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PubMed1977

Metergoline as a selective 5-hydroxytryptamine antagonist in the cerebral cortex.

In rats anaesthetized with a mixture of methoxyflurane, nitrous oxide, and oxygen, the depressant actions on the cerebral cortical neurones of iotophoretically applied 5-hydroxytryptamine (5-HT) but not of noradrenaline, histamine, AMP Ca2+, and gamma-aminobutyric acid were antagonized by metergoline. These observations indicate that metergoline may be a selective 5-HT antagonist in the cerebral cortex.

Action Potentials↗
PubMed2002

Effects of metergoline on symptoms in women with premenstrual dysphoric disorder.

OBJECTIVE: The authors investigated the role of acute serotonergic modulation in the efficacy of selective serotonin reuptake inhibitors (SSRIs) in women with premenstrual dysphoric disorder. METHOD: Patients with premenstrual dysphoric disorder (whose symptoms had remitted during treatment with fluoxetine) and a group of unmedicated healthy comparison women received the serotonin receptor antagonist metergoline as part of a double-blind, placebo-controlled crossover study. RESULTS: The patients with premenstrual dysphoric disorder experienced a return of symptoms 24 hours after treatment with metergoline but not diphenhydramine (active placebo). The comparison women experienced no changes in mood. CONCLUSIONS: These data support the role of altered serotonergic transmission in the efficacy of SSRI treatment for premenstrual dysphoric disorder.

Adult↗
PubMed1976

Growth hormone and prolactin release in acromegalic patients following metergoline administration.

In six acromegalite patients oral administration of 4 mg of metergoline, an antiserotonin agent, produced a fall in plasma growth hormone (GH) and prolactin (PRL) concentrations. In the same patients this inhibitory effect was observed after administration of dopaminergic drugs, L-Dopa and 2-Br-alpha-ergocryptine. Both GH and PRL levels remained suppressed during a 6 day course of treatmnt with metergoline. These results are consistent with the hypothesis that the inhibitory effect of netergoline on GH and PRL release is determined by inactivation of serotonin receptors in the hypothalamus or at the pituitary.

Acromegaly↗
PubMed1977

Action of metergoline in suppressing prolactin release induced by mechanical breast emptying.

Ten women were studied during the first post-partum week. Mechanical breast emptying with a breast pump for 30 min induced a marked increase in plasma prolactin (PRL) reaching a maximum 30 min after the beginning of stimulation. In all patients oral administration of the antiserotonin agent metergoline, 8 mg daily for two days, completely blocked any PRL secretion induced by breast stimulation. These results confirm the inhibitory effect of metergoline on PRL release.

Adult↗
PubMed1978

Suppression of puerperal lactation by metergoline.

Based on the known stimulatory effect of serotonin on prolactin secretion, a trial of suppression of puerperal lactation by a potent serotonin antagonist, metergoline, was carried out in 30 puerperal women who did not want to nurse. The drug was administered orally at the dose of 4 mg tid for 5 days to all subjects, starting between 24 and 72 hours from delivery. Lactation was either prevented or rapidly suppressed in all subjects. Rebound of lactation after the end of treatment was observed in 10% of cases. Metergoline administration was associated with a significant suppression of the plasma prolactin levels.

Depression, Chemical↗
PubMed1981

Impaired insulin secretion in human diabetes mellitus III. The effect of the serotonin antagonist metergoline.

The present study was aimed at investigating the effect of metergoline, a powerful and long-lasting antiserotoninergic agent, on insulin responses to glucose and arginine in adult-onset diabetic subjects. The repeated administration of this agent (10 mg daily for two days plus a 4 mg dose 1 hour before the post-treatment test) or placebo did not influence acute insulin response to intravenous glucose (20 g), total insulin secretion or glucose disappearance rates. Similarly, plasma glucose and insulin levels following arginine (30 g perfused over a period of 40 min) were similar before and after metergoline treatment. These results do not support the hypothesis that an endogenous monoamine mechanism plays an important part in defective insulin secretion in human non insulin-dependent diabetes mellitus.

Adult↗
PubMed1984

Methysergide and metergoline reduce morphine analgesia with no effect on the development of tolerance in rats.

A single subcutaneous injection of 5 mg/kg metergoline or 10 mg/kg methysergide, two serotonin antagonists, or 1 mg/kg naloxone, significantly reduced the effect of a subcutaneous dose of 3 mg/kg morphine in the tail immersion test in rats. The same drugs and doses were administered concurrently with 10 mg/kg morphine twice daily for 3 days and nociceptive responses were measured 96 h later. Tolerance to the effect of 3 mg/kg morphine was comparable in animals which had received vehicle + morphine or serotonin antagonists + morphine, whereas naloxone completely prevented the development of tolerance. The results argue against a role of serotonin in the development of tolerance to the antinociceptive effect of morphine and suggest it may be possible to dissociate morphine analgesia from tolerance development, at least in the conditions used in the present study.

Analgesia↗
PubMed1985

Effect of metergoline on human anxiety.

