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  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 335 (1987), S. 701-704 
    ISSN: 1432-1912
    Schlagwort(e): Rabbit mesenteric arteries ; Presynaptic opioid receptors ; Neurogenic vasoconstriction ; [Met5]enkephalin
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The perivascular nerves of rabbit mesenteric arteries were stimulated with 15 pulses at 2 Hz, and decreases in external diameter were measured by means of a photoelectric device. Both extra- and intraluminally added [Met5]-enkephalin 1 μmol/l depressed vasoconstriction, although with the second mode of application a larger inhibition occurred. Therefore, in the subsequent experiments all opioids were added into the lumen. [Met5]enkephalin 0.1 μmol/l had no effect. [d-Pen2, l-Pen5]enkephalin 3 μmol/l was less potent than [Met5]enkephalin 1 μmol/l. ICI 174864 1 μmol/l was also without effect when given alone, but antagonized the action of [Met5]enkephalin 1 μmol/l.Ethylketocyclazocine, dynorphin A(1–13), normorphine and DAGO, all 1 μmol/l, were ineffective. [Met5]enkephalin 1 μmol/l did not change the vasoconstriction evoked by the application of noradrenaline (0.1 –3 μmol/l). It is concluded that in the mesenteric artery action potential-induced transmitter release, and in consequence vasoconstriction can be inhibited by the activation of presynaptic opioid δ-receptors.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 334 (1986), S. 48-55 
    ISSN: 1432-1912
    Schlagwort(e): Rabbit jejunal arteries ; Noradrenaline release ; Presynaptic opioid receptors ; Presynaptic α2 ; Ethylketocyclazocine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary We sought for presynaptic, release-inhibiting opioid receptors at the postganglionic sympathetic axons innervating the jejunal arteries of rabbits. Evoked excitatory junction potentials (e.j.p.s; trains of 15 pulses at 1 Hz) as well as the evoked overflow of tritium after preincubation with [3H]-noradrenaline (trains of 120 pulses at 1 Hz) were used to estimate transmitter release. In otherwise untreated tissues ethylketocylazocine reduced neither the e.j.p. amplitudes nor the evoked overflow of tritium; [Met5]-enkephalin depressed the evoked overflow of tritium. Ethylketocyclazocine reduced e.j.p. amplitudes, however, in tissues exposed to either yohimbine, tolazoline or phentolamine, but not in tissues exposed to prazosin. Ethylketocyclazocine also depressed the evoked overflow of tritium when yohimbine was present. The inhibition produced by ethylketocyclazocine in the presence of yohimbine was antagonized by (-)-3-furylmethyl)-α-noretazocine (MR 2266) but not by N,N-diallyl-Tyr-α-aminoisobutyric acid-α-aminoisobutyric acid-Phe-Leu-OH (ICI 174864). It is concluded that the sympathetic neurones of rabbit jejunal arteries possess presynaptic κ-receptors in addition to the previously identified δ-receptors. The κ-receptors become operative only when presynaptic α2-adrenoceptors have been blocked.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 332 (1986), S. 57-61 
    ISSN: 1432-1912
    Schlagwort(e): Opioid receptor types ; Stimulus intensity ; Excitatory junction potential ; Vas deferens
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary In the mouse isolated vas deferens the amplitude of excitatory junction potentials (e.j.p.s) recorded intracellularly from smooth muscle cells varied with the strength of stimulation. Receptor type selective opioids were tested in this preparation. The μ-agonist normorphine (2,000 nmol/l) reduced the amplitude of e.j.p.s and shifted the stimulus-response curve in a parallel way to the right. By contrast, the ϰ-agonist U-50488 (1,000 nmol/l) and the δ-agonist [d-Ala2,d-Leu5]-enkephalin (2 nmol/l) caused a nonparallel shift of the curve. In addition, opioids having a lower selectivity for one type of receptor were also used. The preferential ϰ-agonists ethylketocyclazocine (40 nmol/l) and dynorphin A1–13 (100 nmol/l) produced parallel and nonparallel shifts, respectively. Thus, normorphine and ethylketocyclazocine were more effective in depressing e.j.p.s evoked by low intensities of stimulation than those evoked by high intensities of stimulation. U-50488, dynorphin A1–13 and [d-Ala2,d-Leu5]-enkephalin caused an equal depression of e.j.p.s evoked by either intensity of stimulation. The preferential μ- and δ-antagonists naloxone (1,000 nmol/l) and ICI 154129 (10,000 nmol/l), reversed the action of the respective agonists normorphine and [d-Ala2,d-Leu5]-enkephalin. In addition, ICI 154129 (10,000 nmol/l) reversed the action of dynorphin A1–13, as well. The preferential ϰ-antagonist MR-2266 (1,000 nmol/l) prevented the effect of both ethylketocyclazocine and U-50488. It is concluded that under the conditions of these experiments normorphine and ethylketocyclazocine acted at μ-, U-50488 at ϰ-, and dynorphin A1–13 and [d-Ala2,d-Leu5]-enkephalin at δ-receptors. In the mouse vas deferens more excitable fibres are probably equally sensitive to all three types of opioids, whereas less excitable fibres seem to be more sensitive to δ- and ϰ-, than to μ-agonists.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 4
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 336 (1987), S. 267-273 
    ISSN: 1432-1912
    Schlagwort(e): Rabbit jejunal arteries ; Vasoconstriction ; Excitatory junction potentials ; Neuroeffector transmitter ; Noradrenaline ; Adenosine 5′-triphosphate
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary Vasoconstriction or excitatory junction potentials (e.j.ps) evoked by nerve stimulation (15 field pulses at 2 Hz every 3 min) were recorded in rabbit isolated jejunal arteries. The resting diameter of the arteries and its decrease in response to stimulation was measured by a photoelectric method. Vasoconstriction was insensitive to prazosin 0.1 or 1 μmol/l. Yohimbine 1 μmol/l considerably enhanced, whereas α,β-methylene ATP (α,β-meATP) 1 μmol/l abolished the contractile response. In order to test the effect of exogenously applied transmitter candidates, noradrenaline (0.1–1 μmol/l) and ATP (10–30 μmol/l) were added in concentrations which evoked a vasoconstriction comparable to that induced by electrical stimulation. The action of noradrenaline was prevented by prazosin 0.1 μmol/l, but was unaffected by both yohimbine 1 μmol/l and α,β-meATP 1 μmol/l. α,β-meATP 1 μmol/l depressed the effect of ATP. The e.j.ps evoked by a train of 15 pulses showed facilitation up to the third response and thereafter depression; a partial summation was also observed. Prazosin 0.1 μmol/l did not change the e j.p. amplitudes. By contrast, when yohimbine 0.1 or 1 μmol/l was added to the prazosin-containing medium, both the late e j.ps in the train and the summation were enhanced in a concentration-dependent manner. α,β-meATP 1 μmol/l almost abolished the e.j.ps. In conclusion, in rabbit jejunal arteries, stimulation of postganglionic sympathetic nerves may release noradrenaline together with ATP which is probably the sole neuroeffector transmitter under our conditions. Transmitter release seems to be modulated by the activation of presynaptic α2-adrenoceptors. Under the stimulation conditions of the present experiments the released transmitter does not activate postsynaptic α1-adrenoceptors.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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