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At least 163 records · Page 9Linked to original sources
PubMed1999

Ergocryptine and other ergot alkaloids stimulate the release of [3H]dopamine from rat striatal synaptosomes.

Ergocryptine is an ergot alkaloid that affects dopaminergic activity principally by interacting with D2-type receptors. In this study the ability of ergocryptine and several other ergot alkaloids to release [3H]dopamine from isolated nerve endings was demonstrated using in vitro superfusion of rat striatal synaptosomes. Ergocryptine, ergocristine, and bromocryptine produced an elevation in baseline dopamine release of approximately 400% with effective concentrations (EC50) of approximately 30 microM. Ergotamine, ergonovine, ergovaline, and ergocornine were devoid of activity. The time-course of the ergocryptine-stimulated release was relatively slow compared with amphetamine, nicotine, or K+-stimulated [3H]dopamine release; the maximal increase in release required a 5-min treatment. A number of receptor antagonists were examined for their ability to block ergocryptine-stimulated release. Of the dopaminergic, adrenergic, serotonergic, GABA-ergic, and cholinergic antagonists examined, only phentolamine produced a moderate attenuation in evoked release. Omission of Ca++ from the medium did not affect ergocryptine-evoked release. Following ergocryptine treatment, the synaptosomes were fully responsive to other stimulant. The results indicate that, in addition to interacting with dopamine receptors, several ergot alkaloids may produce dopaminergic effects by increasing the release of dopamine from central nerve endings. Several mechanisms to account for the evoked neurotransmitter release are discussed.

Animals↗
PubMed1979

Hepatocellular injury with distinctive mitochondrial changes induced by lergotrile mesylate: a dopaminergic ergot derivative.

Increased serum activities of the enzymes alanine aminotransferase (ALT) and aspartate aminotransferase (AST) occurred in 12 out of 19 patients with idiopathic parkinsonism when they were treated with the ergot derivative lergotrile at an oral dose varying from 50 to 150 mg daily. Hepatocellular injury was confirmed by microscopic examination of liver biopsies obtained from 3 of these patients when the serum activities of ALT and AST were appreciably elevated. Light microscopy revealed features of mild acute hepatocellular injury, and electron microscopy showed proliferation of the smooth endoplasmic reticulum and apparently unique mitochondrial changes in hepatocytes. This is the first report of pathological changes in the liver associated with the therapeutic use of an ergot derivative. The presence of a potentially reactive cyanide group in the lergotrile molecule could be causally related to the observed hepatocellular injury. It is suggested that serum ALT and AST activities should be monitored carefully when the therapeutic potential of any new ergot derivative is assessed.

Adolescent↗
PubMed1983

Influence of ergot derivatives on prolactin secretion in rats. Mechanisms of action and clinical implications.

Ergot derivatives are the most effective compounds in the treatment of migraine attacks. It has been proposed that these compounds exert this effect by direct action on skull arteries or arteriovenous anastomoses, or by interfering with peripheral or central serotonin receptors. It is also possible that these compounds influence monoaminergic neurotransmission and, thereby, endorphins modulating the threshold for pain or sensory perception. In testing these hypotheses, changes in receptor sensitivity or function have to be considered since we have observed simultaneous tolerance and supersensitivity development in the same animal treated chronically with lisuride. We therefore propose that ergot derivatives can reduce the well documented higher sensitivity of migraine sufferers to various stimuli. In humans, prolactin-levels can be used for determining bioavailability of some ergot derivatives and for studying whether dopaminergic mechanism plays a role in their antimigraine effect.

Animals↗
PubMed1997

Ergotism and photosensitization in swine produced by the combined ingestion of Claviceps purpurea sclerotia and Ammi majus seeds.

