Search results for "Sympatholytics"
showing 10 items of 33 documents
The effect of S-(+)-boldine on the α1-adrenoceptor of the guinea-pig aorta
1996
1. The cardiovascular activity of S-(+)-boldine, an aporphine alkaloid structurally related to papaverine, was determined. The work includes functional studies on guinea-pig isolated aorta contracted with noradrenaline, caffeine, KCl or Ca2+, and on guinea-pig trachea contracted with acetylcholine or histamine. 2. S-(+)-boldine inhibited in a concentration-dependent manner the contractile response evoked by noradrenaline (10 microM) in guinea-pig aorta (IC50 = 1.4 +/- 0.2 microM) while the KCl depolarizing solution (60 mM)- or the Ca2+ (1 mM)-induced contractions were only partially affected by boldine up to 300 microM. In contrast, papaverine relaxed noradrenaline (NA), KCl or Ca2+ induced…
Different muscarinic receptors mediate autoinhibition of acetylcholine release and vagally-induced vasoconstriction in the rat isolated perfused heart
1990
Experiments were carried out on rat isolated perfused hearts with both vagus nerves attached. The acetylcholine stores were labelled with [14C]-choline. The effects of muscarinic receptor antagonists on the [14C]-overflow and increase in perfusion pressure evoked by vagus nerve stimulation (10 Hz, 4-10 mA) were studied in order to determine the muscarinic receptor type involved in autoinhibition of acetylcholine release and vagally-induced vasoconstriction in the rat heart. Stimulation of the vagus nerves (1200 pulses) caused an increase in [14C]-overflow and in perfusion pressure which was significantly reduced by hexamethonium 500 mumol/l and abolished by tetrodotoxin 0.3 mumol/l or perfu…
Differentiation of calcium antagonists with respect to their effects in normal and skinned taenia caeci preparations
1987
Abstract In taenia preparations, depolarized by a K+-rich medium, Ca2+ caused contraction and cinnarizine (0.4–100 μM), trifluoperazine (2–100 μM) and verapamil (0.02–10 μM) caused concentration-dependent antagonism of Ca2+, displacing the Ca2+ log concentration-effect curve to the right and depressing the maximal response. Equieffective (IC75) antispasmogenic concentrations were selected. The antispasmogenic effects of verapamil were readily offset by removing the drug from the bathing fluid but those of the other drugs were not. The calcium antagonists (antispasmogenic IC75) were then tested for spasmolytic activity in tissues generating tension in response to the EC80 of Ca2+. Verapamil …
Effects of Intraaccumbens Microinjections of Quinpirole on Head Turning and Circling Movement in the Rat
1998
This study was designed to evaluate whether nucleus accumbens dopamine D2 receptors are involved in the initiation of the movement, as distinguished from its execution. For this purpose, the effects of the quinpirole-induced increase of nucleus accumbens dopamine D2 receptor activity were observed on specific parameters of the circling behavior and of its first stage, the head-turning (HT) movement. The experiments were performed on rats with unilateral 6-hydroxydopamine (6-OHDA) lesion of the pars compacta of the substantia nigra and d-amphetamine i.p. (3 mg/kg). Bilateral intraaccumbens microinjections of quinpirole (1, 5, and 10 microg/0.5 microl), an agonist of the D2 receptor family, w…
Formation and release of acetylpyrrolidinecholine (N-methyl, N-acetoxyethylpyrrolidinium) as a false cholinergic transmitter in the myenteric plexus …
1977
1. Longitudinal muscle strips of the guineapig small intestine were incubated with Tyrode solution containing the choline analogue pyrrolidinecholine. At the end of the incubation the concentrations of acetylcholine and its analogue acetylpyrrolidinecholine were determined in the strips by gas chromatography. 2. After 120 min of incubation with 1 mM pyrrolidinecholine, acetylpyrrolidinecholine comprised about 15% of the total amount of acetylcholine plus acetylpyrrolidinecholine. Electrical stimulation (1 Hz) of the strips during the incubation slightly increased the proportion of acetylpyrrolidinecholine to 21%. 3. The acetylcholine content of control strips increased significantly during …
The effects of methacholine and calcium deprivation on the release of the false transmitter, ?-methyladrenaline, from the isolated rabbit heart
1976
1. Anaesthetized rabbits were infused for 20 min with 85 μg · kg−1 · min−1 (±)-α-methyladrenaline. The hearts dissected 15 min after the infusion contained 1.49 μg/g α-methyladrenaline; the endogenous noradrenaline content was correspondingly decreased. 2. Hearts from α-methyladrenaline-infused animals were isolated with the right sympathetic nerves intact and perfused. Ventricular rate, right atrial and right ventricular tensions were recorded using the transverse method. 3. Electrical stimulation (10 Hz, 1 ms, 1 min) of sympathetic nerves, perfusion with the nicotinic drug, p-aminophenethyltrimethylammonium (PAPETA) or perfusion with 54 mM KCl (high K+) solution evoked an output of both α…
6-Hydroxydopamine lesioning differentially affects α-synuclein mRNA expression in the nucleus accumbens, striatum and substantia nigra of adult rats
2002
The effect of a unilateral 6-hydroxydopamine (6-OHDA) lesion and/or repeated administration of levodopa (L-DOPA) to normal and 6-OHDA-lesioned rats on alpha-synuclein mRNA expression was investigated by in situ hybridization histochemistry. A 6-OHDA lesion of the nigro-striatal pathway alone, confirmed by the loss of nigral tyrosine hydroxylase mRNA expression, markedly decreased alpha-synuclein mRNA in the lesioned substantia nigra (SN). In contrast, the levels of alpha-synuclein mRNA in the denervated striatum and nucleus accumbens were not altered. Chronic administration of L-DOPA to normal or 6-OHDA-lesioned rats had no effect on alpha-synuclein mRNA expression in the SN, striatum or nu…
Die Hemmbarkeit der inhibitorischen Adrenalinbzw. Noradrenalinwirkung durch Adrenolytika
1958
Dibenamine, dihydroergotamine, regitin and priscol were found to antagonize specifically the inhibitory action of adrenaline and noradrenaline on the electrically stimulated isolated ileum of the guinea-pig. The antagonistic action of dibenamine was irreversible.
Der Antagonismus verschiedener Sympatholytica gegen�ber dem inhibitorischen Adrenalin- oder Noradrenalineffekt am elektrisch gereizten Meerschweinche…
1958
Adrenaline and noradrenaline were found to depress the contractions of the electrically stimulated isolated ileum of the guinea-pig; this action was related to the dose. In these experiments smaller amounts of adrenaline were required than those necessary for the depression of the spontaneous movements of the isolated rabbit duodenum.
Functional consequences of prejunctional receptor activation or blockade in the iris.
1994
The iris is innervated by nerves of the sympathetic, parasympathetic, and sensory nervous systems. The terminal nerve fibres are endowed with prejunctional receptors which modulate neurotransmitter release. Activation or blockade of prejunctional receptors by drugs may have an influence on iris smooth muscle tone. Several findings are in favour of the hypothesis that prejunctional receptors may be involved in regulation of iris smooth muscle tone and/or pathophysiological events. (i). Release of acetylcholine from parasympathetic nerves of guinea-pig iris sphincter evoked by electrical stimulation is subject to autoinhibition via prejunctional M2 muscarinic receptors, and the release can be…