Cat. No. 0581
Chemical Name: 2-[(4-Phenylpiperazin-1-yl)methyl]-
Biological ActivityVery potent ligand for α1 sites (Ki for displacement of prazosin = 0.2 nM). Displays different binding properties for each α1 subtype (pKi values are 8.74, 9.44 and 9.57 for α1B, α1D and α1A adrenoceptors respectively). Also binds to 5-HT1A sites (Ki = 50 nM).
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Romeo et al (2003) New pyrimido[5,4-b]indoles as ligands for α1-adrenoceptor subtypes. J.Med.Chem. 46 2877. PMID: 12825930.
Russo et al (1991) Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective α1 adrenoceptor ligands. J.Med.Chem. 34 1850. PMID: 1648138.
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