Poisoning of domestic animals happens frequently in the southeast of Buenos Aires Province (Argentina). Intoxications are produced mainly by the ingestion of plants and mycotoxins, but animals are rarely affected simultaneously by both types of agents. One herd of pigs suffered simultaneous intoxications by ergot alkaloids from Claviceps purpurea sclerotia and furocoumarins from Ammi majus seeds. Pigs were fed a diet composed of wheat (poor quality) or corn and protein and vitamin supplements. This diet was completed with forage sorghum. Nervous signs were first observed 5-7 days after the initiation of feeding the suspect ration. These signs were followed by cutaneous irritation. Snout ulcers, eyelid edema, and conjunctivitis were observed in several piglets. Ten days after the start of feeding the incriminated ration, 8 abortions were observed. Many of the sows that were nursing piglets developed udder edema and teat cracking. Dermal lesions were observed in most of the animals with unpigmented areas in the skin but not in a Duroc-Jersey boar. Removal of the incriminated diet and feeding of another diet prepared with good-quality wheat allowed all the animals to recover in 15 days. The herd experienced normal pregnancies and parturitions, litter sizes, and piglet weights when fed a cleaned portion of the poor-quality wheat. No photosensitization lesions were observed. Examination of impurities in the suspected wheat indicated the presence of 2.2% of A. majus seeds and 0.14% of C. purpurea sclerotia. The quantitative analysis indicated the presence of 3.2 g xanthotoxin and 0.65 g bergaptene/100 g A. majus seeds and 0.73 g ergot alkaloids (expressed as ergonovine) per 100 g of C. purpurea sclerotia. Qualitative analysis demonstrated the presence of ergotamine, ergocristine, and ergonovine. These results indicate that clinical signs and lesions were caused by the ingestion of large quantities of these biologically active compounds.

Animal Feed↗
PubMed2005

Presumptive gangrenous ergotism in free-living moose and a roe deer.

Presumptive gangrenous ergotism in 10 moose (Alces alces) and one roe deer (Capreolus capreolus) is reported. Three of the moose came from a municipality in southeastern Norway where the disease occurred as a cluster in 1996. The other moose represented solitary or sporadic cases diagnosed in four municipalities in northwestern Norway between 1996 and 2004. Affected moose (seven calves, three yearlings) were found between October and June, showing distal limb lesions on one to three limbs. The lesions in the moose found during October and November presented as dry gangrene, whereas moose found between December and June presented with loss of the distal part of the limbs or open lesions close to sloughing. Four of the moose also had bilateral ear lesions affecting the outer third of the pinnae. A retrospective diagnosis of ergotism (June 1981) was made in a 1-yr-old roe deer from northwestern Norway showing loss of the distal part of all four limbs.

Animals↗
PubMed1981

Inhibition of neurotransmitter receptor binding by ergot derivatives.

Bromocriptine, lergotrile, lisuride, metergoline, and the Sandoz ergot derivatives 25-397, 29-712, and 29-717 have been tested for their ability to inhibit the synaptic receptor binding of spiroperidol, 5-hydroxytryptamine (5-HT), d-lysergic acid diethylamide (LSD), quinuclidinyl benzilate (QNB), WB.4101, and gamma-aminobutyric acid (GABA). Only GABA binding was not affected, and QNB binding was decreased only by lergotrile and metergoline at high concentrations. The most potent inhibitors of the other ligands were bromocriptine and lisuride for spiroperidol (1-2 nMM), metergoline for 5-HT (29 nM), lisuride for LSD (15 nM), and lergotrile for WB.4101 (17 nM). The direct receptor effects of the ergot derivatives in vitro may contribute to understanding their in vivo effects on behavior and in predicting their therapeutic potential in neurological and neuroendocrine disorders.

Adrenergic alpha-Antagonists↗
PubMed2006

Ergot alkaloids in cereal products: results from the Bavarian Health and Food Safety Authority.

The danger of ergot alkaloids has been well known for centuries. The origin and toxicology of these compounds have been clarified and flour mills assure us that they have mastered the problem technologically. Nevertheless, one can find food products with sometimes relatively high contents of these toxic alkaloids. Here we report on our experiences and results of an LC-MS/MS-method which we have developed to determine ergot alkaloids and which was applied to commercial products during the past two years.

Bread↗
PubMed1995

Teratogen update: ergot and ergotamine.

Ergotamine is a purified ergot alkaloid that has been suspected of being teratogenic. Animal data have shown effects mainly at doses toxic to the mother. Clinical reports in humans have been anecdotal, but in many the malformations are consistent with vascular injury. However, epidemiologic studies have not shown any clear increase in malformations among exposed infants. This may reflect the limited exposure and toxicity when used episodically. Ergot toxicity which can result in severe vasospasm does not spare the fetus or mother and ergotamine should not be considered without risk. Ergotamine should be avoided in pregnancy, and the counselling of the woman with an exposed fetus should focus on possible toxic exposure.

Abnormalities, Drug-Induced↗
PubMed1978

Blockade of photically induced epilepsy by 'dopamine agonist' ergot alkaloids.

