By R W Foster (Eds.)
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Extra resources for Basic Pharmacology
These effects are called (rather imprecisely) sympathomimetic effects. Hence agonists at adrenoceptors can also be called directly acting sympathomimetics. Contrast these agents with other drugs that cause the same effects but by different mechanisms - the indirectly acting sympathomimetics. Examples include tyramine-like agents which displace NA from axon terminals (page 48) and agonists at the nicotinic cholinoceptors of ganglia (pages 27 and 48). Structurelactivity relationships for agonists at adrenoceptors Most directly acting sympathomimetics are structural analogues of adrenaline.
This may explain the very brief duration of edrophonium's action in vivo. AChE and ChE are equally sensitive to the actions of the competitive inhibitors. Non-competitive inhibitors Ecothiopate, malaoxon from malathion The inhibition of AChE produced by these agents cannot be overcome by increasing the substrate (for example, ACh) concentration and the inhibited enzyme cannot be reactivated by dialysis - the inhibition is irreversible. 25). Ecothiopate is the only member of the group possessing a quaternized N atom and is therefore the only member of the group that also attaches to the anionic site of AChE.
Prazosin, however, is selective for postjunctional (ax) adrenoceptors and the size of the reflex tachycardia can still be limited by the normal feedback inhibition via prejunctional a2-adrenoceptors. 32 The physiological role of prejunctional a2-adrenoceptors in the heart Other antagonists at a-adrenoceptors have useful properties unrelated to a-adrenoceptor blockade. Chlorpromazine (a phenothiazine) is an antipsychotic which is valuable in the treatment of schizophrenia and can suppress vomiting.