ChemInform Abstract: Regioisomeric 3-, 4-, and 5-Aminomethylisoxazoles: Synthesis and Muscarinic Activity.

ChemInform Abstract: Design and Pharmacology of Quinuclidine Derivatives as M2-Selective Muscarinic Receptor Ligands.

Conformational Isomerism in Drug Action: Does the Free Energy of Binding Induce the Pharmacophoric Conformation of Semi-Rigid Muscarinic Agonists?

The physiological neurotransmitter Acetylcholine has been shown to have great molecular flexibility, and because of this, the possibility of forming numerous energetically different conformations. This property makes the determination of the biologically active conformation extremely complicated. In attempts to solve this problem various research groups have tried two basically different approaches: (1) (1) The determination of the energetically most stable conformation using crystallographic methods (X-ray diffraction studies), nuclear magnetic resonance and quantum-mechanical calculations [1–16]. Same workers hypothesized that the energetically most favourable form was also the biological…

Synthese und pharmakologische Wirkung von carbocyclischen Muskarinanalogen

Als carbocyclische Muskarinanaloga wurden das (3-Hydroxycyclopentylmethyl)trimethyl-ammonium-jodid und dessen Acetat dargestellt und am isolierten Ileum des Meerschweinchens untersucht. Synthesis and Pharmacological Activity of Carbocyclic Analogs of Muscarine As carbocyclic analogs of muscarine (3-hydroxycyclopentylmethyl)trimethylammonium iodide and (3-acetoxycyclopentylmethyl)trimethylammonium iodide were synthesized and tested on the isolated guinea pig ileum.