STRUCTURE OF MELATONIN<sup>1</sup>

Lerner, Aaron B.; Case, James D.; Heinzelman, R. V.

doi:10.1021/ja01531a060

Cited by 435 publications

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“…This bioassay was used to isolate melatonin from pineal extracts, which led to the elucidation of its chemical structure (Lerner et al, 1959). The action of melatonin to aggregate pigment granules (melanosomes) of amphibian dermal melanophores was used to 1) postulate the presence of melatonin receptors (Heward and Hadley, 1975); 2) establish the first structure-activity relationships of melatonin analogs (Heward and Hadley, 1975); and 3) demonstrate that melatonin receptors are coupled to a pertussis toxin-sensitive G-protein (White et al, 1987).…”

Section: B Melatonin Receptor Discovery: Historical Backgroundmentioning

confidence: 99%

“…The field of mammalian melatonin receptors got off to a slow start; the first pharmacological characterization of a functional mammalian melatonin receptor (Dubocovich, 1983) and the cloning of the first human melatonin receptor came 25 and 36 years, respectively, after melatonin itself was discovered (Lerner et al, 1959). Now, however, the field is moving quickly, and there are sufficient data upon which to organize and classify the known mammalian melatonin receptors.…”

Section: Introductionmentioning

confidence: 99%

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International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

et al. 2010

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Section: B Melatonin Receptor Discovery: Historical Backgroundmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

et al. 2010

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“…To confirm that this was not an important factor in the present study, the effect of lysis upon the activation of exogenous PKA added to the lysis medium was Melatonin and PKA in pars tuberalis 0.6 7 0.5-0. 4 investigated. The AR of exogenous PKA added to unstimulated cells at lysis was not significantly different from basal levels observed for the endogenous enzyme in the same cell preparations (Fig.…”

mentioning

confidence: 99%

Melatonin Inhibits the Activation of Cyclic AMP‐Dependent Protein Kinase in Cultured Pars Tuberalis Cells from Ovine Pituitary

Hazlerigg

Morgan²,

Lawson³

et al. 1991

J Neuroendocrinology

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The effect of melatonin upon the activation of the intracellular effector enzyme, cyclic AMP (CAMP)-dependent protein kinase (PKA), was investigated in primary cultures of ovine pars tuberalis cells. Incubation of these cells with forskolin caused a rapid and dose-dependent activation of PKA (ED, 10-6M). When cells were incubated with forskolin and melatonin simultaneously, the activation of PKA by forskolin was dramatically inhibited. This inhibitory effect of melatonin was dose-dependent (EDa 10-"M).Furthermore, treatment with melatonin rapidly deactivated PKA in cells prestimulated with forskolin. When pars tuberalis cell extracts were incubated with 8N,-[32P]cAMP, an analogue of cAMP used for photoaffinity labelling of native PKA, specific binding was observed in three bands with M, of 54, 52 and 48 kd. representing the regulatory subunits of PKA II (in phosphorylated and dephosphorylated forms) and PKA I, respectively. These results indicate that melatonin is a potent inhibitory regulator of CAMPmediated signal transduction in the ovine pars tuberalis, and suggest that the cellular effects of melatonin in this tissue a r e mediated by the dephosphorylation of specific substrate proteins.

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“…There is the possibility that other acidic and basic compounds are present in the brain. 5-Methoxyindol-3-ylacetic acid has been isolated from the pineal gland by Lerner, Case, Biemann, Heinzelman, Szmuszkovicz, Anthony & Krivis (1959), and other 5-OR indolyl derivatives such as N-acetyl-5-methoxytryptamine have also been isolated (Lerner, Case & Heinzelman, 1959). Because the methods used here would not distinguish all of these compounds it was found preferable to describe the substances by the general term of 5-OR indolyl compounds.…”

Section: Discussionmentioning

confidence: 99%

Drug‐induced Changes in the Concentration of 5‐or Indolyl Compounds in Cerebrospinal Fluid and Caudate Nucleus

Ashcroft

Sharman

1962

British Journal of Pharmacology and Chemotherapy

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The effects of reserpine and imipramine on the concentration of indolyl compounds bearing an OR group in position 5 (5-OR indolyl compounds) in the cerebrospinal fluid and the caudate nucleus of the dog have been studied. Reserpine was shown to produce an increase in the concentration of these compounds in the cerebrospinal fluid. In the caudate nucleus reserpine produced a fall in the concentration of the basic 5-OR indolyl compounds accompanied by an equivalent increase in the concentration of acidic 5-OR indolyl compounds. No significant change in the concentration of 5-OR indolyl compounds in the cerebrospinal fluid was observed after treatment with imipramine.In a previous publication (Ashcroft & Sharman, 1960) it was reported that there was a difference in the concentration of 5-hydroxyindolyl compounds in the cerebrospinal fluid of patients suffering from depressive psychoses and patients with neurological diseases. The present investigation on dogs was carried out to test the possibility that changes in the metabolism of 5-hydroxytryptamine in the body might be reflected in changes in the cerebrospinal fluid level of indolyl compounds bearing an OR group in position 5. Sharman (1960) has shown that many indolyl compounds bearing an OR group in position 5, where R is a hydrogen atom, or an aryl or alkyl group, and unsubstituted in the 2 position of the indole nucleus, show the fluorescence in 3N hydrochloric acid attributed to 5-hydroxyindolyl compounds by Udenfriend, Bogdanski & Weissbach (1955) and demonstrated for N-acetyl-5-methoxytryptamine by Axelrod & Weissbach (1961). It is possible that traces of indolyl compounds bearing an OR group in position 5 other than 5-hydroxytryptamine or 5-hydroxyindol-3-ylacetic acid are present in the cerebrospinal fluid.

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STRUCTURE OF MELATONIN¹

Cited by 435 publications

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International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

Melatonin Inhibits the Activation of Cyclic AMP‐Dependent Protein Kinase in Cultured Pars Tuberalis Cells from Ovine Pituitary

Drug‐induced Changes in the Concentration of 5‐or Indolyl Compounds in Cerebrospinal Fluid and Caudate Nucleus

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STRUCTURE OF MELATONIN1

Cited by 435 publications

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International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

Melatonin Inhibits the Activation of Cyclic AMP‐Dependent Protein Kinase in Cultured Pars Tuberalis Cells from Ovine Pituitary

Drug‐induced Changes in the Concentration of 5‐or Indolyl Compounds in Cerebrospinal Fluid and Caudate Nucleus

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STRUCTURE OF MELATONIN¹