Methylation of imidazoline related compounds leads to loss of alpha(2)-adrenoceptor affinity. Synthesis and biological evaluation of selective I(1) imidazoline receptor ligands.

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Schann S, Greney H, Gasparik V, Dontenwill M, Rascente C, Lacroix G, Monassier L, Bruban V, Feldman J, Ehrhardt JD, Bousquet P

Methylation of imidazoline related compounds leads to loss of alpha(2)-adrenoceptor affinity. Synthesis and biological evaluation of selective I(1) imidazoline receptor ligands.

Bioorg Med Chem. 2012 Aug 1;20(15):4710-5. doi: 10.1016/j.bmc.2012.06.008. Epub 2012 Jun 9.

PubMed ID

22750139 [ View in PubMed

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Abstract

Methylated analogues of imidazoline related compounds (IRC) were prepared; their abilities to bind I(1) imidazoline receptors (I(1)Rs), I(2) imidazoline binding sites (I(2)BS) and alpha(2)-adrenoceptor subtypes (alpha(2)ARs) were assessed. Methylation of the heterocyclic moiety of IRC resulted in a significant loss of alpha(2)AR affinity. Amongst the selective ligands obtained, LNP 630 (4) constitutes the first highly selective I(1)R agent showing hypotensive activity after intravenous administration.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clonidine	Alpha-2A adrenergic receptor	Ki (nM)	8.71	N/A	N/A	Details
Clonidine	Alpha-2B adrenergic receptor	Ki (nM)	31.62	N/A	N/A	Details
Clonidine	Alpha-2C adrenergic receptor	Ki (nM)	9.33	N/A	N/A	Details