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).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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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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Keywords: 3-MPPI, supplier, 5-HT1A, ligand, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenoceptor, Serotonin, Receptors, 5-HT1, α1-adrenergic, alpha1-adrenergic, a1-adrenergic, Tocris Bioscience, Adrenergic α1 Receptor Ligand products
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Selective, high affinity, non-competitive α1A adrenoceptor antagonist
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