kidney. More than 90% of the dose
is eliminated in the first 24 hours via the kidney, while
approximately 1% is eliminated in the faeces
Check Digit Verification of cas no
The CAS Registry Mumber 75438-57-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,5,4,3 and 8 respectively; the second part has 2 digits, 5 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 75438-57:
(7*7)+(6*5)+(5*4)+(4*3)+(3*8)+(2*5)+(1*7)=152
152 % 10 = 2
So 75438-57-2 is a valid CAS Registry Number.
InChI:InChI=1/C9H12ClN5O/c1-5-13-7(10)6(8(14-5)16-2)15-9-11-3-4-12-9/h3-4H2,1-2H3,(H2,11,12,15)
75438-57-2Relevant articles and documents
SYNTHESIS OF SUBSTITUTED AMINOPYRIMIDINES
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Page/Page column 17; 18, (2015/02/19)
The present invention relates to a novel process for the manufacture of certain substituted aminopyrimidines having Formula (I) or a tautomer or salt thereof, wherein R1 is selected from hydrogen, halogen, C1-4alkoxy, C1-4alklthio, C1-4alkyl, C3-5cycloalkyl, for example R1 is halogen such as chloro; R2 is C1-4alkyl, for example methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), such as methyl; and R3 is selected from hydrogen, C1-4alkoxy, C1-4alkylthio, C1-4alkyl, C3-5cycloalkyl, for example C1-4alkyl such as methyl, ethyl, i-propyl, n-propyl or butyl (any isomer), for example methyl; crystalline forms thereof as well as chemical intermediates suitable for use in performing the process.
PROCESS FOR THE PRODUCTION OF MOXONIDINE
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Paragraph 0057-0058, (2014/08/19)
4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.
Process for the preparation of moxonidine
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Paragraph 0037, (2013/05/09)
The present invention provides an improved process for the preparation of 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)aminopyrimidine. The present invention also provides an improved process for the preparation of moxonidine. The present invention further provides a process for the purification of moxonidine.