5 results for "Vasopressin Receptor Antagonists" in Products

Vasopressin Receptor Antagonists

Vasopressin receptors are a group of G-protein-coupled receptors that mediate vasoconstriction, antidiuresis and ACTH release. They are currently divided into three subtypes, V1A, V1B and V2 and are closely related to oxytocin receptors (OT).

V1A is coupled to Gq/11 proteins and is found at high density on smooth muscle cells. It is involved in regulation of blood pressure through arterial vasoconstriction and has been found to stimulate VEGF secretion. V1B is located in the hypothalamus, where it controls ACTH secretion, and in the pancreas, where it is involved in insulin release. V2 is coupled to Gs proteins and is found exclusively on the basolateral membrane of collecting duct cells in the kidney, where it regulates water excretion.

Selective, orally active vasopressin V1A receptor antagonist

Alternate Names: Relcovaptan
Chemical Name: (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide
Purity: ≥98%
Selective, orally active vasopressin V1A receptor antagonist
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Selective vasopressin V1A antagonist

Purity: ≥95%
Selective vasopressin V1A antagonist
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Potent and selective vasopressin V1B antagonist

Alternate Names: Nelivaptan
Chemical Name: (2S,4R)-1-[(3R)-5-Chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-(2-methoxyphenyl)-2-oxo-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidinecarboxamide
Purity: ≥98%
Potent and selective vasopressin V1B antagonist
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Potent and selective vasopressin V2 receptor antagonist; renoprotective and orally active

Alternate Names: OPC-41061
Chemical Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Purity: ≥98%
Potent and selective vasopressin V2 receptor antagonist; renoprotective and orally active
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Potent and selective V1B receptor antagonist; orally bioavailable

Chemical Name: 2-(3-Chloro-4-fluorophenyl)-N-(1-methylethyl)-6-[3-(4-morpholinyl)propoxy]-4-oxo-pyrido[2,3-d]pyrimidine-3(4H)-acetamide hydrochloride
Purity: ≥98%
Potent and selective V1B receptor antagonist; orally bioavailable
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