Imidazoline receptors: a challenge

摘要: Abstract The hypotensive effect of imidazoline-like drugs (IMs) directly injected into the rostroventrolateral part brainstem (NRL/RVLM) was shown to involve non-adrenergic imidazoline specific receptors (IRs). Some IMs caused hypotension when there, irrespective their affinity and selectivity for any α-adrenoceptor subtype. Compounds, such as LNP 509, S 23515, 23757 or benazoline with very high selectivities IRs over α 2 -adrenoceptors (A Rs), became available recently. these compounds (LNP 23515) alone NRL/RVLM region. Nevertheless, will not predict by its own capability elicit some substances behaved antagonists towards effects latter. As far hybrid drugs, i.e., mixed binding profiles (I 1 /α ), were concerned, a significant correlation has been reported between central IRs. Imidazoline antagonists, idazoxan, repeatedly competitively prevent reverse centrally induced IMs. sole stimulation A Rs within region sufficient decrease blood pressure much did, lack lowering α-methylnoradrenaline (α-MNA). No observed effects. It is also noticeable that yohimbine, an antagonist, abolish hybrids but usually in non-competitive manner. Mutation acting drugs. concluded (i) highly selective I can reduce own; (ii) needs implication appears be facilitated additional activation Rs; (iii) this requires intact along sympathetic pathways.