In order to assess the role played by serotonin (5-HT) in subjective anxiety, three groups of 12 healthy volunteers were given 12 mg metergoline (MET), 10 mg diazepam (DZ) or placebo (PB), under double-blind conditions, and submitted to a simulated public speaking (SPS) test. MET increased state-anxiety scores, measured by Spielberg's State-Trait Anxiety Inventory. The effect of MET was significantly different from both the PB and DZ groups immediately before the SPS test (prestress) as well as 24 h after medication, and from the DZ group only, 2.5 h after the test (poststress). In contrast, DZ did not significantly affect subjective anxiety. The SPS test significantly increased anxiety in DZ- or PB-treated subjects as compared to prestress scores, whereas the increases in the MET group were not significant, probably because pretest levels were already high. No drug effect on heart rate, skin electrical conductance and quality of sleep during the night following medication was found. In addition, the drugs did not cause bodily symptoms that could secondarily affect mood. Since MET is a 5-HT receptor antagonist, active on the central nervous system, an inhibitory role of 5-HT on subjective anxiety might be suggested.

Adult↗
PubMed1990

Metergoline abolishes the prolactin response to buspirone.

Pretreatment of nine healthy subjects with the non-selective 5-HT receptor antagonist, metergoline (4 mg), abolished the increase in plasma prolactin produced by the anxiolytic drug, buspirone (15 mg). While these findings are consistent with a role for 5-HT receptors in the stimulatory effect of buspirone on plasma prolactin, a dopaminergic mechanism cannot be excluded by the present data.

Adult↗
PubMed1988

Metergoline, naloxone, and sodium valproate did not modify arginine vasopressin response to insulin-induced hypoglycemia in man.

The present study was carried out in order to determine whether insulin-induced hypoglycemia exerts its stimulatory effect on plasma concentrations of arginine vasopressin (AVP) by interacting with a serotonergic, a GABA-ergic or an opioid pathway. For this purpose, the effect of the serotonergic antagonist metergoline (10 mg/day for 4 days po), the GABA-ergic agonist sodium valproate (600 mg in three divided doses po) and the opioid-receptor blocker naloxone (10 mg in a iv bolus) on the AVP response during an insulin (0.15 IU/kg bw) tolerance test (ITT) was evaluated in three groups of 6 normal men each. In all men, control ITTs were performed without drug treatments. Basal and ITT-stimulated AVP secretion was not modified by drug administration, suggesting that serotonergic, GABAergic and naloxone-sensitive opioid receptors are not involved in the regulation of AVP secretion in response to insulin-induced hypoglycemia.

Adrenocorticotropic Hormone↗
PubMed1993

Effects of serotonin and the serotonin blocker metergoline on meal patterns and macronutrient selection.

Serotonin [5-hydroxytryptamine(5-HT)] in the paraventricular nucleus (PVN) of rats has a suppressive effect on feeding behavior and causes a selective decrease in carbohydrate ingestion, specifically at the onset of the natural (dark) feeding period. Studies conducted here provide further evidence for this phenomena, showing a similar dose-related decrease in carbohydrate ingestion at dark onset after PVN injection of 5-HT or of the agonists, d-norfenfluramine or fluoxetine, which act through endogenous 5-HT. To further characterize the effects of this indoleamine on the macrostructure of feeding, a computer-automated data acquisition system was used to analyze macronutrient feeding patterns in freely feeding animals maintained on the pure diets of protein, carbohydrate, and fat. Results indicate that PVN administration of 5-HT at dark onset decreases intake of the carbohydrate nutrient by decreasing meal size, feeding time, and feeding rate for this nutrient and increasing the satiating effect of carbohydrate. These effects, which occur specifically during the first meal after injection, are opposite those seen after peripheral administration of the 5-HT receptor antagonist, metergoline. This drug stimulates feeding through a selective increase in carbohydrate intake, characterized by an increase in meal size, percent composition, and feeding time for this nutrient and a decrease in the satiety ratio for carbohydrate. These results implicate the serotonergic system in the termination of carbohydrate-rich meals that are prevalent during the early hours of the natural feeding cycle.

Animals↗
PubMed1996

Metergoline potentiates natural feeding and antagonizes the anorectic action of medical hypothalamic 5-hydroxytryptamine.

Medial hypothalamic injections of 5-hydroxytryptamine (5-HT) or its agonists have been reported to inhibit feeding elicited by norepinephrine (NE), suggesting that these two transmitter systems interact antagonistically in the control of ingestive behavior. The present study was designed to directly test the hypothesis that 5-HT inhibits adrenergic feeding, specifically at the onset of the rat's nocturnal eating cycle. Free-feeding animals were injected with 5-HT (5-20 nmol) immediately before NE (20 nmol) and food intake was measured 1.5 h postinjection. In separate groups of rats, the serotonergic antagonist metergoline (MET) (2.5-20nmol) was injected into the paraventricular nucleus (PVN) immediately before 5-HT, or before combined injections of 5-HT and NE. The feeding-stimulant action of MET alone, injected IP (0.25-2 mg/kg) or centrally (2.5-40 nmol), was also examined. Results indicated that administration of 5-HT into the PVN suppressed dark onset feeding and dose-dependently blocked NE-stimulated eating. Pretreatment with MET attenuated the inhibitory action of 5-HT on feeding, and reversed the serotonergic blockade of the adrenergic eating response. Further, systemically injected MET significantly increased dark onset feeding, whereas PVN injections failed to alter food intake reliably. These findings provide the first direct evidence that serotonergic and adrenergic systems within the PVN interact in a competitive manner to modulate the natural high rates of feeding displayed by rats during the early dark period. Although MET effectively blocked the anorectic effect of 5-HT, the feeding-stimulant action of this compound alone does not appear to be mediated within the PVN.

