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Potentiation by deprenyl of the autoreceptor-mediated inhibition of [3H]-5-hydroxytryptamine release by 5-methoxytryptamine

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Summary

The 5-hydroxytryptamine (5HT) receptor agonist, 5-methoxytryptamine, inhibited in a concentration-dependent manner the electrically-evoked release of 3H-5HT from superfused rat hypothalamic slices, with an IC50 of 560 nmol/l, without affecting the spontaneous outflow of radioactivity. In the presence of the selective monoamine oxidase B (MAO B) inhibitor, (−)-deprenyl (1 μmol/l), the concentration-effect curve for 5-methoxytryptamine was shifted significantly to the left, and the IC50 was decreased to 25 nmol/l. Under the same experimental conditions, the potency of the 5HT receptor agonist lysergic acid diethylamide (LSD) at inhibiting the electrically-evoked release of 3H-5HT was the same in the presence as well as in the absence of (−)-deprenyl. The IC50 values for LSD were 34 nmol/l in the absence of deprenyl, and 31 nmol/l in the presence of the MAO B inhibitor. It is concluded that deprenyl potentiates the inhibition by 5-methoxytryptamine of 3H-5HT release, by preventing its inactivation through MAO B. Since 5-methoxytryptamine may be present in the pineal gland of some species, the potent effects of this 5-HT receptor agonist on seretoninergic neutrotransmission may be of physiological relevance.

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References

  • Balemans MGM, Pévet P, Van Benthem J, Haldar-Misra C, Smith I, Hendriks H (1983) Day and night rhythmicity in the methylating capacities for different 5-hydroxyindoles in the pineal, the retina and the Harderian gland of the Golden Hamster (Mesocricetus auratus) during the annual seasons. J Neural Transm 56:53–72

    Google Scholar 

  • Beck D, Jonsson G, Lundman A (1981) 5-Methoxyindoles in pineal gland of cow, pig, sheep and rat. Naunyn-Schmiedeberg's Arch Pharmacol 318:49–55

    Google Scholar 

  • Becker RE, Giambalvo C, Fox RA, Macho M (1983) Endogenous inhibitors of monoamine oxidase present in human cerebrospinal fluid. Science 221:476–478

    Google Scholar 

  • Blier P, de Montigny C (1983) Electrophysiological investigations on the effect of repeated zimelidine administration on serotonergic neurotransmission in the rat. J Neurosci 3:1270–1278

    Google Scholar 

  • Bosin TR, Beck O (1979) 5-Methoxytryptamine in the human pineal gland: Identification and quantification by mass fragmentography. J Neurochem 32:1853–1855

    Google Scholar 

  • Bosin TR, Jonsson G, Beck O (1979) On the occurrence of 5-methoxytryptamine in brain. Brain Res 173:79–88

    Google Scholar 

  • De Lean A, Munson PJ, Rodbard D (1978) Simultaneous analysis of families of sigmoidal curves: Application to bioassay, radioligand assay and physiological dose-response curves. Am J Physiol 235:97–102

    Google Scholar 

  • Engel G, Göthert M, Hoyer D, Schlicker E, Hillenbrand K (1986) Identity of inhibitory presynaptic 5-hydroxytryptamine (5HT) autoreceptors in the rat brain cortex with 5HT1B binding sites. Naunyn-Schmiedeberg's Arch Pharmacol 332:1–7

    Google Scholar 

  • Fowler CJ, Tipton KF, MacKay AVP, Youdim MBH (1982) Human platelet monoamine oxidase. A useful enzyme in the study of psychiatric disorders. Neuroscience 7:1577–1594

    Google Scholar 

  • Fuentes JA, Neff NH (1975) Selective monoamine oxidase inhibitor drugs as aids in evaluating the role of type A and B enzymes. Neuropharmacology 14:819–825

