Molecular requirements of the active sites of the cholinergic receptors. XIX-Size evaluation of the muscarinic subsite.

Several ethers and acetylderivatives of deoxamuscarine (I) and its isomers have been synthesized and tested to evaluate the volumetric requirements of the site interacting with the hydroxyl moiety of the agonist (muscarinic subsite). The good potency and affinity for the muscarinic receptor shown by some of these compounds will allow the insertion of an alkylating function in this position of the molecule. Such compounds will be useful to get more information on the topography of the active site and in the isolation of the receptor molecule.