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  • Oxford University Press (OUP)  (2)
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  • Oxford University Press (OUP)  (2)
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  • 1
    Online Resource
    Online Resource
    Oxford University Press (OUP) ; 2011
    In:  Journal of Pharmacy and Pharmacology Vol. 43, No. 5 ( 2011-04-12), p. 331-336
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 43, No. 5 ( 2011-04-12), p. 331-336
    Abstract: This study has been undertaken to determine whether pentazocine induces catecholamine efflux from the adrenal medulla as a mechanism for its sympathomimetic effect. Dog isolated adrenals were perfused retrogradely with modified Locke's solution. The efflux of catecholamines from dog perfused adrenals was increased from the resting output of 0.18 ± 0.04 μg min−1 (mean ± s.e.), to 0.47 ± 0.13 μg min−1 by the administration of pentazocine (50 μM). The pentazocine-induced catecholamine efflux was dose-dependent in the 50–400 μM dose range. This effect of pentazocine was not inhibited by either a combination of atropine and (+)-tubocurarine, or verapamil, in contrast to acetylcholine-induced catecholamine release. There was no significant difference in potency among stereoisomers, i.e. (+)-, (—) and (+)-pentazocine, in inducing catecholamine efflux. Naloxone did not influence the effects of either (+)-or (—)-pentazocine. The interaction of pentazocine with acetylcholine-induced catecholamine release was also examined. Both (+)-and (—)-pentazocine inhibited acetylcholine-induced catecholamine release dose-dependently, and these inhibitory effects were not reversed by naloxone. Acetylcholine-induced catecholamine release was accompanied by increased dopamine-β-hydroxylase release, whereas pentazocine-induced catecholamine efflux was not. These results suggest that pentazocine directly acts on the adrenal medulla to induce catecholamine efflux via a non-exocytotic mechanism, and that opioid receptors do not play a role in this action.
    Type of Medium: Online Resource
    ISSN: 2042-7158 , 0022-3573
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2011
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
    Location Call Number Limitation Availability
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  • 2
    Online Resource
    Online Resource
    Oxford University Press (OUP) ; 2011
    In:  Journal of Pharmacy and Pharmacology Vol. 45, No. 7 ( 2011-04-12), p. 632-635
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 45, No. 7 ( 2011-04-12), p. 632-635
    Abstract: This study was carried out to determine the relative potencies of local anaesthetics to inhibit the cholinergic synaptic transmission using cultured bovine adrenal chromaffin cells, and to clarify if the inhibitory action would correlate with biophysical and pharmacological properties. Local anaesthetics (bupivacaine, etidocaine, tetracaine, lignocaine and procaine; 0·02–2 Mm) inhibited carbachol-induced catecholamine release from the cells in a concentration-dependent manner. This inhibition was completely reversible. IC50 (concentration of 50% inhibition) of each anaesthetic showed no correlation with the lipid solubility. The local anaesthetics showed greater inhibitory potency at a higher extracellular pH. The results suggest that clinically relevant concentrations of local anaesthetics inhibit the stimulus-secretion coupling in the chromaffin cells. The un-ionized base form plays a major role, and the inhibitory potency does not depend on the lipid solubility of the anaesthetics.
    Type of Medium: Online Resource
    ISSN: 2042-7158 , 0022-3573
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2011
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
    Location Call Number Limitation Availability
    BibTip Others were also interested in ...
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