    Google Scholar 

  • Galzin AM, Moret C, Verzier B, Langer SZ (1985) Interaction between tricyclic and non-tricyclic 5HT uptake inhibitors and the presynaptic 5HT inhibitory autoreceptors in the rat hypothalamus. J Pharmacol Exp Ther 235:200–211

    Google Scholar 

  • Giambalvo CT (1984) Purification of endogenous modulators of monoamine oxidase from plasma. Biochem Pharmacol 33:3929–3932

    Google Scholar 

  • Göthert M, Schlicker E (1983) Autoreceptor-mediated inhibition of 3H-5-hydroxytryptamine release from rat brain cortex slices by analogues of 5-hydroxytryptamine. Life Sci 32:1183–1191

    Google Scholar 

  • Langer SZ, Moret C (1982) Citalopram antagonizes the stimulation by LSD of presynaptic inhibitory serotonin autoreceptors in the rat hypothalamus. J Pharmacol Exp Ther 222:220–226

    Google Scholar 

  • Langer SZ, Raisman R (1983) Binding of [3H]-imipramine and [3H]-desipramine as biochemical tools for studies in depression. Neuropharmacology 22:407–413

    Google Scholar 

  • Langer SZ, Moret C, Raisman R, Dubocovich ML, Briley M (1980) High-affinity [3H]-imipramine binding in rat hypothalamus: Association with uptake of serotonin but not of norepinephrine. Science 210:1133–1135

    Google Scholar 

  • Neff NH, Garrison CK, Fuentes J, Seaborg JB, Wyatt RJ (1976) Trace amines and the monoamine oxidases. In: Usdin E, Sandler M (eds) Trace amines and the brain, vol 1. Marcel Dekker, Inc., New York Basel, pp 41–57

    Google Scholar 

  • Pévet P (1983) Is 5-methoxytryptamine a pineal hormone? Psychoneuroendocrinology 8:61–73

    Google Scholar 

  • Pévet P, Balemans MGM, de Reuver GF (1981) The pineal gland of the Mole (Talpa europae L) VII Activity of hydroxyindole-O-methyl-transferase (HIOMT) in the formation of 5-methoxytryptophan, 5-methoxytryptamine, 5-methoxy-indole-3-acetic acid, 5-methoxytryptophol and melatonin in the eyes and the pineal gland. J Neural Transm 51:271–282

    Google Scholar 

  • Raisman R, Briley M, Langer SZ (1979) Specific tricyclic antidepressant binding sites in rat brain. Nature 281:148–150

    Google Scholar 

  • Schlicker E, Göthert M, Hillenbrand K (1985) Cyanopindolol is a highly potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Naunyn-Schmiedeberg's Arch Pharmacol 331:398–401

    Google Scholar 

  • Sulser F, Vetulani J, Mobley PL (1978) Mode of action of antidepressant drugs. Biochem Pharmacol 27:257–261

    Google Scholar 

  • Tabakoff B, Lee JM, De Lean-Jones F, Hoffman PL (1985) Ethanol inhibits the activity of the B form of monoamine oxidase in human platelet and brain tissue. Psychopharmacology 87: 152–156

    Google Scholar 

  • Verge D, Daval G, Patey A, Gozlan HM, El-Mestikawy S, Hamon M (1985) Presynaptic 5HT autoreceptors on serotonergic cell bodies and/or dendrites but not terminals are of the 5HT1A subtype. Eur J Pharmacol 113:463–464

    Google Scholar 

  • Zsilla G, Barbaccia ML, Gandolfi O, Knoll J, Costa E (1983) (−)-Deprenyl, a selective MAO “B” inhibitor increases [3H]-imipramine binding and decreases β-adrenergic receptor function. Eur J Pharmacol 89:111–117

    Google Scholar 

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Galzin, AM., Langer, S.Z. Potentiation by deprenyl of the autoreceptor-mediated inhibition of [3H]-5-hydroxytryptamine release by 5-methoxytryptamine. Naunyn-Schmiedeberg's Arch. Pharmacol. 333, 330–333 (1986). https://doi.org/10.1007/BF00512949

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