| Identification | More | [Name]
Moxonidine | [CAS]
75438-57-2 | [Synonyms]
4-CHLORO-6-METHOXY-2-METHYL-5-(2-IMIDAZOLIN-2-YL)AMINOPYRIMIDINE HCL
4-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-6-methoxy-2-methyl-3h-pyrimidin-2-amine hydrochloride
4-CHLORO-N-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)-6-METHOXY-2-METHYL-5-PYRIMIDINAMINE HYDROCHLORIDE
BDF-5895 HCL
MOXONIDINE
MOXONIDINE HCL
MOXONIDINE HYDROCHLORIDE
4-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamin
bdf5895
be5895
Moxonidin
4-Chloro-5-(2-imidazolin-2-ylamino)-6-methoxy-2-methylpyrimidine
MOXONIDINE/4-CHLORO-N-(4,5-DIHYDRO-1H-2-IMIDAZOLYL)-6-METHOXY-2-METHYL-5-PYRAMINE
4-Chloro-N-(4，5-dihydro-1H-imidaml-2-y1)-6-methoxy-2-methyl-5-pyrimidinamine
Cynt
Physioterls
4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamine
4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine
Norcynt | [EINECS(EC#)]
629-833-3 | [Molecular Formula]
C9H13Cl2N5O | [MDL Number]
MFCD06795643 | [Molecular Weight]
278.14 | [MOL File]
75438-57-2.mol |
| Chemical Properties | Back Directory | [Melting point ]
217-219° (dec) | [Boiling point ]
364.7±52.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Very slightly soluble in water, sparingly soluble in methanol, slightly soluble in methylene chloride, very slightly soluble in acetonitrile. | [form ]
neat | [pka]
7.11±0.10(Predicted) | [color ]
White to Almost white | [Water Solubility ]
800.3mg/L(temperature not stated) | [Merck ]
14,6293 | [InChIKey]
WPNJAUFVNXKLIM-UHFFFAOYSA-N | [CAS DataBase Reference]
75438-57-2(CAS DataBase Reference) |
| Safety Data | Back Directory | [RIDADR ]
UN 2811 6.1/PG III | [WGK Germany ]
3
| [RTECS ]
UV6260290
| [HS Code ]
2933.99.5300 | [HazardClass ]
6.1 | [PackingGroup ]
III |
| Questions And Answer | Back Directory | [Description]
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. | [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 |
| Hazard Information | Back Directory | [Chemical Properties]
White Solid | [Originator]
Beiersdorf (Germany) | [Uses]
Antihypertensive;Imidazoline receptor agonist | [Uses]
Moxonidine is an antihypertensive agent. | [Definition]
ChEBI: Moxonidine is an organohalogen compound and a member of pyrimidines. | [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 |
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