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- 1991 (11) (entfernen)
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- Anorganische Chemie (9)
- Stereoselectivity (2)
- (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride/pharmacology (1)
- (Acetoxymethyl)methylphenylgermane (1)
- (Acetoxymethyl)methylphenylsilane (1)
- Chemische Synthese (1)
- Difenidol (1)
- Hexahydro-difenidol analogues (1)
- Hexahydro-sila-difenidol analogues (1)
- Hexbutinol (1)
- Muscarinic M1 receptors (1)
- Muscarinic receptor antagonists (selective) (1)
- Olfaktorische Analyse (1)
- Superior cervical ganglia (calf) (1)
- Temperaturabhängigkeit (1)
- Trihexyphenidyl (1)
- acetylcholine (1)
- animals (1)
- antihypertensive agents / pharmacology (1)
- aorta, abdominal / drug effects (1)
- aorta, abdominal / physiology (1)
- aorta, abdominal / ultrastructure (1)
- arecoline (1)
- arecoline/analogs & derivatives (1)
- atropine (1)
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- dicyclidol (1)
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- enantiomers of / Muscarinic receptors (1)
- endothelium, vascular / drug effects (1)
- endothelium, vascular / physiology (1)
- hexahydro-difenidol enantiomers (1)
- hexamethonium (1)
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- muscarinic receptor subtypes (1)
- muscle contraction (1)
- muscle relaxation (1)
- norepinephrine (1)
- p-Fluoro-hexahydro-sila-difenidol (1)
- p-fluoro-hexahydro- (1)
- parasympatholytics (1)
- perfumes (1)
- piperidines (1)
- pirenzepine (1)
- rabbits (1)
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Institut
A method was developed to detennine the affinities of antimuscarinic drugs at M\(_1\) receptors. [\(^3\)H](±)-Telenzepine served as radioligand in crude preparations of calf superior cervical ganglia and showed high affinity for a single receptor population. consisting of M1 receptors (K\(_D\) = 1.12 nM). Kinetic experiments showed monophasic association (k\(_1\) =0.017 min\(^{-1}\) nM\(^{-1}\) ) and dissociation (k\(_1\) = 0.017 min\(^{-1}\) ) kinetics, the half-life of dissociation being 41 min at 37°C. The kinetie K\(_D\) value amounted to 1.00 nM. M\(_1\) affinities for pirenzepine, methoctramine. hexahydro-sila-difenidol and p-fluoro-hexahydro-sila-difenidol detennined in competition experiments were similar to those found in functional studies with MI receptors in rabbit isolated vas deferens. The binding assay was used to deterriline the affinities of the (R) and (S) enantiomers of tertiary (trihexyphenidyl, hexahydro-difenidol. hexbutinol, p-fluoro-hexbutinol) and quatemary musearlnie antagonists (trihexyphenidyl methiodide. hexbutinol methiodide). Comparison of results obtained with the rabbit vas deferens suggested that the ionic environment may influence the affinities.