75438-58-3 Usage
Description
Moxonidine hydrochloride is a centrally acting antihypertensive agent. Mixed I1 imidazoline receptor and α2-adrenergic agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors.Moxonidine is a selective high-affinity imidazoline I1-receptor agonist and a selectively low-affinity α2-adrenoceptor agonist. It exhibits anti-hypertensive properties by reducing blood pressure efficiently. Moxonidine also exhibits spinal analgesic activity through the α2C-adrenoceptor component.
Uses
Moxonidine is a new-generation centrally acting antihypertensive drug approved for the treatment of mild to moderate essential hypertension. It is suggested to be effective in cases where other agents such as thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or irresponsive. As well, moxonidine has been shown to present blood pressure-independent beneficial effects on insulin resistance syndrome.Moxonidine hydrochloride is used as antihypertensive agent. It has been reported to produce dose-dependent analgesia in multiple acute pain assays and has been reported to potently inhibit the binding of [3H]-clonidine to VLM (ventrolateral medulla) membranes in a dose-dependent manner with the IC50 value of 53 ± 10nM.
Application
Moxonidine hydrochloride has been used:as a standard to study its blood-brain barrier (BBB) permeability in porcine brain lipid extract by parallel artificial membrane permeability assay (PAMPA) method.as a standard to study the chromatographic behavior and lipophilicity by reversed-phase thin-layer chromatography (RP-TLC).as an imidazoline I1 receptor agonist to study its effects on excitatory inputs in airway vagal preganglionic neuron (AVPN).
Biological Activity
Moxonidine is a selective high-affinity imidazoline I1-receptor agonist and a selectively low-affinity α2-adrenoceptor agonist. It exhibits anti-hypertensive properties by reducing blood pressure efficiently. Moxonidine also exhibits spinal analgesic activity through the α2C-adrenoceptor component.
Check Digit Verification of cas no
The CAS Registry Mumber 75438-58-3 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 8 respectively.
Calculate Digit Verification of CAS Registry Number 75438-58:
(7*7)+(6*5)+(5*4)+(4*3)+(3*8)+(2*5)+(1*8)=153
153 % 10 = 3
So 75438-58-3 is a valid CAS Registry Number.
InChI:InChI=1/C9H14ClN5O.ClH/c1-9(15-8-11-3-4-12-8)13-6(10)5-7(14-9)16-2;/h5,14H,3-4H2,1-2H3,(H2,11,12,15);1H
75438-58-3Relevant articles and documents
Synthesis of substituted aminopyridines
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Paragraph 0041, (2015/02/25)
The present invention relates to a novel process for the manufacture of certain substituted aminopyridines 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.