The Inhibitory Effect of an Ergoline Derivative (Lergotrile, Compound 83636) on Prolactin Secretion in Man

Lemberger, Louis; Crabtree, Ross E.; Clemens, James A.; Dyke, Richard W.; Woodburn, Robert

doi:10.1210/jcem-39-3-579

Cited by 36 publications

(6 citation statements)

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“…reversed the GBL-induced increase in DA concentrations in the striatum, nucleus accumbens and olfactory . Lergotrile has been shown to lower basal serum prolactin concentrations with a similar time course to that ofbromocriptine (Lemberger et al, 1974;Clemens et al, 1975;Thorner et al, 1978). The effect of lergotrile on the rate of DA synthesis in terminals of the nigrostriatal and mesolimbic DA systems in saline-and GBL-treated rats is presented in Fig.…”

Section: Resultsmentioning

confidence: 81%

Differential action of bromocriptine on nigrostriatal versus mesolimbic dopaminergic neurons

Barton

Moore

Demarest

1987

J. Neural Transmission

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The present study was undertaken to compare the abilities of the dopaminergic agonists apomorphine, bromocriptine, and lergotrile to inhibit the synthesis of dopamine (DA) in terminals of nigrostriatal and mesolimbic DA neurons. The in vivo synthesis of DA was estimated by measuring the rate of accumulation of dihydroxyphenylalanine (DOPA) in terminals of nigrostriatal (striatum) and mesolimbic (nucleus accumbens, olfactory tubercle) neurons 30 min after the administration of NSD 1015, a decarboxylase inhibitor. The activation of DA autoreceptors in these regions was evaluated by measuring the abilities of the DA agonists to inhibit DA synthesis in brain regions of rats pretreated with gamma-butyrolactone (GBL). Apomorphine (0.03-1.0 mg/kg for 45 min) and bromocriptine (0.1-10 mg/kg for 90 min) produced dose-dependent decreases in the rate of DA synthesis in all three brain regions of both vehicle- and GBL-treated rats. A time course of the effects of the highest dose of bromocriptine (10 mg/kg), however, demonstrated dramatic regional differences in the ability of this drug to inhibit DA synthesis in saline-versus GBL-pretreated rats. Bromocriptine inhibited the GBL-induced increase in DA synthesis for 6 hours in all regions examined. In the striatum of saline-treated rats the decrease in DA synthesis was evident only at 1.5 hours after bromocriptine administration, while in the nucleus accumbens and olfactory tubercle DA synthesis remained inhibited for 6 hours. By contrast, lergotrile reduced DA synthesis to a similar extent in all three regions for at least 6 hours in both vehicle- and GBL-treated rats. These results suggest that there is no regional difference in the ability of bromocriptine to inhibit DA synthesis via DA autoreceptor mechanisms, but there appear to be differences in postsynaptic DA receptor-mediated mechanisms which regulate nigrostriatal versus mesolimbic DA neurons.

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Section: Resultsmentioning

confidence: 81%

Differential action of bromocriptine on nigrostriatal versus mesolimbic dopaminergic neurons

Barton

Moore

Demarest

1987

J. Neural Transmission

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“…Food acts as a stimulant to prolactin secretion (Quigley et al, 1981;Carlson et al, 1983) (Thomer et al, 1978;Perryman etal., 1981) or perphenazine (Lemberger et al, 1974(Lemberger et al, , 1980. This study was not designed to assess the duration of action of SK&F 101468 on prolactin release.…”

Section: Discussionmentioning

confidence: 99%

A dose rising study of the safety and effects on serum prolactin of SK&F 101468, a novel dopamine D2‐receptor agonist.

Acton¹,

Broom²

1989

Brit J Clinical Pharma

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1. SK&F 101468, a non phenolic indolone derivative, has been characterised preclinically as a novel, potent and specific dopamine D2‐ receptor agonist. 2. Its tolerability and effects on serum prolactin were investigated in 14 healthy male volunteers in a study of the first administration of SK&F 101468 to man. 3. Doses between 80 micrograms and 2.5 mg caused statistically significant (P less than 0.05) lowering of basal and food stimulated serum prolactin, relative to placebo, over a 6 h post treatment period. 4. SK&F 101468 was well tolerated up to 1 mg with symptoms of nausea and postural hypotension at higher doses.

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“…Chemically they derive from the ergoline nucleus of the ergot alkaloids and many are 9,10-dihydro compounds, because the reduc tion of this double bond reduces or eliminates the vasoconstrictive properties of the alkaloids (57). Figure 6 (upper part) shows the 6-methylergoline nucleus, from which 6-methyl-8-substituted derivatives (6-methyl-8-(3-carboxamide, 6-methyl-8-formamide and 6-methyl-8-methyl ergolines) have been obtained (59) and (lower part), the structure of three ergolines which are currently undergoing experimental and clinical trials for treatment of PRL-and GH-dependent disorders (59)(60)(61). Table V shows that inether- …”

Section: Endocrine Effects O F Ergoline Derivativesmentioning

confidence: 99%

Pituitary Hormones and Ergot Alkaloids

Müller¹,

Panerai²,

Gil-Ad³

et al. 1978

Pharmacology

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From the data presented it appears that ergot drugs are both a useful tool for use in the study of neuroendocrine control of pituitary hormone secretion and a valid pharmacologic weapon for treatment of hyperprolactinemic states, GH and, probably, ACTH and MSH hypersecretion. In fact, they are capable of a long-lasting disruption of PRL secretion from a normal or turn oral pituitary gland, are unable to affect directly the somatotrophs of an intact AP, but inhibit GH and, possibly, ACTH secretion from a hyperplastic or tumoral gland. Ergolines also exert clear-cut PRL-lowering effects and are capable of suppressing GH secretion in acromegaly. The intimate mechanism(s) and hence site(s) of action of some of these compounds await clarification.

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The Inhibitory Effect of an Ergoline Derivative (Lergotrile, Compound 83636) on Prolactin Secretion in Man

Cited by 36 publications

References 0 publications

Differential action of bromocriptine on nigrostriatal versus mesolimbic dopaminergic neurons

Differential action of bromocriptine on nigrostriatal versus mesolimbic dopaminergic neurons

A dose rising study of the safety and effects on serum prolactin of SK&F 101468, a novel dopamine D2‐receptor agonist.

Pituitary Hormones and Ergot Alkaloids

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