A nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes); selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes); selective for rat over human V1 receptors (Kis = 25 and 8

OPC 21268 – 25 mg

Brand:
Cayman
CAS:
131631-89-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

OPC 21268 is a nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes).{46359} It is selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes). It is also selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin; Item No. 24154) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg).{46360} It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.{46361}  

 

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SKU: 27226 - 25 mg Category:

Description

A nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes); selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes); selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively); inhibits pressor responses induced by arginine vasopressin in pithed rats at 0.03-1 mg/kg; inhibits arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg); induces hypotension in aged SHRs and stroke-prone SHRs at 3 mg/kg

Formal name: N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide

Synonyms: 

Molecular weight: 449.5

CAS: 131631-89-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Stroke||Research Area|Cardiovascular System|Vasculature|Vasodilation

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