We studied a protein phosphorylation system that is regulated by the dopamine-mimetic ergot bromocriptine. Bromocriptine was found to inhibit selectively the endogenous phosphorylation of a threonine residue(s) in 50,000- and 60,000-dalton proteins in a synaptosome fraction. The bromocriptine-sensitive phosphorylation is stimulated by calcium and by calmodulin, and occurs predominantly in the b...

A patient with a macroprolactinoma was treated with bromocriptine 15 mg daily. Both the size of the tumour as shown by computed tomography and the serum prolactin concentration decreased over several months but then increased. The dose of bromocriptine was increased to 40 mg daily but tumour growth continued, and the tumour was resected. Production of prolactin by cultured cells was not inhibit...

B romocriptine is a sympatholytic D2-dopamine agonist that has been approved for the treatment of type 2 diabetes. Based on animal and human studies, timed bromocriptine administration within 2 h of awakening is believed to augment low hypothalamic dopamine levels and inhibit excessive sympathetic tone within the central nervous system (CNS), resulting in a reduction in postmeal plasma glucose ...

We analysed the interaction between the dorsal striatum (motor coordination and planning) and the hippocampus (sensory information processing and integration) during performance of goal-directed tasks. The performance of rats that had been injected with different doses of the D(2)-antagonist Sulpiride into the dorsal striatum was tested in an egocentric 4-arm maze task that tests striatal funct...

The aim of this study was to investigate whether the concomitant administration of the substrates or inhibitors of PEPT1, OCTN1, OCTN2, and P-glycoprotein affects the intestinal absorption of sulpiride in rats. The absorption of sulpiride from rat intestine was decreased by the substrates or inhibitors of PEPT1, OCTN1, and OCTN2. On the other hand, the absorption was increased by the substrates...

Sulpiride and tiapride are often used in the treatment of depression, schizophrenia and psychopathology of senescence, gastric or duodenal ulcers and are also partly excreted by kidney. This work developed a simple and sensitive method for their simultaneous monitoring in human urine based on capillary electrophoresis coupled with electrochemiluminescence detection by end-column mode. beta-Cycl...

We investigated whether the uptake of a specific antipsychotic agent, sulpiride, in Caco-2 cells is mediated by a carrier-mediated system. Caco-2 cell monolayers were cultured in plastic culture dishes and uptake and efflux studies were conducted. The determination of sulpiride was performed by HPLC. At 37 degrees C, sulpiride uptake in pH 6.0 was twice as much as in pH 7.4. At 4 degrees C, how...

HANEW, K., SASAKI, A. and YOSHINAGA, K. Evidence for Endogenous Dopaminergic Control of OH Release in Man. Tohoku J. exp. Med., 1981, 135 (1), 103-108 In order to determine whether or not there is a tonic dopamine (DA) control of GH release, the effect of an anti-dopaminergic agent, sulpiride, on GH secretion was studied in 12 normal subjects. After the administration of sulpiride, serum concen...

PURPOSE Prolactinoma (prolactin-secreting pituitary adenoma) is one of the most common estrogen-related functional pituitary tumors. As an agonist of the dopamine D2 receptor, bromocriptine is used widely to inhibit prolactinoma progression. On the other hand, it is not always effective in clinical application. Although a dopamine D2 receptor deficiency contributes to the impaired efficiency of...

The pattern of androgen dependent enzyme activities of epididymis was studied after the administration of prolactin and bromocriptine in albino rats. Prolactin activated the glycogenolysis and hexose mono and diphosphate pathways, which would be essential for sperm maturation. But bromocriptine inhibited these activities of epididymis. Hence role of bromocriptine in decreasing epididymal functi...