Search results for "Muscari"

Noncompetitive agonism at nicotinic acetylcholine receptors; functional significance for CNS signal transduction.

1995

The alkaloids (-)physostigmine (Phy), galanthamine (Gal) and codeine (Cod), and several derivatives and homologous compounds, can act as noncompetitive agonists (NCA) of nicotinic acetylcholine receptors (nAChR) from Torpedo electrocytes, frog and mammalian muscle cells, clonal rat pheochromocytoma cells, cultured hippocampal neurons and several ectopic expression systems, by interacting with a binding site on the alpha-subunits of these nAChRs that is insensitive to the natural transmitter, acetylcholine (ACh), and ACh-competitive agonists and antagonists. Several endogenous ligands, including opioid-type compounds, can also act via this site, albeit at higher concentrations than is typica…

Therapeutic Modulation of Urinary Bladder Function: Multiple Targets at Multiple Levels

2015

Storage dysfunction of the urinary bladder, specifically overactive bladder syndrome, is a condition that occurs frequently in the general population. Historically, pathophysiological and treatment concepts related to overactive bladder have focused on smooth muscle cells. Although these are the central effector, numerous anatomic structures are involved in their regulation, including the urothelium, afferent and efferent nerves, and the central nervous system. Each of these structures involves receptors for—and the urothelium itself also releases—many mediators. Moreover, hypoperfusion, hypertrophy, and fibrosis can affect bladder function. Established treatments such as muscarinic antago…

Chapter 27: Peptidergic and cholinergic receptors on cultured astrocytes of different regions of the rat CNS

1992

Publisher Summary This chapter discusses whether astrocytes possess peptidergic and cholinergic receptors. There is strong evidence that in addition to neurons, astrocytes also express receptors for neurotransmitters and neuromodulators. The investigations were carried out in explant cultures of the spinal cord, brain-stem, cerebellum, and neocortex of fetal and newborn rats. By the means of autoradiography, it was demonstrated that astrocytes possess binding sites for the vasoactive peptides 3 H-Ang II, 125 I- VIP, 125 I-ET-l, ET-3, and 125 I-AVP. These findings are consistent with electrophysiological studies demonstrating that Ang II, ET, and AVP cause a depolarization of the glial membr…

PRESYNAPTIC MUSCARINIC CONTROL OF NORADRENALINE RELEASE

1980

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

2010

Synthesis and in vitro evaluation of galanthamine derivatives for examination of nicotinic acetylcholine receptor system

2001

ISunmrary: The syntheses and radioactive labeling of several galanthamine derivatives, 6-O-demethyl-6-O-fluoroethylgalanthamine, 10-N-demethyl-lO-Nfluoroethylgalanthamine and N-methylgalanthaminium are reported. First ill vitro evaluations were carried out to determine their properties as allosterically potentiating ligands of nicotinic receptors. N-methylgalanthaminium was found to be a promising candidate for further investigations. The most commonly applied therapeutic approach to balance nicotinic cholinergic deficits in Alzheimer’s disease (AD) patients is the administration of acetylcholinesterase inhibitors (AChE-I) although they have been proven to be of limited therapeutic value [ …

Pre- and Postsynaptic Effects of Muscarinic Antagonists in the Isolated Guinea Pig Ileum

1986

Several compounds have been claimed to differentiate between subtypes of muscarinic receptors (2). In the experiments described in this chapter we have studied in the guinea-pig ileum whether the presynaptic muscarinic receptors of the cholinergic nerves differ from the postsynaptic muscarinic receptors of the longitudinal muscle in their affinities for several muscarinic antagonists (methylatropine; trihexyphenidyl; clozapine; DAMP). Inhibition by oxotremorine of the evoked release of acetylcholine (ACh) was used as a parameter of presynaptic activity, and the increase by oxotremorine of smooth muscle tension as a postsynaptic parameter. The affinity constants (pA2 values) of the antagonis…

Heteroreceptor-mediated modulation of noradrenaline and acetylcholine release from peripheral nerves

2006

Allosteric modulation of nicotinic acetylcholine receptors as a treatment strategy for Alzheimer's disease

2000

The basic symptoms of Alzheimer's dementia, i.e., a loss in cognitive function, are due to impaired nicotinic cholinergic neurotransmission. To compensate for this impairment by drug treatment, blockers of the acetylcholine-degrading enzyme acetylcholinesterase are applied, even though this approach obviously is prone to many side-effects, including those of muscarinic nature. We have recently described a novel class of nicotinic acetylcholine receptor ligands which, similar to the action of benzodiazepines on GABA(A) receptors, allosterically potentiate submaximal nicotinic responses. The sensitizing effect is a consequence of facilitated channel opening in the presence of allosterically p…

Atropine-resistant effects of the muscarinic agonists McN-A-343 and AHR 602 on cardiac performance and the release of noradrenaline from sympathetic …

1974

Abstract 1 The effects of 4-(m-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium chloride (McN-A-343) and N-benzyl-3-pyrrolidyl acetate methobromide (AHR 602) on cardiac performance and noradrenaline release from terminal sympathetic fibres were measured in isolated perfused hearts of rabbits. 2 In the presence of sufficient atropine to block muscarinic receptors, high concentrations of McN-A-343 and AHR 602 caused no cardiac stimulation and there was no increase in the resting output of noradrenaline into the perfusates. 3 McN-A-343 and AHR 602 increased both the mechanical responses and the transmitter overflow evoked by electrical stimulation of the sympathetic nerves (SNS) but inhibi…