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At least 19 recordsLinked to original sources
PubMed1977

Interaction of perphenazine and an ergoline derivative on oestrogen-induced adenohypophyseal growth.

Male and female rats were injected twice a week for three weeks with doses of 1 mg oestradiol benzoate (OE), were given perphenazine (P, 2 mg/rat/day) or the ergoline derivative D-6-methyl-8-ergoline-(I)-yl acetic acid amide (Deprenon SPOFA, D, 200 microng/rat/day) in their food or were treated with various combinations of all three factors. OE-induced adenohypophyseal growth was inhibited by D, but the inhibitory effect of D was completely suppressed by P. D also inhibited the OE-induced increase in the thyroxine-binding capacity of the adenohypophyseal proteins, but this inhibition was not suppressed by the simultaneous administration of P. The administration of OE was followed by elevation of the serum ceruloplasmin level, which was not inhibited by P or D, either alone or combined. Ovarian weight rose markedly after D and the increase was inhibited by the simultaneous administration of either OE or P.

Adrenal Glands↗
PubMed1979

Two novel prolactin release-inhibiting 8 alpha-amino-ergolines.

Prolactin secretion inhibition and changes in striatal dopamine metabolism in rats were compared after the administration of 8 alpha-amino-ergoline CH 29-717 and 2 derivates. CQ 32-084 was similar to but less potent than CH 29-717, while 32-085, the l-methyl derivative, showed delayed dopaminomimetic effects.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1979

Lisuride hydrogen maleate: an ergoline with beta-adrenergic antagonist activity.

Lisuride hydrogen maleate is identified as a potent beta-adrenergic antagonist using a hormone-sensitive adenylate cyclase system and [3H]dihydroalprenolol binding in cell free homogenates of rabbit cerebellum. Lisuride and two other ergolines, lergotrile and bromocriptine, and the phenothiazine, fluphenazine, all interact with spiroperidol binding sites (dopamine receptors) in the anterior pituitary; however, among these compounds lisuride is unique in its ability to antagonize the beta-adrenoceptor.

Adenylyl Cyclases↗
PubMed1979

Ergot alkaloids. Synthesis of nitrosourea derivatives of ergolines as potential anticancer agents.

Nitrosourea derivatives of ergolines have been synthesized for the purpose of obtaining agents with both prolactin-and tumor-inhibitory activity. Two derivatives of 8-amino-6-methylergoline (3), 8-[3-(2-chloroethyl)-3-nitrosoureido]-1-nitroso-6-methylergoline (5c) and 8-[3-2-chloroethyl)-3-nitrosoureido]-6-methylergoline (5a), have been prepared. In addition, nitroso (7) and chloroethylcarbamyl (8) derivatives of elymoclavine (6) are reported. Compounds 5a and 5c have activity against L1210 leukemia in mice but only moderate prolactin-inhibiting activity. The chloroethylcarbamyl derivative 8 of elymoclavine is a potent prolacting inhibitor.

Animals↗
PubMed1978

Ergot alkaloids. New ergolines as selective dopaminergic stimulants.

A new two-step sequence for the epimerization of methyl dihydrolysergate (5) at C-8 leading to methyl dihydroisolysergate (7) is presented. The latter compound was used as a starting material for the synthesis of various ergolines, of which (5R,8R,10R)-8-(cyanomethyl)-6-methylergoline (4) is a very strong and long-lasting central dopaminergic agent. Furthermore, it was found that some 8-(arylthiomethyl)-6-methyler-golenes are not able to induce apomorphine-like stereotyped behavior in normal rats but exhibit a remarkable activity in rats unilaterally lesioned by 6-OH-DA in the nigrostriatal region. Compound 4 and (5R,8R)-8-[(2-pyridyl)thiomethyl]-6-methylergolene (9) were further tested for their ability to inhibit ovum implantation and to depress serum prolactin levels in rats. Their potency was evaluated in comparison with (5R,8S,10R)-8-(cyanomethyl)-6-methylergolines (2a and 2b) and 2-bromo-alpha-ergocryptine (1) as standards.

Animals↗
PubMed1977

Experiences with a new ergoline (CF 25-397) in parkinsonism.

Studies on rats with unilateral nigral lesions suggest that a new ergoline, CF 25-397, is a dopaminergic agonist that might improve parkinsonism. CF 25-397 induces less stereotyped behavior than other dopaminergic agents in rats, and might therefore cause less dyskinesia than levodopa in man. We investigated the clinical actions of CF 25-397 in nine patients. During treatment, severe deterioration resulted in hypokinesia and rigidity; five patients showed marked dysphagia and dysphonia. There was statistically significant deterioration in four timed tests. Mild improvement, not statistically significant, was noted in tremor. These results indicate that clinical implication of the response to potential therapeutic agents in rodent models of parkinsonism must be interpreted with caution.

Aged↗
PubMed1976

Effect of d-6-methyl-8-ergoline-i-ylacetamide (Deprenon) on the FSH content of the pituitary in castrated female rats.

The authors studied the effect of Deprenon (D-6-methyl-8-ergoline-I-acetylamide tartrate) on the FSH content of the adenohypophysis of female rats which had been castrated 3 and 6 weeks previously. The FSH content, determined by the method of Johnson and Naqui (1970), is expressed at the mean weights of the recipients' ovaries compared with a group given only 30 I.U. HCG. Within 30 min after administration, a single peroral dose of 0.5 mg Deprenon/kg produced a drop in the pituitary FSH content. This was not very pronounced 3 weeks after castration, but was highly significant 6 weeks after castration, when the amount of FSH in the control animals' pituitaries rose.

Acetamides↗
PubMed1978

Ergoline derivatives with oral, prolonged, alpha-adrenolytic activity.

The alpha-adrenolytic activity of 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate (XV, formula II) is, both in vitro and parenterally, quite similar to that of dihydroergotamine. By oral route the new compound is more active, and longer lasting than dihydroergotamine.

Administration, Oral↗
PubMed1979

Diminution of prostate by ergoline derivative VUFB--6638 (Dironyl) in rats.

Experiments in male rats showed that the administration of prolactin secretion inhibitor-N-(D-6-methyl-8-isoergolin-I-yl)-N', N'-diethylurea -- led to a decrease of prostate weight, while a simultaneous administration of prolactin prevented this effect. The histological examination showed that the quantity of secretions in the prostate glands are decreased.

Animals↗
PubMed1975

Effect of ergoline derivative VUFB-6638 on the adenohypophysial prolactin concentration in rats.

The compound VUFB-6638 (N-/D-6-methyl-8-isoergolin-I-yl/N'-N'-diethylurea hydrogen maleinate) was administered for four consecutive days to lactating rats in daily oral doses of 0.1, 1.0 and 2.0 mg/kg. The adenohypophysial prolactin concentration decreased by 34% to 68%, respectively. Moreover, this compound reduced or even completely suppressed the lactation. In view of the assumed relations between prolactin and breast carcinoma, a potential use of the drug is noted.

Animals↗