The effect of the intravenous administration of ergot alkaloids on epileptic responses to intermittent photic stimulation )IPS) has been studied in adolescent baboons, Papio papio, from Senegal. Ergocornine, 1--2 mg/kg, produced marked autonomic and behavioural effects, slowed the EEG, and abolished myoclonic responses to IPS for 30--90 min. Ergometrine, 1 mg/kg, activated the EEG and blocked the induction of myoclonic responses for 1--3 h. Bromocriptine, 0.5--4 mg/kg, did not consistently prevent myoclonic responses to IPS. After pretreatment with a subconvulsant dose of allylglycine (180--200 mg/kg), lysergic acid diethylamide, 0.1 mg/kg, retained the capacity to block myoclonic responses to IPS, and ergocornine 1 mg/kg reduced such responses. The convulsant effect of allylglycine was enhanced, however, so that prolonged seizure sequences began 19--96 min after ergocornine administration. The protective action of ergot alkaloids against epileptic responses induced by sensory stimulation is interpreted in terms of effects at several sites, including dopaminergic and serotoninergic synapses.

Allyl Compounds↗
PubMed1979

Treatment of Schizophrenia with ergot derivatives.

Seven neuroleptic-free schizophrenic patients received bromocriptine and eight schizophrenic patients received CF 25-397, both ergot derivatives with dopamine agonist activity. Psychosis failed to improve in response to either drug at the relatively low doses administered. Unlike the antipsychotic property of apomorphine at low dose levels, neither of these ergot drugs improved schizophrenic symptomatology.

Adult↗
PubMed1979

Ergotism in a patient with a portosystemic shunt.

A case of ergotism is described in a patient with Banti's syndrome in whom a porto-systemic shunt had been made three times. She was admitted to hospital with severe ischaemia of the extremities after having taken a single oral dose of 1 mg ergotamine tartrate. Her condition improved rapidly after 2 to 3 days and the circulation was normal after one week. The possible mechanism of ergotism in this patient is discussed. Although the plasma concentration of ergotamine was not measured, the likeliest explanation was that the serious side effects were related to the altered pharmacokinetics and loss of first-pass metabolism of the drug due to the venous bypass of the liver.

Adult↗
PubMed1988

[A method for the determination of ergot alkaloids in food].

A suitable method has been developed for the routine analysis of the ergot alkaloids ergometrine, ergometrinine, ergosine, ergosinine, ergotamine, ergotaminine, ergocornine, ergocorninine, alpha-ergocryptine, alpha-ergocryptinine, beta-ergocryptine, beta-ergocryptinine, ergocristine and ergocristinine in cereal products. The method consists of food extraction, cleaning of the crude extract by a modified form of the Extrelut method, and identification and quantitative determination of the alkaloids by high pressure liquid chromatography (HPLC). The results are confirmed by thin layer chromatography (TLC) and gas-chromatography/mass spectrometry (GC/MS). Market investigations have shown contaminations in ecological as well as in conventional products, with rye products mainly being contaminated. Within the EEC, a maximum value of 0.05% ergot respectively a total alkaloid content of 1 mg/kg in cereals used for food production is prescribed. This value was not exceeded in any of the investigated samples.

Chromatography, High Pressure Liquid↗
PubMed1991

Physiological controls and regulation of ergot alkaloid formation.

Innovation and technical development of ergot alkaloids (EA) has moved closer to scientific research. Circumstantial evidence presently links the initiation of EA metabolism to changes in a range of parameters--morphology, concentrations of enzymes and their substrates, nutrients and external stress. The biosynthesis of EA begins at the level of the genetic information apparatus and continues at the level of physiological expression. EA and their formation play a role in the physiology of the production organism. Insufficient insight into Claviceps physiology hampers the deployment of computers in the control and regulation of the EA process. Knowledge of physiological controls and genetic manipulation are the principal tools of modern EA production. In principle it is now possible to improve EA yields by a concerted breeding of the ergot fungus by sexual and parasexual genetic engineering.

Biotechnology↗
PubMed2005

Norleucine, a natural occurrence in a novel ergot alkaloid gamma-ergokryptinine.

A novel natural peptide ergot alkaloid gamma-ergokryptinine containing norleucine has been isolated from ergot sclerotia of the field-growing parasitic fungus Claviceps purpurea CCM 8059. Its structure was deduced from the NMR and mass spectral data. The final structural proof was provided by the crystal structure determination, which is the first X-ray structure of a natural Nle-containing secondary metabolite. The conformations of three ergopeptinines: gamma-ergokryptinine, ergoladinine, and alpha-ergokryptinine were compared.

