Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Besser, G. M.; Delitala, G.; Grossman, Ashley; Stubbs, W. A.; Yeo, Tun Kuan

doi:10.1111/j.1476-5381.1980.tb10974.x

Cited by 33 publications

(13 citation statements)

References 24 publications

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“…Domperidone, a dopamine antagonist that blocks the □^-receptors stimulated by bromocriptine [2], was without significant effect on GHRH-induced GH release, although there was a tendency for the serum GH response to GHRH to be lower in the presence of the drug. This is compatible with recent data demonstrating that metoclopramide also has no effect on the GH response to GHRH [17].…”

Section: Discussionmentioning

confidence: 96%

“…An in travenous forearm cannula was inserted at 08.00 h, and two basal blood samples taken via this cannula at 08.30 and 09.00 h. Follow ing the second sample, either a tablet of bromocriptine (2.5 mg) or a placebo was given by mouth with a glass of water, and thereafter blood was sampled at 15-min intervals for serum GH over 4 h. The study was repeated on two further occasions, but with the addition of GHRH( I 29)NH:, given as a rapid 50-ug intravenous bolus at 90 min. In a separate study, the same subjects were given either domperidone, a dopamine antagonist [2], or pirenzepine. a cholin ergic antagonist [15,16], just before either an intravenous dose of GHR(I-29)NH2 or placebo.…”

Section: Methods and Subjectsmentioning

confidence: 99%

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Dopaminergic and Cholinergic Influences on the Growth Hormone Response to Growth Hormone-Releasing Hormone in Man

et al. 1987

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It is well established that compounds that modify dopaminergic and cholinergic activity in man may induce changes in circulating growth hormone (GH). We have, therefore, investigated the effect of a dopamine agonist, bromocriptine, and a dopamine antagonist, domperidone, as well as a muscarinic cholinergic antagonist, pirenzepine, on the GH response to an analogue of GH-releasing hormone (GHRH) in normal male subjects. GHRH(1–29)NH₂ induced a rise in serum GH that was augmented by bromocriptine, antagonized by pirenzepine, but was unaltered by domperidone. As this dose of GHRH(l-29) NH₂ has been shown to be maximally stimulatory to GH release, it is suggested that there are dopamine stimulatory and cholinergic inhibitory receptors to GH release independent of GHRH in man.

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Section: Discussionmentioning

confidence: 96%

Section: Methods and Subjectsmentioning

confidence: 99%

Dopaminergic and Cholinergic Influences on the Growth Hormone Response to Growth Hormone-Releasing Hormone in Man

et al. 1987

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“…This unexpected inversion of the activity might be attributed to a biphasic effect of the active factor, namely, stimulating at high concentrations and inhibiting at low concentrations. In fact a biphasic effect of dopamine and haloperidol on in vitro prolactin secretion has been reported which invert their effect at high concentration (12,13). Moreover it cannot be excluded that the stimulating factor lost its biological activity during this purification step thus disclosing the inhibitory activity of another factor.…”

Section: General Methodsmentioning

confidence: 99%

Identification, purification, and partial characterization of a factor from rabbit serum that inhibits prolactin secretion by pituitary cells cultured in vitro

et al. 1997

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SUMMARY. A biological factor that inhibited prolactin secretion by pituitary cells cultured in vitro was identified, purified, and partially characterized from normal rabbit serum. This biological factor was also found to potentiate dopamine-mediated aortic contraction using rabbit aortic strips in vitro. Following SDS-PAGE, this factor displayed an apparent Mr of 17 kDa, which is different from the Mr of most known endogenous factors having an inhibiting activity on pituitary prolactin secretion, suggesting that this may be a yet-to-be identified novel molecule.

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“…The existence of DA receptors in the anterior, intermediate and posterior lobes of the pituitary gland have been demonstrated using in vitro radio receptor assays (Brown et aL, 1976;Cole et aL, 1981;Cronin et aL, 1978;Cronin and Weiner, 1979;Creese et aL, 1977;Munemura et aL, 1980;Seeman, 1980). It is generally assumed that hyperprolactinemia induced by neuroleptic drugs is the result of blockade of dopamine receptors negatively or uncoupled (Meunier and Labrie, 1982) to an adenylate cyclase system (D-2 receptors according to Kebabian and Calne, 1979), in experimental animals and in man (Besser et aL, 1980;Rubin and Haus, 1980). While it appears clear that DA exerts important physiological functions in the pituitary gland, little is still known about the regulation of the pituitary DA receptor and its function in vivo.…”

Section: Introductionmentioning

confidence: 99%

Specificin vivo binding of3H-spiperone to individual lobes of the pituitary gland of the rat. Evidence for the labelling of dopamine receptors

Køhler

Fahlberg

1985

J. Neural Transmission

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The in vivo binding of 3H-spiperone to individual lobes of the pituitary gland was studied after intravenous injections in unanesthetized male rats. The binding was found to be saturable and reversible. The percentage of total binding of 3H-spiperone that was specific binding was highest in the intermediate (approximately equal to 75%) and lowest in the posterior (approximately equal to 35%) lobes. The regional distribution of 3H-spiperone binding 1 hour after injections was the following: intermediate greater than anterior greater than posterior. Pharmacological analysis of the in vivo 3H-spiperone binding showed that dopamine agonists (e.g. bromocriptine, N-n-propylnorapomorphine) and antagonists could prevent the in vivo binding of 3H-spiperone in all three parts of the gland. The substituted benzamide drugs remoxipride and raclopride blocked the in vivo 3H-spiperone binding in the anterior and intermediate lobes but did not reduce the 3H-spiperone binding in the posterior part, except when given in very high doses. Taken together, the present study has shown that 3H-spiperone can be used in studies of the dopamine receptors in the anterior, intermediate and posterior lobes of the pituitary gland, but the proportion of non-specific binding is higher than in the striatum. The use of in vivo 3H-spiperone binding may thus be a useful method to study the regulation and pharmacology of these receptors in situ.

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Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Cited by 33 publications

References 24 publications

Dopaminergic and Cholinergic Influences on the Growth Hormone Response to Growth Hormone-Releasing Hormone in Man

Dopaminergic and Cholinergic Influences on the Growth Hormone Response to Growth Hormone-Releasing Hormone in Man

Identification, purification, and partial characterization of a factor from rabbit serum that inhibits prolactin secretion by pituitary cells cultured in vitro

Specificin vivo binding of3H-spiperone to individual lobes of the pituitary gland of the rat. Evidence for the labelling of dopamine receptors

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