Ergoline derivatives: receptor affinity and selectivity

Mantegani, Sergio; Brambilla, Enzo; Varasi, Mario

doi:10.1016/s0014-827x(99)00028-2

Cited by 48 publications

(32 citation statements)

References 15 publications

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“…Dopamine receptors belong to the family of seven transmembrane domain G protein coupled receptors and include five different receptor subtypes, named D 1 -D 5 . The members of the dopamine receptor family are encoded by genes localized at different chromosomal loci, displaying a considerable homology in their protein structure and function.…”

Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

“…The members of the dopamine receptor family are encoded by genes localized at different chromosomal loci, displaying a considerable homology in their protein structure and function. The analysis of dopamine receptor structure and function suggests the existence of two different groups of receptors: D 1 -like, including D 1 and D 5 receptors, generally associated to a stimulatory function, and D 2 -like, including D 2 -D 4 receptors, generally associated to an inhibitory function (1). The D 1 and D 5 receptors are encoded by genes lacking introns and share an 80% homology in their transmembrane domains.…”

Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

“…The D 2 receptor shares a 75% homology with the D 3 and a 53% homology with the D 4 transmembrane domains, and all three receptor subtypes are encoded by genes which are interrupted by introns (1). The NH 2 -terminal stretch has a similar number of amino acid residues in all the receptor subtypes and carries a variable number of consensus Nglycosylation sites, which can also be present in the extracellular loops: the D 1 and D 5 receptors possess two such sites, the D 2 has four, the D 3 has three, and the D 4 possesses only one potential N-glycosylation site. The carboxy terminus, which is about seven times longer for the D 1 -like than for the D 2 -like receptors, is rich in serine and threonine residues and contains a cysteine residue, probably involved in the anchorage of the cytoplasmic tail to the membrane.…”

Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

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Novel insights in dopamine receptor physiology

Pivonello¹,

Ferone

Lombardi³

et al. 2007

eur j endocrinol

126

103

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The dopaminergic system has a pivotal role in the central nervous system but also plays important roles in the periphery, mainly in the endocrine system. Dopamine exerts its functions via five different receptors, named D 1 -D 5 , belonging to the category of G protein coupled membrane receptors. Dopamine receptors are heterogeneously expressed in different cells, tissues and organs, where they stimulate or inhibit different functions, including neurotransmission and hormone synthesis and secretion. In particular, the dopamineric system has a pivotal role in the physiological regulation of the hypothalamus-pituitary-adrenal axis. Recent data have demonstrated the expression and function of dopamine receptors not only in endocrine organs but also in endocrine tumors, mainly those belonging to the hypothalamus-pituitary-adrenal axis, and also in the so-called 'neuroendocrine' tumors. These data confirm the important role of the dopaminergic system in this endocrine axis, as well as in the neuroendocrine system. This review summarizes the main structural and functional characteristics of dopamine receptors, emphasizing the most recent novelties, and focused on the physiological and pathological regulation of the hypothalamus-pituitary-adrenal axis by the dopaminergic system. In addition, the recent findings on the relationship between dopamine receptors and neuroendocrine tumors are summarized.European Journal of Endocrinology 156 S13-S21

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Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

Section: Structural Characteristics Of Dopamine Receptorsmentioning

confidence: 99%

See 1 more Smart Citation

Novel insights in dopamine receptor physiology

Pivonello¹,

Ferone

Lombardi³

et al. 2007

eur j endocrinol

126

103

View full text Add to dashboard Cite

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“…The ergot alkaloids, 21,22 derivatives of lysergic acid or ergoline structures show a broad range of pharmacological activities. Many of them are DA D 2 receptor agonists, 23,24 but some ergoline derivatives also interact with serotonin receptors [25][26][27] and adrenoceptors 28,29 with very high affinities.…”

Section: Introductionmentioning

confidence: 99%

Salvage of sildenafil failures with cabergoline: a randomized, double-blind, placebo-controlled study

Safarinejad¹

2006

Int J Impot Res

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To evaluate the safety and efficacy of cabergoline in men with erectile dysfunction (ED) who did not respond to sildenafil. Four hundred two sildenafil nonresponders aged from 21 to 59 years were included in the study. Patients were randomly divided into group 1, those who received 0.5-1 mg cabergoline weekly for 6 months and group 2, who received placebo for the same period. They underwent preliminary assessment, including medical and sexual history, self-administered International Index of Erectile Function (IIEF) and intravaginal ejaculatory latency time (IVELT) evaluation. Standard biochemistry and hematological laboratory tests, and measurement of serum testosterone and prolactin levels were also carried out. When indicated, other tests were used to establish the diagnosis of vasculogenic and neurogenic ED, including penile color duplex Doppler ultrasonography, pudendal nerve conduction test and impaired sensory-evoked potentials studies. The efficacy of two treatments was assessed every 2 weeks during treatment, at the end of the study, using responses to IIEF, IVELT evaluation, mean intercourse satisfaction domain, mean weekly coitus episodes and adverse drug effects. The trial was completed by 370 (92%) men. Positive clinical results were seen in 31.2% of patients in the cabergoline group compared with 7.1% of patients in the placebo group (P ¼ 0.04). The mean weekly intercourse episodes increased from pretreatment values of 1.4 and 1.2 to 2.2 and 1.4, for cabergoline and placebo, respectively (P ¼ 0.04). Baseline mean intercourse satisfaction domain values of IIEF 10 and 11 reached to 15 and 10 at 6-month treatment in groups 1 and 2, respectively (P ¼ 0.04). The IVELT after cabergoline and placebo gradually increased from 98 and 101 s to approximately 242 and 116 s, respectively (P ¼ 0.001). More drug-related adverse effects occurred in cabergoline group and 12 (5.9%) had to discontinue treatment (P ¼ 0.001). Cabergoline is moderately effective salvage therapy for sildenafil nonresponse. Further studies with different dosages and treatment regimens are necessary to draw final conclusions on the efficacy of this drug in ED.

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“…Overall, cabergoline is more potent when compared to bromocriptine in the binding and activation of the D 2 -like receptors. 4,5 Dopamine receptors mediate the effects of dopamine and dopaminergic drugs via a number of different signal transduction pathways. The most important of these is the modulation of adenylyl cyclase activity resulting in either stimulation or inhibition of cyclic AMP accumulation.…”

mentioning

confidence: 99%