Claviceps↗
PubMed1980

Anorectic effect of lisuride and other ergot derivatives in the rat.

Three ergot derivatives, lisuride, lergotrile and bromocriptine, given to rats trained to eat 4 h a day, induced a dose- and time-related anorexia. They were more potent in this context than either amphetamine or fenfluramine. Lisuride and lergotrile failed to increase locomotor activity or to induce stereotyped behaviour at doses corresponding to the ID50 on food intake. At this dose, bromocriptine slightly stimulated motor activity. The anorectic effect of the three compounds was selectively antagonized by blockers of dopamine (DA) receptors in the central nervous system but not by either inhibiton of catecholamine synthesis or blockade of alpha- or beta-adrenoceptors or of serotonergic receptors. Also two blockers of 'peripheral' DA receptors failed to antagonize ergoline-induced anorexia. These findings indicate that stimulation of DA receptors involved in feeding behaviour was responsible for the anorexigenic effect of the ergot derivatives investigated. In most instances this effect occurred at dose levels which failed to induce central stimulant effects.

Animals↗
PubMed1982

Dopaminergic and serotonergic mediation of the discriminable effects of ergot alkaloids.

The involvement of dopamine (DA) and serotonin (5-HT) neuronal systems in the discriminative stimulus effects of various ergot derivatives was assessed by administering four ergots to 36 rats which had been trained to discriminate either apomorphine (APO) or d-lysergic acid diethylamide (LSD) from saline. Lergotrile, lisuride and LSD substituted for APO (0.25 mg/kg) while bromocriptine and ergonovine (ergometrine) did not; only lisuride mimicked LSD (0.08 mg/kg). Antagonism tests showed that the DA antagonist haloperidol but not the 5-HT antagonist BC-105 (pizotifen) blocked the APO cue; both the LSD cue and the substitution of LSD for APO were blocked by BC-105 but not by haloperidol. It was concluded that DA receptor activation plays a prominent role in the discriminative stimulus effects of lergotrile and lisuride as well as APO and a secondary role in the LSD cue; 5-HT seems to be of major importance in the mediation of the effects of LSD and, to a lesser extent, lisuride. The functions of the two monoamines in the discriminable effects of bromocriptine and, particularly, ergonovine are less clear.

Animals↗
PubMed1986

Selectivity of some ergot derivatives for 5-HT1 and 5-HT2 receptors of rat cerebral cortex.

The affinities of several ergot derivatives for 5-HT1 and 5-HT2 receptors were evaluated using [3H]5-HT and [3H]mianserin, and membranes prepared from rat frontal cortex. CQ 32-084, which had a Ki value against the 5-HT2 component of [3H]mianserin binding of 9 nM, had little effect on [3H]5-HT binding and was selective for the 5-HT2 receptor. Lisuride and LY-158A also displayed preferential affinity for the 5-HT2 receptor. Dihydroergocryptine, CM 29-712, lergotrile and LY-062 were more selective for the 5-HT1 receptor. Bromocriptine showed little selectivity for either subtype. Overall, the ergot derivatives displayed markedly different affinities and selectivities for central 5-HT receptors suggesting that their serotonergic actions should be considered when evaluating their pharmacological spectrum of activity.

Animals↗
PubMed1988

The selectivity of newly synthesized ergot derivatives to alpha 1- and alpha 2-adrenoceptors, D1- and D2-dopaminergic receptors, muscarinic acetylcholinoceptors and beta-adrenoceptors.

1. We tested affinities of newly synthesized ergot derivatives to alpha 1- and alpha 2-adrenoceptors, D1- and D2-dopamine receptors, muscarinic acetylcholinoceptors and beta-adrenoceptors using radioligand binding techniques. 2. BAM-1110 was alpha 2-selective, though its affinity to alpha 2-adrenoceptors was one tenth less than that of yohimbine. 3. BAM-1303, which was non-selective, had high affinity to alpha-adrenoceptors. The pKi-values for BAM-1303 was 10.11 against both [3H]prazosin (alpha 1-ligand) and [3H]rauwolscine (alpha 2-ligand). 4. New ergot derivatives were selective to D2-dopamine receptors. BAM-1125 and BAM-1303 had high selectivity to D2-receptors. 5. They had less affinity to muscarinic receptors and beta-adrenoceptors.

Animals↗