Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.

Article Details

Citation

Barlocco D, Cignarella G, Montesano F, Leonardi A, Mella M, Toma L

Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.

J Med Chem. 1999 Jan 14;42(1):173-7.

PubMed ID
9888842 [ View in PubMed
]
Abstract

A still unknown tricyclic heterocyclic system (5) was synthesized from 6-hydroxy-2-methylpyridazin-3-one and its structure identified as 2,8-dichloro-6-methylpyrrolo[1,2-b:3,4-d']dipyridazin-5(6H)- one by spectroscopic investigations. Selective condensation of 5 with 2-[4-(2-substituted-phenyl)piperazin-1-yl]ethylamine gave the 2-arylpiperazinylethylamino-8-chloro derivatives 6a-c, which were investigated in binding studies toward the three alpha1-adrenergic and 5-HT1A-serotonergic receptor subtypes. They displayed high potency on all the assays and some selectivity for alpha1a and alpha1d subtypes.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PrazosinAlpha-1A adrenergic receptorKi (nM)0.58N/AN/ADetails
PrazosinAlpha-1B adrenergic receptorKi (nM)0.28N/AN/ADetails
PrazosinAlpha-1D adrenergic receptorKi (nM)0.29N/AN/ADetails