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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 321 (1982), S. 218-222 
    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
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  • 2
    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
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