Identification | |||||||||||
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Name | Saprisartan | ||||||||||
Accession Number | DB01347 | ||||||||||
Type | small molecule | ||||||||||
Description | Saprisartan is an AT1 receptor antagonist. It is based on medications of losartan's prototypical chemical structure. The mode of (functional) AT1 receptor antagonism has been characterized as insurmountable/noncompetitive for saprisartan. It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism.(10579749) | ||||||||||
Structure |
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Categories (*) | |||||||||||
Molecular Weight | 611.431 | ||||||||||
Groups | approved | ||||||||||
Monoisotopic Weight | 610.049723164 | ||||||||||
Pharmacology | |||||||||||
Indication | Saprisartan is used in the treatment of hypertension and heart failure. | ||||||||||
Mechanism of action | Saprisartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Saprisartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Saprisartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors. | ||||||||||
Absorption | Not Available | ||||||||||
Protein binding | Not Available | ||||||||||
Biotransformation | Not Available | ||||||||||
Route of elimination | Not Available | ||||||||||
Toxicity | Not Available | ||||||||||
Affected organisms |
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Interactions | |||||||||||
Drug Interactions |
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Food Interactions | Not Available |
Type-1 angiotensin II receptor | |
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Name | Type-1 angiotensin II receptor |
Gene Name | AGTR1 |
Pharmacological action | yes |
Actions | antagonist |
References | |
DTHybrid score | 0.6666 |