Details
Stereochemistry | ACHIRAL |
Molecular Formula | C9H12ClN5O.ClH |
Molecular Weight | 278.138 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=NC(C)=NC(Cl)=C1NC2=NCCN2
InChI
InChIKey=ZZPAWQYZQVUVHX-UHFFFAOYSA-N
InChI=1S/C9H12ClN5O.ClH/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);1H
Moxonidine is a second-generation, centrally acting antihypertensive drug with a distinctive mode of action. Moxonidine activates I1-imidazoline receptors (I1-receptors). Imidazoline I1-receptor agonism represents a new mode of antihypertensive action to inhibit peripheral alpha-adrenergic tone by a central mechanism. Adrenaline, noradrenaline and renin levels are reduced, a finding consistent with central inhibition of sympathetic tone. Moxonidine acts centrally to reduce peripheral sympathetic activity, thus decreasing peripheral vascular resistance. In patients with mild to moderate hypertension, moxonidine reduces blood pressure (BP) as effectively as most first-line antihypertensives when used as monotherapy and is also an effective adjunctive therapy in combination with other antihypertensive agents. It improves the metabolic profile in patients with hypertension and diabetes mellitus or impaired glucose tolerance, is well tolerated, has a low potential for drug interactions and may be administered once daily in most patients. Moxonidine is a good option in the treatment of patients with mild to moderate hypertension, particularly as adjunctive therapy in patients with the metabolic syndrome.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q9Y2I1|||Q9UFW3 Gene ID: 11188.0 Gene Symbol: NISCH Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8380858 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PHYSIOTENS Approved UsePhysiotens is indicated for the treatment of hypertension. |
|||
Palliative | Unknown Approved UseUnknown |
|||
Palliative | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Blockade by agmatine of catecholamine release from chromaffin cells is unrelated to imidazoline receptors. | 2001 Apr 6 |
|
Interactions of ligands at angiotensin II-receptors and imidazoline receptors. | 2001 Feb |
|
Pharmacodynamic models for the cardiovascular effects of moxonidine in patients with congestive heart failure. | 2001 Jan |
|
[Effect of moxonidine on the cardiac chronotropic regulation in hypertensive rats SHR-SP]. | 2001 Jan-Feb |
|
[ACE-dependent and sympathetic components of blood pressure regulation in patients with essential hypertension]. | 2001 Jul-Aug |
|
Lowering of microalbuminuria in diabetic patients by a sympathicoplegic agent: novel approach to prevent progression of diabetic nephropathy? | 2001 Mar |
|
[Treatment of hypertension in obesity]. | 2001 May |
|
[The alpha 2-adrenergic receptors: molecular structure and in vivo function]. | 2001 Sep |
|
[Clinical assessment of prolonged therapy of patients with hypertension and diabetes with imidazoline receptor agonist moxonidine]. | 2002 |
|
The "unsympathetic" nervous system of heart failure. | 2002 Apr 16 |
|
alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. | 2002 Jan |
|
Naphazoline-induced neuroendocrine changes: increases in ANP and cGMP levels, but suppression of NE, 3H-NE, and cAMP levels in rabbit eyes. | 2002 Jul |
|
Imidazoline receptors in the heart: characterization, distribution, and regulation. | 2002 Jun |
|
Contractile responses of the rat vas deferens after epithelium removal. | 2002 May 3 |
|
Pharmacological evidence of a role for prejunctional imidazoline (I(1)) receptors in ocular function. | 2002 Nov |
|
Characterization of sucrose-induced changes in cardiac phenotype. | 2002 Oct |
|
Quinidine does not affect the renal clearance of moxonidine. | 2002 Sep |
|
[Current views on migraine and anti-migraine preparations]. | 2003 |
|
[Ambulatory monitoring of blood pressure in regular dialysis therapy]. | 2003 Apr |
|
The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X. | 2003 Aug |
|
The I(1)-imidazoline receptor in PC12 pheochromocytoma cells reverses NGF-induced ERK activation and induces MKP-2 phosphatase. | 2003 Aug 1 |
|
Moxonidine displays a presynaptic alpha-2-adrenoceptor-dependent synergistic sympathoinhibitory action at imidazoline-1 receptors. | 2003 Dec |
|
The role of I(1)-imidazoline receptors and alpha(2)-adrenergic receptors in the modulation of glucose and lipid metabolism in the SHROB model of metabolic syndrome X. | 2003 Dec |
|
Identification and pharmacological characterization of a specific agmatine transport system in human tumor cell lines. | 2003 Dec |
|
Non-adrenergic exploratory behavior induced by moxonidine at mildly hypotensive doses. | 2003 Feb 21 |
|
Dual effect of agmatine in the bisected rat vas deferens. | 2003 Mar |
|
Adverse mortality effect of central sympathetic inhibition with sustained-release moxonidine in patients with heart failure (MOXCON). | 2003 Oct |
|
The effects of imidazoline agents on the aggregation of human platelets. | 2004 Feb |
|
Pharmacological therapy can increase capillary density in post-infarction remodeled rat hearts. | 2004 Feb 15 |
Sample Use Guides
In Vivo Use Guide
Sources: https://gp2u.com.au/static/pdf/P/PHYSIOTENS-PI.pdf
Treatment should be started with 0.2 mg Physiotens in the morning. The dose may be titrated after two weeks to 0.4 mg given as one dose or as divided doses (morning and evening) until a satisfactory response is achieved. If the response is still unsatisfactory after a further 2 weeks treatment, the dosage can be increased up to a maximum of 0.6 mg in divided doses (morning and evening). A single daily dose of 0.4 mg and a divided daily dose of 0.6 mg of Physiotens should not be exceeded. Physiotens may be taken with or without food.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15305091
It was investigate the effects of moxonidine on neurons in the rostral ventrolateral medulla (RVLM) with electrophysiological properties similar to premotor sympathetic neurons in vivo. Moxonidine (2-10 microM) was applied to the perfusate on 4 irregularly firing neurons, and 2 regularly firing neurons. Moxonidine (2 microM) produced only minor depolarization in 2 of these neurons. However, on 4 tested neurons, moxonidine (10 microM) elicited a profound inhibitory effect with hyperpolarization (near -20 mV); these neurons practically ceased firing. These changes were partially reversible. The results would indicate that neurons in the RVLM, recorded in vitro and with similar electrophysiological characteristics to a group of neurons previously identified in vivo in the same bulbar region as barosensitive premotor sympathetic neurons, can be modulated by imidazoline-derivative adrenergic agonists. These results could help to understand the hypotensive effects of moxonidine.
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
5RYW07SK5E
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY | |||
|
m7649
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY | Merck Index | ||
|
11231255
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY | |||
|
DBSALT002876
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY | |||
|
75438-58-3
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY | |||
|
DTXSID20996890
Created by
admin on Sat Dec 16 04:17:35 GMT 2023 , Edited by admin on Sat Dec 16 04:17:35 GMT 2023
|
PRIMARY |
SUBSTANCE RECORD