RESUMEN
An interactive computer-graphics analysis of 24 antagonists of acetylcholine at peripheral autonomic post-ganglionic (muscarinic) nervous junctions and at similar junctions in the central nervous system, the crystal structures of which are known, has led to the determination of a single, consistent, energetically favorable conformation for all 24 substances, although their observed crystal structure conformations vary widely. The absolute configuration and the single, consistent (ideal) conformation of the chemical groups required for maximum anticholinergic activity are described quantitatively.
Asunto(s)
Fármacos Neuromusculares Despolarizantes , Fármacos Neuromusculares no Despolarizantes , Curare , Compuestos de Decametonio , Trietyoduro de Galamina , Indoles , Modelos Químicos , Modelos Estructurales , Conformación Molecular , Pancuronio , Receptores de Droga , Relación Estructura-Actividad , Estricnina , Succinilcolina , Moldes Genéticos , Toxiferina , TubocurarinaRESUMEN
The molecular configuration of lysergic acid diethylamide (LSD) in crystals of the iodobenzoate has been determined by using x-ray diffraction techniques. The configuration shows strain and steric hindrance and the conformation is fixed. Some of the implications of this for the hallucinogenic activity of LSD are discussed.
Asunto(s)
Dietilamida del Ácido Lisérgico , Modelos Estructurales , Conformación Molecular , Difracción de Rayos XRESUMEN
The three-dimensional structure of O,O',N-trimethyl-d-tubocurarine, a neuromuscular blocking agent, has been determined by x-ray crystallography. This may help to provide insight into its pharmacologic action.
Asunto(s)
Cristalografía , Tubocurarina , Yoduros , Métodos , Modelos Estructurales , Nitrógeno , TemperaturaAsunto(s)
Dioxoles , Compuestos de Amonio Cuaternario , Fenómenos Químicos , Química , Cristalización , Yoduros , Modelos EstructuralesAsunto(s)
Atropina , Receptores de Droga , Acetilcolina , Fenómenos Químicos , Química , Cristalografía , Modelos EstructuralesRESUMEN
A correlation of the crystal structure analyses of the potent nicotinic agonists acetylcholine, acetyl-alpha-methylcholine, lactoylcholine, 1,1-dimethyl-4-phenylpiperazine, and nicotine allows one to determine the conformation of cholinergic agonists relevant to nicotinic nerve receptors.
Asunto(s)
Acetilcolina , Colina , Nicotina , Piperazinas , Células Receptoras Sensoriales , Fenómenos Químicos , Química , ParasimpaticomiméticosRESUMEN
There are only a few possible conformations of D-lysergic acid diethylamide and hallucinogenic derivatives of tryptamine and phenylethylamine. Of these possible conformations there is a high structural correlation among the probable conformations of active hallucinogenic molecules and between these conformations and the known conformations of several central nervous system transmitter molecules.