Moxonidine
C02A - Antiadrenergic agents, centrally acting
ATC C02AC05
Small molecule
approved 1991
Oral
Natural product
JFDA label: Cynt
Mechanism of Action
Agonist of Nischarin — Nischarin agonist
| Target | Action | Gene / class |
|---|---|---|
| Nischarin efficacy | AGONIST | NISCH · Other cytosolic protein |
Indications
Approved
- Hypertension — hypertension
Off-label
- Heart Diseases
Adverse Reactions
Very Common >10%Common 1–10%Uncommon 0.1–1%
Rare 0.01–0.1%Very Rare <0.01%Not Known
Vascular disorders (2)
Rare Hypotension · Orthostatic hypotension
Nervous system disorders (3)
Rare Dizziness · Headache · Somnolence
Gastrointestinal disorders (2)
Rare Dry mouth · Nausea
Skin and subcutaneous tissue disorders (5)
Rare Angioedema · Dermatitis · Pruritus · Rash · Urticaria
Psychiatric disorders (3)
Rare Anxiety · Insomnia · Sleep disorder
General disorders and administration site conditions (1)
Rare Asthenia
Chemistry & Properties
| Formula | C9H12ClN5O |
|---|---|
| Molecular weight | 241.68 g/mol |
| IUPAC name | 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine |
| CAS | 75438-57-2 |
| PubChem CID | 4810 |
| InChIKey | WPNJAUFVNXKLIM-UHFFFAOYSA-N |
| logP | 0.82 (XLogP 0.6) |
| Polar surface area | 71.43 Ų |
| H-bond acceptors / donors | 6 / 2 |
| Drug-likeness (QED) | 0.75 |
| Lipinski violations | 0 |
SMILES
COc1nc(C)nc(Cl)c1NC1=NCCN1Biology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | Yes |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Substrate | — |
| CYP2C19 | Substrate | — |
| CYP3A4 | Substrate | — |
Receptor binding (top 6)
| Target | Action | Affinity |
|---|---|---|
| α2A-adrenoceptor (ADRA2A) | Agonist | pEC50 8.5 |
| α2A-adrenoceptor (ADRA2A) | Agonist | pIC50 7.5 |
| α2B-adrenoceptor (ADRA2B) | Agonist | pIC50 7.5 |
| α2B-adrenoceptor (ADRA2B) | Agonist | pEC50 7.1 |
| α2C-adrenoceptor (ADRA2C) | Agonist | pEC50 6.9 |
| α2A-adrenoceptor (ADRA2A) | Agonist | pKi 5.0 |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (4)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Cynt | Tablet 0.2 mg | 30 tab pack varies | Abu Sheikha Drug Store | 6.720 |
| Cynt | Tablet 0.4 mg | 30 tab pack varies | Abu Sheikha Drug Store | 6.750 |
| Cynt | Tablet 0.2 mg | 7X14 pack varies | Abu Sheikha Drug Store | 18.660 |
| Cynt | Tablet 0.4 mg | 7X14 pack varies | Abu Sheikha Drug Store | 18.660 |