An α-AR antagonist; inhibits norepinephrine-induced contractions in rat vas deferens

Dapiprazole (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
72822-13-0
Storage:
-20
UN-No:
Non-Hazardous - /

Dapiprazole is an α-adrenergic receptor (α-AR) antagonist.{48750} It inhibits norepinephrine-induced contractions in rat vas deferens, guinea pig spleen, and rat aorta, regions that express high levels of α1A-AR, α1B-AR, and α1D-ARs, respectively (pA2s = 7.93, 7.13, and 8.26, respectively). It also inhibits contractions induced by histamine, angiotensin II, pentagastrin (Item No. 28546), carbamoylcholine (carbachol; Item No. 14486), and serotonin (Item No. 14332) in guinea pig ileum in a dose-dependent manner.{48751} Dapiprazole (0.05%, intracameral) reverses pupil dilation induced by a combination of the α1A-AR agonist phenylephrine and the muscarinic M4 antagonist tropicamide (Item No. 16606) in rabbits.{48752} Formulations containing dapiprazole have been used in the treatment of iatrogenically induced mydriasis by adrenergic or parasympatholytic agents in certain eye examinations.  

 

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Description

An α-AR antagonist; inhibits norepinephrine-induced contractions in rat vas deferens, guinea pig spleen, and rat aorta, regions that express high levels of α1A-AR, α1B-AR, and α1D-ARs, respectively (pA2s = 7.93, 7.13, and 8.26, respectively); inhibits histamine-, angiotensin II-, pentagastrin-, carbachol, and serotonin-induced contractions in guinea pig ileum in a dose-dependent manner; reverses pupil dilation induced by the combination of phenylephrine and tropicamide in rabbits

Formal name: 5,6,7,8-tetrahydro-3-[2-[4-(2-methylphenyl)-1-piperazinyl]ethyl]-1,2,4-triazolo[4,3-a]pyridine, monohydrochloride

Synonyms: 

Molecular weight: 361.9

CAS: 72822-13-0

Purity: ≥98%

Formulation: A crystalline solid

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