In vivo interaction of cabergoline with rat brain dopamine receptors labelled with [3H]N-n-propylnorapomorphine

Benedetti, Μ. Strolin; Dostert, P.; Barone, Domenico; Efthymiopoulos, Constantin; Peretti, G.; Roncucci, R.

doi:10.1016/0014-2999(90)90367-f

Cited by 53 publications

(10 citation statements)

References 21 publications

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“…However, in hyperprolactinemia, in which cabergoline is used at much lower doses (.25 to 3.5 mg/week) (51,55), six recent cross-sectional studies of patients treated for several years with the drug (45–79 months) found an association between moderate valvular regurgitation only at the highest cumulative doses of cabergoline (54,56,57). We found that systemic administration of a low dose of cabergoline (.25–.5 mg/kg) (21,58) was sufficient to significantly reduce ethanol-consumption and -seeking in rodents. Furthermore, a pilot study conducted on cocaine addicts reported that cabergoline significantly reduced cocaine use, as evaluated by analysis of cocaine metabolite levels in urine samples and self-report of substance use, with a weekly dose of only .5 mg (59).…”

Section: Discussionmentioning

confidence: 96%

Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor

Carnicella

Ahmadiantehrani

et al. 2009

Biological Psychiatry

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Section: Discussionmentioning

confidence: 96%

Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor

Carnicella

Ahmadiantehrani

et al. 2009

Biological Psychiatry

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“…These findings suggest that CG has a higher affinity for the D2 receptor of pituitary cells as compared to BC. A previous study has shown that the affinity of CG for dopamine receptors is about twice that of BC in rat striatal tissue [31].…”

Section: Analysis Of De Novo Synthesis Of Prlmentioning

confidence: 91%

Effect of Cabergoline, a Dopamine Agonist, on Estrogen-Induced Rat Pituitary Tumors: In Vitro Culture Studies.

et al. 1995

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Abstract.Cabergoline (CG) is a dopamine agonist that inhibits secretion of prolactin (PRL) and growth hormone.The purpose of this study was to investigate the PRL-lowering effect and antitumor effect of cc on estradiol-induced rat pituitary tumors in vitro and to elucidate these mechanisms. We compared the effects of CG with those of bromocriptine (BC) in terms of the inhibition of hormone secretion as well as antitumor effects on rat pituitary tumors. Primary cultures of dissociated pituitary tumor cells were used in these studies.A significant inhibition of prolactin (PRL) secretion was observed for both drugs within 12 h after treatment, and the inhibitory effects of CG and BC were antagonized by sulpiride or haloperidol.Inhibitory effect on PRL secretion after 12-h BC or CG pretreatment was more pronounced with CG than BC treatment at all time points. PRL secretion in group pretreated with CG was significantly suppressed at 72 h when compared to that of vehicle. Inhibition of de novo PRL synthesis was better demonstrated in the CG group. These findings suggest that CG has a higher affinity for the D2 receptor of pituitary cells as compared to BC and may preferentially inhibit PRL secretion rather than PRL production.An antitumor effect of CG has been confirmed at a lower dosage than that of BC.

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“…Seven (12%) of the patients previously found to be resistant to bromocriptine were completely resistant to cabergoline (Ͻ50% decrease in PRL levels). It is not known for certain why cabergoline can be effective in patients resistant to bromocriptine, but possible explanations include the higher affinity of cabergoline for dopamine binding sites, its greater occupancy of the receptor, and slower elimination from the pituitary (324). Two large, prospective European randomized studies compared bromocriptine to cabergoline with respect to drug efficacy, thus allowing a comparison of the prevalence of resistance to each drug within the same study.…”

Section: Resistance To Prolactin-lowering Effectsmentioning

confidence: 96%

Advances in the Treatment of Prolactinomas

et al. 2006

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Prolactinomas account for approximately 40% of all pituitary adenomas and are an important cause of hypogonadism and infertility. The ultimate goal of therapy for prolactinomas is restoration or achievement of eugonadism through the normalization of hyperprolactinemia and control of tumor mass. Medical therapy with dopamine agonists is highly effective in the majority of cases and represents the mainstay of therapy. Recent data indicating successful withdrawal of these agents in a subset of patients challenge the previously held concept that medical therapy is a lifelong requirement. Complicated situations, such as those encountered in resistance to dopamine agonists, pregnancy, and giant or malignant prolactinomas, may require multimodal therapy involving surgery, radiotherapy, or both. Progress in elucidating the mechanisms underlying the pathogenesis of prolactinomas may enable future development of novel molecular therapies for treatment-resistant cases. This review provides a critical analysis of the efficacy and safety of the various modes of therapy available for the treatment of patients with prolactinomas with an emphasis on challenging situations, a discussion of the data regarding withdrawal of medical therapy, and a foreshadowing of novel approaches to therapy that may become available in the future.

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In vivo interaction of cabergoline with rat brain dopamine receptors labelled with [3H]N-n-propylnorapomorphine

Cited by 53 publications

References 21 publications

Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor

Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor

Effect of Cabergoline, a Dopamine Agonist, on Estrogen-Induced Rat Pituitary Tumors: In Vitro Culture Studies.

Advances in the Treatment of Prolactinomas

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