Allosteric Interactions of Quaternary Strychnine and Brucine Derivatives with Muscarinic Acetylcholine Receptors

The affinity and allosteric properties of 22 quaternary derivatives of strychnine and brucine at the m1−m4 subtypes of muscarinic receptors have been analyzed and compared. The subtype selectivity, in terms of affinity, was in general m2 > m4 > m1 > m3. The highest affinities were found for...

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Veröffentlicht in:	Journal of medicinal chemistry 1999-02, Vol.42 (3), p.438-445
Hauptverfasser:	Gharagozloo, Parviz, Lazareno, Sebastian, Popham, Angela, Birdsall, Nigel J. M
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Animals Biological and medical sciences CHO Cells Cholinergic system Cricetinae Humans Medical sciences Muscarinic Antagonists - pharmacology N-Methylscopolamine - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptors, Muscarinic - metabolism Structure-Activity Relationship Strychnine - analogs & derivatives Strychnine - chemistry Strychnine - metabolism
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