Search results for "acetylcholine receptor"
showing 10 items of 263 documents
ChemInform Abstract: Regioisomeric 5(3)-Aminomethyl-3(5)-phenylisoxazoles: Synthesis, Spectroscopic Discrimination, and Muscarinic Activity.
2010
The regioselective synthesis of isomeric 5(3)-aminomethyl-3(5)-phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea-pig ileum and atria as well as on isolated rabbit vas deferens. Regioisomere 5(3)-Aminomethyl-3(5)-phenyl-isoxazole: Synthese, spektroskopische Unterscheidung und muskarinische Aktivitat Es werden verschiedene Verfahren zur regioselektiven Darstellung von 5(3)-Aminomethyl-3(5)-phenyl-isoxazolen beschrieben, die anhand ihrer spektroskopischen Daten, insbesondere der massenspektrosk…
Altered receptor binding densities in experimental antiphospholipid syndrome despite only moderately enhanced autoantibody levels and absence of beha…
2013
Abstract Experimental antiphospholipid syndrome (eAPS) in Balb/c mice causes neuropsychiatric abnormalities including hyperactivity, increased explorative behavior and cognitive deficits. Recently, we have demonstrated that these behavioral changes were linked to an upregulation of serotonergic 5-HT1A receptor binding densities in cortical and hippocampal regions while excitatory and inhibitory neurotransmitter receptors remain largely unchanged. To examine whether the observed behavioral features depend on a critical antibody concentration, mice with only moderately enhanced antiphospholipid antibodies (aPL), about 50–80% of high levels, were analyzed and compared to controls. The staircas…
Mucosa-dependent muscarinic liberation of prostaglandins from rat isolated trachea.
1995
1. The present study examined whether cholinoceptor stimulation modulates the release of arachidonic acid-derived mediators from rat isolate tracheae. 2. Tracheae were preincubated with [3H]-arachidonic acid and the outflow of 3H-compounds was determined. Acetylcholine and the muscarinic agonist, carbachol but not nicotine, increased the rate of tritium outflow maximally by about 30%. The M3 receptor-preferring antagonist rho-fluoro-hexahydrosiladiphenidol was more effective than pirenzepine and methoctramine in antagonizing the effect of acetylcholine. 3. High performance liquid chromatography analysis (methanol gradient) of the released 3H-compounds showed that one peak, co-eluting with […
Pre- and postsynaptic effects of muscarinic agonists in the guinea-pig ileum
1980
The effects of several muscarinic agonists on smooth muscle (postsynaptic effect) and on acetylcholine release (presynaptic effect) were compared in the longitudinal muscle-myenteric plexus preparation of the guinea-pig ileum. 1. For release experiments the acetylcholine stores of the preparation were labelled with 3H-choline. Electrical field stimulation in the absence of a cholinesterase inhibitor caused an outflow of tritium that reflected release of 3H-acetylcholine. The agonists oxotremorine, arecaidinepropargylester, methylfurmethide, muscarine, carbachol, arecoline and pilocarpine inhibited the stimulation-induced outflow in a concentration-dependent manner. At the highest concentrat…
Compensatory mechanisms enhance hippocampal acetylcholine release in transgenic mice expressing human acetylcholinesterase
2001
Central cholinergic neurotransmission was studied in learning-impaired transgenic mice expressing human acetylcholinesterase (hAChE-Tg). Total catalytic activity of AChE was approximately twofold higher in synaptosomes from hippocampus, striatum and cortex of hAChE-Tg mice as compared with controls (FVB/N mice). Extracellular acetylcholine (ACh) levels in the hippocampus, monitored by microdialysis in the absence or presence of 10(-8)-10(-3) M neostigmine in the perfusion fluid, were indistinguishable in freely moving control and hAChE-Tg mice. Muscarinic receptor functions were unchanged as indicated by similar effects of scopolamine on ACh release and of carbachol on inositol phosphate fo…
Cholinergic–Adrenergic Presynaptic Interactions in the Heart and Characterization of the Receptors Involved
1991
ABSTRACT The rabbit perfused atria preparation with the extrinsic sympathetic and vagus innervation intact has been used to study the mutual interactions between the two branches of the autonomic nervous system by measuring the respective transmitter overflow rates upon electrical stimulation. Using this method the stimuli exciting vagus and sympathetic nerves can be applied at selected time intervals which provides an advantage over the common method of field stimulation where all kinds of neurons are stimulated simultaneously. In the absence of drugs, presynaptic interactions resulting in a decreased noradrenaline overflow occurred when the vagal stimuli preceded the sympathetic ones by 3…
Tissue Differences in the Effect of Atropine on the Evoked Release of Acetylcholine
1979
The effect of atropine on the release of acetylcholine (ACh) from different peripheral parasympathetically innervated tissues was investigated. My enteric plexus The longitudinal muscle-myenteric plexus preparation of the guinea-pig was incubated in eserinecontaining Tyrode solution. The ACh release evoked by high K+ (45 or 108 μ) or by the nicotinic drug dimethylphenylpiperazinium (DMPP) (10 pM) was increased by atropine (0.1–10 μ) in a concentration-dependent fashion. Muscarinic agonists (oxotremorine; propargylester of arecaidine) prevented the facilitatory effect of atropine on ACh release. These results suggest that the ACh release from the myenteric plexus is regulated via presynaptic…
Chapter 21 Modulation of acetylcholine release by nitric oxide
1996
Publisher Summary This chapter reviews the studies in which the effects of endogenous and exogenous nitric oxide (NO) on the release of acetylcholine were investigated. As tools for the involvement of endogenous NO, the effects of NO synthase inhibitors on release of acetylcholine were studied. The cholinergic neurons are tonically stimulated by endogenous NO. On the other hand, NO synthase inhibitors fail to change either basal or electrically evoked acetylcholine release from slices of rat hippocampus and striatum. Endogenous and exogenous NO increase basal acetylcholine release from central and peripheral cholinergic neurons. The effect is tetrodotoxin sensitive and calcium-dependent, th…
Different muscarine receptors mediate the prejunctional inhibition of [3H]-noradrenaline release in rat or guinea-pig iris and the contraction of the…
1989
To investigate the muscarine receptor type mediating inhibition of [3H]-noradrenaline release from the isolated rat and guinea-pig iris we have determined the potency of antimuscarinic drugs to antagonize the methacholine-induced inhibition of [3H]-noradrenaline overflow evoked by field stimulation (3 Hz, 2 min). The prejunctional apparent affinities were compared with those obtained for postjunctional muscarine receptors mediating the methacholine-induced contraction of the isolated rabbit iris sphincter muscle. Prejunctional apparent affinity constants of pirenzepine (6.67), himbacine (8.51), methoctramine (7.92), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, 8.00), hexahydro-d…
The Sources of Ca2+ for Muscarinic Receptor-induced Contraction in the Rat Ileum
1996
Abstract The contractile responses obtained by activation of different muscarinic receptor subtypes in the longitudinal muscle of the rat ileum and especially the responses of this muscle to acetylcholine in a Ca2+-free medium have been investigated. In Ca2+-containing solution, acetylcholine elicited similar concentration-dependent contractile responses in the duodenum, jejunum and ileum strips of the rat intestine. The response to a maximal concentration of the agonist (1 μM) consisted of a rapid phasic response followed by a slower tonic one. Nifedipine completely relaxes or inhibits the sustained response and only partially diminishes the phasic one, which suggests that the phasic contr…