Search results for "Pirenzepine"
showing 10 items of 30 documents
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…
Facilitatory and inhibitory muscarine receptors on the rat phrenic nerve: effects of pirenzepine and dicyclomine
1988
Neuronal transmitter stores of the rat phrenic nerve were labelled by an incubation with [3H]choline. Release of [3H]acetylcholine was elicited either by a short (100 pulses, 5 Hz) or by a long (1500 pulses, 5 or 25 Hz) period of electrical nerve stimulation. Pirenzepine and dicyclomine enhanced transmitter release evoked by the short stimulation period. Both antagonists reduced transmitter release evoked by the long stimulation period. Pirenzepine reduced transmitter release at low concentrations (1 nmol/l) whereas a higher concentration was necessary for the enhancing effect; the opposite pattern was found for dicyclomine. A low concentration of oxotremorine (10 nmol/l) enhanced and a hig…
Inhibitory and excitatory muscarinic receptors modulating the release of acetylcholine from the postganglionic parasympathetic neuron of the chicken …
1992
The effects of muscarinic receptor antagonists on ACh release were studied in the absence or presence of cholinesterase (ChE) inhibition using the isolated perfused chicken heart. Presynaptic inhibitory muscarinic autoreceptor were characterized by determining the potency of various antagonists to enhance [3H]-ACh release evoked by field stimulation (3 Hz, 1 min). The order of potencies was: (±)-telenzepine > atropine > 4-DAMP > silahexocyclium > pirenzepine > hexahydro-siladifenidol > AF-DX 116. The comparison with known pA2 values for M1-, M2- and M3-receptors revealed that the presynaptic autoreceptor meets the criteria of an M1-receptor. Basal, not electrically evoked overflow of unlabe…
Two types of neuronal muscarine receptors modulating acetylcholine release from guinea-pig myenteric plexus
1985
Longitudinal muscle strips of the guinea-pig ileum were incubated with [3H]choline and the effects of muscarinic agonists on smooth muscle contraction and on spontaneous and electrically-evoked outflow of tritium were studied. Muscarine and pilocarpine concentration-dependently increased both muscle contraction and spontaneous outflow of [3H]ACh, and inhibited the electrically-evoked outflow of [3H]ACh. The increase in spontaneous outflow was prevented by tetrodotoxin and scopolamine, but not by hexamethonium. Oxotremorine (1-100 microM) did not increase the spontaneous outflow of tritium. Pirenzepine in concentrations of 10 and 100 nM hardly affected the muscle contractions induced by pilo…
Acetylcholine mediates the release of IL-8 in human bronchial epithelial cells by a NFkB/ERK-dependent mechanism
2007
Acetylcholine may play a role in cell activation and airway inflammation. We evaluated the levels of both mRNA and protein of muscarinic M(1), M(2), M(3) receptors in human bronchial epithelial cell line (16HBE). 16HBE cells were also stimulated with acetylcholine and extracellular signal-regulated kinase1/2 (ERK1/2) and NFkB pathway activation as well as the IL-8 release was assessed in the presence or absence of the inhibitor of Protein-kinase (PKC) (GF109203X), of the inhibitor of mitogenic activated protein-kinase kinase (MAPKK) (PDO9805), of the inhibitor of kinaseB-alpha phosphorilation (pIkBalpha) (BAY11-7082), and of muscarinic receptor antagonists tiotropium bromide, 4-Diphenylacet…
Control of Acetylcholine Release and of Intestinal Motility by Subtypes of Muscarine Receptors
1988
Two types of neuronal muscarine receptors have been investigated in the myenteric plexus preparation of the guinea-pig small intestine: 1. Presynaptic receptors activation of which inhibits the depolarization-evoked release of acetylcholine. Pirenzepine and dicyclomine have low affinities to the release-inhibitory receptors (pA2 values 6.9 and 7.6) which suggests that the presynaptic receptors (similar to the smooth muscle receptors) belong to the M2 subtype. The inhibition of the electrically-evoked acetylcholine release by muscarine (0.01 - 1 μmol/1) was not affected by forskolin (1μmol/l). This indicates that cyclic AMP is not crucially involved in the muscarinic inhibition of acetylchol…
The role of vagus activity in the presynaptic control of noradrenaline release from rabbit atria.
1990
Abstract On various heart preparations with the autonomic innervation left intact, vagus nerve stimulation (VNS) has been found to reduce the amount of noradrenaline (NA) that is released in response to sympathetic nerve stimulation (SNS). The following experiments were carried out on an innervated rabbit perfused atria preparation in which the overflow of NA and acetylcholine (ACh) could be determined simultaneously. VNS impulses applied at a fixed time interval before the corresponding SNS impulses reduced NA overflow when the interval was 3–10 ms (early peak) or 200–283 ms (late peak of inhibition). VNS applied 30–167 ms before SNS had no significant effect (“ineffectual period”). Both i…
Olanzepine-induced tardive dyskinesia
2003
Tardive dyskinesia is a serious and common motor side-effect of treatment with traditional neuroleptics, with an unknown pathophysiological basis. It affects 20-30% of patients on long-term neuroleptic therapy, with elderly patients being at higher risk ( [American Psychiatric Association, 1994][1
Proliferative effect of acetylcholine on rat trachea epithelial cells is mediated by nicotinic receptors and muscarinic receptors of the M1-subtype.
2003
Acetylcholine (ACh), synthesized in mammalian non-neuronal cells such as epithelial cells of the airways, digestive tract and skin, is involved in the regulation of basic cell functions (so-called non-neuronal cholinergic system). In the present experiments rat trachea epithelial cells have been cultured to study the proliferative effect of applied ACh by [3H]thymidine incorporation. ACh (exposure time 24 h) caused a concentration-dependent increase in cell proliferation with a doubling of the [3H]thymidine incorporation at a concentration of 0.1 microM. This effect was partly reduced by 30 microM tubocurarine and completely abolished by the additional application of 1 microM atropine. The …
Effects of indomethacin on muscarinic inhibition of endogenous noradrenaline release from rat isolated trachea
1993
The release of endogenous noradrenaline from rat isolated tracheae was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. The muscarine receptor agonist oxotremorine concentration-dependently inhibited the evoked release of noradrenaline by 95% at 1 μmol/l, EC50 values in two series of experiments 41 and 57 nmol/l, respectively. The effect of oxotremorine was antagonized by the non-selective muscarine receptor antagonist scopolamine (10–1000 nmol/l) in a manner suggesting a simple competitive interaction (slope of Schild plot −0.94; pA2 value 8.88). However, the M2 selective muscarine receptor antagonist methoctramine (0.1–10 μm…