Repositioning Candidate Details
| Candidate ID: | R0199 |
| Source ID: | DB00575 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Clonidine |
| Synonyms: | 2-((2,6-Dichlorophenyl)imino)imidazolidine; 2,6-Dichloro-N-2-imidazolidinylidenebenzenamine; Chlofazoline |
| Molecular Formula: | C9H9Cl2N3 |
| SMILES: | ClC1=CC=CC(Cl)=C1NC1=NCCN1 |
| Structure: |
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| DrugBank Description: | Clonidine is an imidazole derivate that acts as an agonist of alpha-2 adrenoceptors. This activity is useful for the treatment of hypertension, severe pain, and ADHD. Clonidine was granted FDA approval on 3 September 1974. |
| CAS Number: | 4205-90-7 |
| Molecular Weight: | 230.094 |
| DrugBank Indication: | Clonidine tablets and transdermal systems are indicated for the treatment of hypertension alone or in combination with other medications. A clonidine injection is indicated for use with opiates in the treatment of severe cancer pain where opiates alone are insufficient. An extended release tablet of clonidine is indicated for the treatment of ADHD either alone or in combination with other medications. Clonidine is also used for the diagnosis of pheochromocytoma, treatment of nicotine dependance, and opiate withdrawal. |
| DrugBank Pharmacology: | Clonidine functions through agonism of alpha-2 adrenoceptors which have effects such as lowering blood pressure, sedation, and hyperpolarization of nerves. It has a long duration of action as it is given twice daily and the therapeutic window is between 0.1mg and 2.4mg daily. |
| DrugBank MoA: | Clonidine is primarily an alpha-2 adrenoceptor agonist which causes central hypotensive and anti-arrhythmogenic effects. The alpha-2 adrenoceptor is coupled to the G-proteins G<sub>o</sub> and G<sub>i</sub>. G<sub>i</sub> inhibits adenylyl cyclase and activates opening of a potassium channel that causes hyperpolarization. Clonidine binding to the alpha-2 adrenoceptor causes structural changes in the alpha subunit of the G-protein, reducing its affinity for GDP. Magnesium catalyzes the replacement of GDP with GTP. The alpha subunit dissociates from the other subunits and associates with an effector. The stimulation of alpha-2 adrenoceptors in the locus coeruleus may be responsible for the hypnotic effects of clonidine as this region of the brain helps regulate wakefulness. Clonidine can also decrease transmission of pain signals at the spine. Finally clonidine can affect regulators of blood pressure in the ventromedial and rostral-ventrolateral areas of the medulla. |
| Targets: | Alpha-2A adrenergic receptor agonist; Alpha-2B adrenergic receptor agonist; Alpha-2C adrenergic receptor agonist; Alpha-1A adrenergic receptor agonist; Alpha-1B adrenergic receptor agonist; Alpha-1D adrenergic receptor agonist |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I12 | 10763 | Hypertension | An artery disease characterized by chronic elevated blood pressure in the arteries. https://en.wikipedia.org/wiki/Hypertension, https://www.ncbi.nlm.nih.gov/pubmed/24352797 | disease of anatomical entity/ cardiovascular system disease/vascular disease/ artery disease | Details |