Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) Prazosin Alpha-1A adrenergic receptor Ki (nM) 0.58 N/A N/A Details Prazosin Alpha-1B adrenergic receptor Ki (nM) 0.28 N/A N/A Details Prazosin Alpha-1D adrenergic receptor Ki (nM) 0.29 N/A N/A Details