Adreno-receptor blocking drug

Smith RL. Polymorphic metabolism of the beta-adreno-receptor blocking drugs and its clinical relevance. Eur J Chn Pharmacol 1985 28(Suppl) 77-84. 

The adverse side-effects of the TCAs, coupled with their toxicity in overdose, provoked a search for compounds which retained their monoamine uptake blocking activity but which lacked the side-effects arising from interactions with Hj, aj-adreno-ceptors and muscarinic receptors. One of the first compounds to emerge from this effort was iprindole, which has an indole nucleus (Fig. 20.3). This turned out to be an interesting compound because it has no apparent effects on monoamine uptake and is not a MAO inhibitor. This, together with its relatively minor antimuscarinic effects, led to it commonly being described as an atypical antidepressant. Mechanisms that could underlie its therapeutic actions have still not been identified but, in any case, this drug has now been withdrawn in the UK. 

Most studies support the view that clonidine and similar drugs exert their antihypertensive action by stimulating central medullary a-adreno-ceptors. Clonidine appears to act directly on the a-receptors since its action in rabbits is not affected by depleting central noradrenergic neurons with 6-hydroxydopamine. These receptors are probably of the pre-synaptic or a2-type and clonidine s actions are blocked by the selective... 

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