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  • 1
    Electronic Resource
    Electronic Resource
    Comparison of [3H]Choline and d-[3H]Aspartate Efflux from Guinea Pig and Human Neocortex (1992)
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 58 (1992), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: The outflow of [3H]choline ([3H]Ch) evoked by electrical field stimulation and the efflux of d-[3H]Asp induced by 35 mM KCl and 1–10 μM ouabain were studied in human and guinea pig cortical slices, kept under identical experimental conditions. [3H]Ch outflow was significantly lower whereas d-[3H]Asp efflux was significantly higher in humans than in guinea pigs. This suggests a different proportion of the two neuronal systems in these two species. Blockade of muscarinic autoreceptors with atropine increased, whereas stimulation of α2 receptors with norepinephrine (NE) reduced, the evoked [3H]Ch outflow to the same extent in human and guinea pig cortical slices. Conversely, NE did not affect ouabain-induced d-[3H]Asp efflux, suggesting that an α2-mediated control is not operative in the glutamatergic cortical structures. Desmethylimipramine, 2–5 μM, was able to increase [3H]Ch outflow through atropine-like mechanisms only in the human. This drug at 20–50 μM inhibited [3H]Ch and d-[3H]Asp efflux in both species, through mechanisms unrelated to its monoamine reuptake blocking properties. Thus, similarities and differences can be detected between humans and guinea pigs with regard to (a) the relative potency of the cholinergic and acidic amino acidergic signals and (b) the modulation of neurotransmitter outflow by drugs acting on auto- and heteroreceptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1471-4159.1992.tb11363.x
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  • 2
    Electronic Resource
    Electronic Resource
    Blockade of nociceptin/orphanin FQ–NOP receptor signalling produces antidepressant-like effects: pharmacological and genetic evidences from the mouse forced swimming test (2003)
    Oxford, UK : Blackwell Science, Ltd
    European journal of neuroscience 17 (2003), S. 0 
    Details
    ISSN: 1460-9568
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Nociceptin/orphanin FQ (N/OFQ), the endogenous ligand of the NOP receptor, regulates several central functions such as pain transmission, learning and memory, fear and anxiety and feeding and locomotor activity. It has been recently reported that NOP receptor antagonists induce antidepressant-like effects in the mouse forced swimming test (FST), i.e. reduce immobility time. This assay was used in the present study for further investigating the involvement of the NOP receptor in depression states. In male Swiss mice, intracerebroventricular injection (i.c.v) of the novel NOP receptor antagonist, UFP-101 (1–10 nmol) dose-dependently reduced the immobility time (control 192 ± 14 s, UFP-101 91 ± 15 s). The effect of 3 or 10 nmol UFP-101 was fully or partially reversed, respectively, by the coadministration of 1 nmol N/OFQ, which was inactive per se. NOP receptor knockout mice showed a reduced immobility time compared with their wild-type littermates (wild-type 215 ± 10 s, knockout 143 ± 12 s). Moreover, i.c.v. injected UFP-101 (10 nmol) significantly reduced immobility time in wild-type mice but not in NOP receptor knockout animals. In conclusion, these results, obtained using a combined pharmacological and genetic approach, indicate that blockade of the N/OFQ-NOP receptor signalling in the brain produces antidepressant-like effects in the mouse FST. These findings support the NOP receptor as a candidate target for the development of innovative antidepressant drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1460-9568.2003.02603.x
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  • 3
    Electronic Resource
    Electronic Resource
    Characterization of nociceptin receptors in the periphery: in vitro and in vivo studies (1999)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 359 (1999), S. 160-167 
    Details
    ISSN: 1432-1912
    Keywords: Key words Nociceptin ; [Phe1Ψ(CH2-NH)Gly2]NC(1 ; 13)NH2 ; Rat and mouse vas deferens ; Guinea pig ileum and renal pelvis ; Blood pressure ; Heart rate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Nociceptin (NC), a series of NC fragments, naloxone as well as the pseudopeptide [Phe1Ψ(CH2-NH)Gly2]NC(1–13)NH2 ([F/G]NC(1–13)NH2) were used to characterize NC receptors in peripheral isolated organs and in vivo. Experiments on isolated organs were performed in the mouse (mVD) and rat (rVD) vas deferens (noradrenergic nerve terminals), in the guinea pig ileum (gpI; cholinergic nerves) and in the renal pelvis (gpRP; sensory nerves), and, in vivo, by measuring the blood pressure (BP) and heart rate (HR) in anaesthetised rats. NC, NCNH2 and NC(1–13)NH2 acted as full agonists with similar affinities, while shorter fragments (e.g. NC(1–12)NH2, NC(1–9)NH2, NC(1–5)NH2) were much weaker or inactive. The inhibitory effects of NC were not modified by naloxone. [F/G]NC(1–13)NH2 acted as an antagonist with similar pA 2-values (6.75 mVD, 6.83 rVD, 7.26 gpI) in the three species. In addition, it blocked NC actions in the rat in vivo. Linear Schild plots with slopes near to unity indicated that [F/G]NC(1–13)NH2 is a competitive antagonist, specific for NC receptors both in vitro (since it was inactive on opioid receptors) and in vivo (since it was inactive against carbachol). [F/G]NC(1–13)NH2 showed a residual agonistic activity in vitro (α = 0.2-0.3 in the rVD and gpI) and especially in vivo (α = 0.4 BP, 0.2 HR). These pharmacological data indicate that NC and related peptides exert their inhibitory effects in peripheral organs of various species by activating the same receptor type. Moreover, [F/G]NC(1–13)NH2 appears to be a useful tool for receptor characterization and classification.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/PL00005338
