Repositioning Candidate Details
| Candidate ID: | R0433 |
| Source ID: | DB01170 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Guanethidine |
| Synonyms: | (2-(hexahydro-1(2h)-azocinyl)ethyl)guanidine; (2-(Octahydro-1-azocinyl)ethyl)guanidine; 2-(1-N,N-Heptamethyleneimino)ethylguanidine; 2-(1'-Azacyclooctyl)ethylguanidine; Azocine, 1-(2-guanidinoethyl)octahydro-; Guanethidine; Guanidine, (2-(hexahydro-1(2H)-azocinyl)ethyl)-; Heptamethylenimine, 1-(2-guanidinoethyl)-; N-(2-Perhydroazocin-1-ylethyl)guanidine |
| Molecular Formula: | C10H22N4 |
| SMILES: | NC(N)=NCCN1CCCCCCC1 |
| Structure: |
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| DrugBank Description: | An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. |
| CAS Number: | 55-65-2 |
| Molecular Weight: | 198.3085 |
| DrugBank Indication: | For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension. |
| DrugBank Pharmacology: | High blood pressure can cause the heart and arteries to not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanethidine works by decreasing the heart rate and relaxing the blood vessels so that blood can flow more easily through the body, thereby reducing these risks. It is a postganglionic sympathetic nerve terminal blocker that prevents the release of norepinephrine from nerve terminals. |
| DrugBank MoA: | Guanethidine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine (NE), rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters to be concentrated within the transmitter vesicles in place of NE, leading to gradual depletion of NE stores in the nerve endings. Guanethidine at the nerve terminal blocks the release of noradrenaline in response to an action potential. In contrast to ganglionic blocking agents, Guanethidine suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, Guanethidine lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more. |
| Targets: | Sodium-dependent noradrenaline transporter inducer |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I16 | 6713 | Cerebrovascular disease | An vascular disease that is characterized by dysfunction of the blood vessels supplying the brain. http://en.wikipedia.org/wiki/Cerebrovascular_disease, http://www.ncbi.nlm.nih.gov/books/NBK378/ | disease of anatomical entity/ cardiovascular system disease/ vascular disease/cerebrovascular disease | Details |
| 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 |