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  • 1
    Electronic Resource
    Electronic Resource
    Effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on 5-HTP-induced head shaking and behavioral symptoms induced by 5-methoxy-N,N,dimethyltryptamine in rats: comparison with some other 5-HT receptor antagonists (1987)
    Springer
    Psychopharmacology 92 (1987), S. 520-523 
    Details
    ISSN: 1432-2072
    Keywords: 5-Hydroxytryptophan ; Head shakes ; 5-Methoxy-N,N-dimethyltryptamine ; Forepaw treading ; Tremor ; ICS 205-930 ; MDL 72222 ; Pirenperone ; Ketanserin ; Methysergide ; 5-HT receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on head shaking behavior induced by l-5-HTP and behavioral symptoms induced with 5-methoxy-N,N,-dimethyltryptamine (5-MeODMT) in rats was evaluated. Both drugs dose-dependently reduced l-5-HTP-induced head shaking but were at least 600 times less potent than pirenperone and ketanserin and at least 50 times less potent than methysergide. ICS 205-930 and MDL 72222 were more than 1000 times less potent than pirenperone or methysergide and 100 times less potent than ketanserin in blocking 5-MeODMT-induced forepaw treading and tremor. Since it appears that head shakes induced by l-5-HTP are mediated by 5-HT2 receptors, these data suggest that ICS 205-930 and MDL 72222 do not significantly interact with 5-HT2 receptors in the brain. Furthermore, the data suggest that ICS 205-930 and MDL 72222 lack appreciable antagonistic activity at the 5-HT receptor(s) mediating those behavioral effects induced by 5-MeODMT.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00176488
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  • 2
    Electronic Resource
    Electronic Resource
    Discriminative stimulus properties of muscarinic agonists (1987)
    Springer
    Psychopharmacology 93 (1987), S. 139-145 
    Details
    ISSN: 1432-2072
    Keywords: Arecoline ; Pilocarpine ; Oxotremorine ; Acetylcholine ; Muscarinic agonist ; Drug discrimination
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In a two-lever, food-reinforced drug-discrimination paradigm separate groups of rats were trained to discriminate either arecoline, pilocarpine or oxotremorine from saline. The discriminative cues of all three agonists were potently blocked by scopolamine, but only by 30–60 fold higher doses of methylscopolamine. The three agonists all suppressed overall response rate. These rate-suppressant effects were not blocked by scopolamine in doses which blocked the discriminative cues. In generalization tests, arecoline elicited selection of the drug-appropriate lever in all groups of trained animals. Pilocarpine was discriminated as drug by all pilocarpine-trained animals and by a majority of oxotremorine-trained animals, but was not significantly discriminated by the arecoline-trained group. Oxotremorine was discriminated by all oxotremorine-trained animals but only by some pilocarpine-trained animals, and was not significantly discriminated by the arecoline-trained group. Morphine, haloperidol, chlordiazepoxide, pentobarbital and nicotine were not generalized to any of the training drugs. The discriminative stimuli produced by the training drugs are therefore specific and exhibit properties indicative of an origin at central muscarinic receptors but may not be identical.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00179923
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Differential effects of SKF 10,047 (N-allyl-normetazocine) on peristalsis and longitudinal muscle contractions of the isolated guinea-pig ileum (1982)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 321 (1982), S. 218-222 
    Details
    ISSN: 1432-1912
    Keywords: N-Allyl-Normetazocine ; Opioid receptors ; Guinea-pig ileum ; Peristalsis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The purpose of this study was to investigate the differential involvement of distinct types of opioid receptors in the modulation of intestinal peristalsis compared to electrically induced longitudinal muscle contractions. Like naloxone, the proposed σ-agonist and μ-antagonist SKF 10,047 (N-allyl-normetazocine) dose-dependently enhanced peristaltic circular muscle contractions in the isolated guinea-pig ileum. Pre-application of SKF 10,047 at a concentration which itself enhanced peristalsis by 20% on average strongly attenuated the inhibition of peristalsis produced by opioids previously proposed to act via μ-opioid-receptors in the guinea-pig ileum, i.e. normorphine, β-endorphin, d-Ala2-d-Leu5-enkephalin and d-Ser2-l-Leu5-enkephalyl-Thr, but less strongly attenuated the inhibition produced by compounds suggested to act via ϰ-opioid-receptors in this tissue, i.e. ethylketazocine and dynorphin (1–13). In contrast to its effect on peristalsis, SKF 10,047 inhibited the electrically induced contractions of the myenteric plexus-longitudinal muscle preparation in a naloxonereversible fashion. It may be concluded that μ- and ϰ-opioid receptors are of a greater functional significance than σ-receptors in the control of peristalsis. σ-Receptors might participate predominantly in modulating the release of acetylcholine which underlies the electrically induced longitudinal muscle contraction.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00505489
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    Paper (German National Licenses)
    Fulltext
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