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  • 4
    Electronic Resource
    Electronic Resource
    Pharmacological characterization of the nociceptin receptor mediating hyperphagia: identification of a selective antagonist (2000)
    Springer
    Psychopharmacology 148 (2000), S. 430-437 
    Details
    ISSN: 1432-2072
    Keywords: Key words Nociceptin ; Orphanin FQ ; Food intake ; Food deprivation ; Neuropeptide Y
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  Rationale: Central injections of nociceptin (NC) stimulate feeding in rats. Objective: The present study evaluated the effect of N-terminal partial sequences or analogues of NC on food intake in male Wistar rats, to characterize pharmacologically the NC receptor mediating the hyperphagic effect. Methods: NC and related peptides were injected into the lateral (LV) or third (3V) cerebroventricle in freely feeding rats. Results: In the LV, NC stimulated feeding. The N-terminal fragment NC(1–13)NH2 proved to be the least active sequence with hyperphagic activity; NC(1–12)NH2 and NC(1–9)NH2 were inactive. [Phe1ψ(CH2-NH)Gly2]NC(1–13)NH2 ([F/G)]NC(1–13)NH2), an analogue of NC(1–13)NH2, markedly stimulated feeding and, coadministered in the LV with NC, never reduced the hyperphagic effect of the natural sequence. These findings suggest that [F/G)]NC(1–13)NH2, which has been reported to act as a NC receptor antagonist in peripheral tissues, be- haves as a full agonist at the central NC receptors controlling feeding. The hyperphagic potencies of NC and [F/G)]NC(1–13)NH2 were much higher following injection into the 3V than in the LV. Another analogue of NC(1–13)NH2, namely [Nphe1]NC(1–13)NH2, injected into the 3V did not stimulate feeding, but reduced the effect of NC. [Nphe1]NC(1–13)NH2 at a dose of 16.8 nmol/rat significantly reduced, and at 168 nmol/rat almost completely abolished the effect of NC (1.68 nmol/rat). The latter dose of [Nphe1]NC(1–13)NH2 significantly reduced also feeding induced by food deprivation, but did not modify the hyperphagic effect of neuropeptide Y (0.3 nmol/rat). Conclusions: The present results confirm the orexigenic effect of NC in freely feeding rats and indicate that [Nphe1]NC(1–13)NH2 may represent a selective NC receptor antagonist to study the physiological and pathophysiological role of NC in feeding behaviour.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002130050073
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacology of endothelins: vascular preparations for studying ETA and ETB receptors (1996)
    Springer
    Molecular and cellular biochemistry 154 (1996), S. 31-37 
    Details
    ISSN: 1573-4919
    Keywords: endothelin ; receptors ; vascular smooth muscle ; rabbit ; ETA and ETB selective antagonists
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology , Medicine
    Notes: Abstract Three rabbit vessels, the carotid and pulmonary arteries and the jugular vein were investigated to identify vascular monoreceptor systems (either ETA or ETB) to be used in structure-activity studies on endothelins and their antagonists. The RbCA has been found to behave as a monoreceptor ETA preparation, since it shows much greater sensitivity to ET-1 than to ET-3 and is insensitive to IRL 1620. The contractile response of the RbCA to ET-1 is reduced in the presence of BQ-123 but is not influenced by BQ-788. The RbPA behaves as a pure ETB system when stimulated with the ETB selective agonist IRL 1620. The contractile effect of IRL 1620 is reduced in the presence of BQ-788 but is not influenced by BQ-123. The RbJV responds to ETA and to IRL 1620 with contractions that are reduced by both BQ-123 and BQ-788, respectively. The RbJV appears to be a mixed ETA and ETB system in which the two functional sites play an equivalent role in the stimulatory contractile response. Thus, contractile ETA and ETB receptors have been found in arterial and venous vessels of the rabbit and some of these vessels provide sensitive and selective (either ETA or ETB) preparations that appear to be adequate for pharmacological studies on ET receptor agonists or antagonists.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00248458
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  • 6
    Electronic Resource
    Electronic Resource
    Candida albicans infection of gastric ulcer frequency and correlation with medical treatment (1985)
    Springer
    Digestive diseases and sciences 30 (1985), S. 178-181 
    Details
    ISSN: 1573-2568
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This paper reports the results of a multicenter prospective study of 188 consecutive patients affected by gastric ulcer, verified by endoscopy, in whom the frequency of a mycotic infection of the lesion was evaluated as well as the eventual influence of such pathology on the efficiency of medical treatment, the healing rate, and the healing time. A mycotic infection, defined as penetration of the periulcerous mucosa by the fungi, was found in only 13 patients (6.9%). No significant differences were found in the healing rate and helaing time among these patients treated with H2-receptor antagonists and a control group of 43 matched gastric ulcer patients treated in the same period with the same therapy. It would appear from the data that mycotic infections of the gastric ulcer do not modify the efficiency of medical treatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01308206
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