2-(Anilinomethyl)imidazolines with 2'-esters or 2'-amides are potent agonists of the cloned human alpha (1)-adrenoceptors in vitro. The size and shape of the ortho substituent can have significant effects on the potency. efficacy, and subtype selectivity of these 2-(anilinomethyl)imidazolines. alpha (1A)-subtype selective agonists have been identified. (C) 2001 Elsevier Science Ltd. All rights reserved.