DB00657 - Mecamylamine
| Identification | |
|---|---|
| Name | Mecamylamine |
| Accession Number | DB00657 (APRD00458) |
| Type | small molecule |
| Description | A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. [PubChem] |
| Structure |
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| Categories (*) | |
| Molecular Weight | 167.2911 |
| Groups | approved |
| Monoisotopic Weight | 167.167399677 |
| Pharmacology | |
| Indication | For the treatment of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension |
| Mechanism of action | Mecamylamine is a ganglionic blocker which prevents stimulation of postsynaptic receptors by acetylcholine released from presynaptic nerve endings. The hypotensive effect of Mecamylamine is attributed to reduction in sympathetic tone, vasodilation, and reduced cardiac output, and is primarily postural. |
| Absorption | Mecamylamine is almost completely absorbed from the gastrointestinal tract |
| Protein binding | 40% |
| Biotransformation | Not Available |
| Route of elimination | Mecamylamine is excreted slowly in the urine in the unchanged form. The rate of its renal elimination is influenced markedly by urinary pH. Alkalinization of the urine reduces, and acidification promotes, renal excretion of mecamylamine. Mecamylamine crosses the blood-brain and placental barriers. |
| Toxicity | Not Available |
| Affected organisms |
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| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| Neuronal acetylcholine receptor subunit alpha-2 | |
|---|---|
| Name | Neuronal acetylcholine receptor subunit alpha-2 |
| Gene Name | CHRNA2 |
| Pharmacological action | yes |
| Actions | inhibitor |
| References |
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| DTHybrid score | 0.5502 |