Animals↗
PubMed1989

Increased food intake and carbohydrate preference in the rat following treatment with the serotonin antagonist metergoline.

The effect on feeding of antagonism of the serotonergic system was studied. Intraperitoneal injection of one of 8 doses of the serotonin antagonist metergoline (MET) (0.06-1.5 mg.kg-1) given prior to a 3 h food deprivation produced a significant dose-related increase in intake of a standard laboratory diet throughout a 2 h measurement period. A 1 mg/kg dose of MET administered prior to one of 3 isocaloric powdered diets a medium carbohydrate, a high carbohydrate, and a non-carbohydrate diet - produced a significant increase in the intake by rats of all 3 diets in the first hour after food presentation. However, in the second hour MET continued to increase consumption of the high carbohydrate diet, whereas intakes of the medium carbohydrate and non-carbohydrate diets were no longer affected by MET treatment. These data suggest that the serotonergic system is a tonic inhibitor of food intake and of carbohydrate preference.

Animals↗
PubMed1982

Treatment of hyperprolactinemic states with different drugs: a study with bromocriptine, metergoline, and lisuride.

One hundred ninety-one hyperprolactinemic patients (78 women and 13 men; 54 with pituitary macroadenoma, 53 with microadenoma, and 84 with idiopathic disease) were treated for 2 to 48 months with one or two of the following prolactin (PRL)-lowering drugs: bromocriptine, metergoline, and lisuride. All of the three drugs used were highly effective in lowering PRL levels and restoring gonadal function both in females and in males in the majority of patients with either idiopathic or tumorous disease. In poorly responsive patients, increasing the drug doses resulted in further PRL lowering for all the three drugs. Mild side effects were frequently encountered with initiation of drug treatment but spontaneously subsided in most cases; severe side effects, necessitating stopping of the treatment, occurred in only 12 instances, but changing of the drug allowed PRL-lowering treatment to be continued in 11 of them.

Adenoma↗
PubMed1988

Differential effect of d-fenfluramine and metergoline on food intake in human subjects.

This study investigated the effect of the 5-HT receptor blocker metergoline (MTG) on d-fenfluramine (d-FF)-induced reduction of food intake in 13 normal male human volunteer subjects. Food was freely available for 2h, 4h after drug administration, from a four-channel automated food dispenser. d-FF (30 mg) reduced total food intake and exerted a marked effect on non-sweet food which was attenuated by the addition of MTG (4 mg). d-FF had less effect on sweet-tasting food while intake of sweet food was significantly increased by MTG. There was a significant interaction between d-FF and MTG on sweet-tasting foods. No effect on MTG was observed on d-FF-induced changes in ratings of hunger.

Adolescent↗
PubMed1978

Effects of serotonin, of its biosynthetic precursors and of the anti-serotonin agent metergoline on the release of glucagon and insulin from rat pancreas.

We have evaluated the effect of serotonin (5-HT) and of its biosynthetic precursors 5-Hydroxytryptophan (5-HTP) and tryptophan (TRP) on the release of immunoreactive glucagon (IRG) and insulin (IRI) from isolated islets and pieces of pancrease of the rat. In isolated islets, 5-HT inhibited the IRI response to a high glucose concentration (3.0 mg/ml), without affecting the IRG response to either a low (0.5 mg/ml) or a high glucose concentration; TRP stimulated the IRG and IRI response to the low glucose concentration, while 5-HTP was ineffective. When pieces of pancreas were used, 5-HT and 5-HTP inhibited IRG response to both glucose concentrations, while IRI release was inhibited only by 5-HT. The anti-5-HT agent metergoline enhanced the release of IRG and IRI by pieces of pancreas at both glucose concentrations. The results indicate that exogenous and endogenous 5-HT inhibit basal as well as glucose-mediated IRG and IRI release; that isolated islets are less sensitive than pieces of pancreas to the inhibitory effect of 5-HT and that TRP acts as an amino acid and not as a precursor of 5-HT.

5-Hydroxytryptophan↗
PubMed1980

Metergoline and cyproheptadine suppress prolactin release by a non-5-hydroxytryptaminergic, non-dopaminergic mechanism.

A dispersed rat anterior pituitary cell system has been used to investigate the effects of cyproheptadine and metergoline on prolactin secretion. Both drugs were potent inhibitors of prolactin secretion. However, the inhibition was not antagonized by either 5-hydroxytryptamine or a variety of dopamine antagonists. We conclude that both drugs act through mechanisms that are neither 5-hydroxytryptaminergic nor dopaminergic.

Animals↗