4-Bromoacetamidoprocaine: An affinity ligand for brain muscarinic and nicotinic cholinergic receptors

  title={4-Bromoacetamidoprocaine: An affinity ligand for brain muscarinic and nicotinic cholinergic receptors},
  author={Manda Saraswati and Mazzaz Hashmi and Leo G. Abood},
  journal={Neurochemical Research},
This study describes the synthesis, receptor binding characteristics, and some behavioral effects of p-bromoacetamidoprocaine (BAP), a new affinity ligand for brain muscarinic and nicotinic cholinergic receptors. The reversible binding of [3H]QNB to rat brain membranes was inhibited in a concentration dependent and saturable manner by both procaine and BAP, with Ki values of 4×10−6 and 3×10−7 M, respectively, and complete inhibition at 1×10−5 M. Both procaine and BAP, although at much… 

A Potential Cholinergic Mechanism of Procaine's Limbic Activation*

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Analysis of the effects of local anesthetics in terms of an allosteric model of drug action showed that they bind to inactive states of sodium channels with at least a 10-fold higher affinity than active states.

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