scholarly journals Discovery, characterization, and optimization of highly selective D 2 dopaminergic antagonists

2013 ◽  
Vol 27 (S1) ◽  
Author(s):  
R. Benjamin Free ◽  
Jingbo Xiao ◽  
Trevor Doyle ◽  
Jennie Conroy ◽  
Steve Titus ◽  
...  
Keyword(s):  
Dopaminergic Antagonists

Dopaminergic suppression of pancreatic somatostatin secretion

1982 ◽  
Vol 101 (1) ◽  
pp. 56-61 ◽  
Author(s):  
Mitsuyasu Itoh ◽  
Brian L. Furman ◽  
John E. Gerich
Keyword(s):  
Pancreatic Islet ◽  
Cell Function ◽  
Potential Interaction ◽  
Beta Adrenergic ◽  
Adrenergic Antagonist ◽  
Adrenergic Mechanism ◽  
D Cell ◽  
D Cells ◽  
Dopaminergic Antagonists

Abstract. To characterize dopaminergic influences on pancreatic islet D cell function and its potential interaction with islet A and B cell function, the effect of dopamine (0.5–100 μm) on immunoreactive somatostatin (IRS), insulin (IRI), and glucagon (IRG) release from rat islets incubated in vitro was studied. Dopamine significantly suppressed the release of IRS (P< 0.001) and IRI (P < 0.001) and augmented IRG release (P < 0.001). Maximum suppression of IRS and IRI release was evident at 20 μm dopamine with half-maximal suppression occurring at 0.5–1 μm. Maximal stimulation of IRG release was observed at 100 μm dopamine with a halfmaximal response occurring at 5–10 μm. Suppression of IRS secretion by dopamine (20 μm) was completely reversed by the dopaminergic antagonists haloperidol (5 μm) and pimozide (5 μm), but was only partially reversed by the alpha adrenergic antagonist phentolamine (2 μm), and was further suppressed by the beta adrenergic antagonist propranolol (2 μm). Suppression of IRI release by dopamine was completely reversed by propranolol, but was unaffected by haloperidol, pimozide, and phentolamine. There results indicate that dopamine directly affects pancreatic islet D cell function, and that islet B and D cells appear to be more sensitive to dopamine than are A cells. Dopamine suppresses IRS secretion predominantly through activation of dopaminergic receptors, whereas it suppresses IRI release through an alpha adrenergic mechanism and stimulates IRG release through a beta adrenergic mechanism.

Dopaminergic antagonists for alcohol dependence

2010 ◽  
Author(s):  
Fabiana Benites Vaz de Lima ◽  
Régis B Andriolo ◽  
Dartiu X da Silveira
Keyword(s):  
Alcohol Dependence ◽  
Dopaminergic Antagonists

scholarly journals Dopaminergic antagonists for alcohol dependence

2018 ◽  
Author(s):  
Fabiana Benites Vaz de Lima ◽  
Regis B Andriolo ◽  
Dartiu X da Silveira
Keyword(s):  
Alcohol Dependence ◽  
Dopaminergic Antagonists

scholarly journals Inhibition of Perforant Path Input to the CA1 Region by Serotonin and Noradrenaline

2005 ◽  
Vol 94 (2) ◽  
pp. 1413-1422 ◽  
Author(s):  
Nonna A. Otmakhova ◽  
Jennifer Lewey ◽  
Brent Asrican ◽  
John E. Lisman
Keyword(s):  
Inhibitory Concentration ◽  
Significant Inhibition ◽  
Perforant Path ◽  
Excitatory Postsynaptic Potential ◽  
Complete Suppression ◽  
Maximal Inhibition ◽  
Ca1 Region ◽  
Postsynaptic Potential ◽  
Postsynaptic Action ◽  
Dopaminergic Antagonists

Bath-applied monoamines—dopamine (DA), serotonin (5-HT), and noradrenaline (NE)—strongly suppress the perforant path (PP) input to CA1 hippocampal region with very little effect on the Schaffer collaterals (SC) input. The effect of DA action on PP field excitatory postsynaptic potential (fEPSP) has been characterized in detail, but relatively little is known about the NE and 5-HT effects. Here we show that the maximal inhibition of the PP fEPSP by NE is ∼55%, whereas 5-HT inhibition is weaker (∼35%). The half-maximal inhibitory concentration of both 5-HT and NE is ∼1 μM. Neither NE nor 5-HT affected paired-pulse facilitation, suggesting that the effect is not presynaptic. This is in contrast to DA, which does have a presynaptic effect. The NE effect was blocked by α2 antagonists, whereas the α1 antagonist corynanthine and β-antagonist propranolol were ineffective. The effect of 5-HT was mimicked by the agonist, 5-carboxamidotryptamine maleate (5-CT), and not affected by adrenergic and dopaminergic antagonists. To determine the 5-HT receptors involved, we tested a number of 5-HT antagonists, but none produced a complete suppression of the 5-HT effect. Of these, only the 5-HT7 and 5-HT2 antagonists produced weak but significant inhibition of 5-HT effect. We conclude that NE inhibits the PP fEPSP through postsynaptic action on α2-adrenoceptors and that 5-HT7, 5-HT2, and some other receptor may be involved in 5-HT action in PP.

Asenapine modulates nitric oxide release and calcium movements in cardyomyoblasts

2016 ◽  
Vol 33 (S1) ◽  
pp. S553-S553
Author(s):  
P. Zeppegno ◽  
C. Gramaglia ◽  
E. Gattoni ◽  
S. Gili ◽  
E. Gambaro ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Hydrogen Peroxide ◽  
Clinical Relevance ◽  
Nitric Oxide Release ◽  
No Release ◽  
Intracellular Ca ◽  
Specific Receptors ◽  
Competing Interest ◽  
Dopaminergic Antagonists ◽  
Serotoninergic Receptors

ObjectiveTo examine the effects of asenapine on NO release and Ca2+ transients in H9C2, which were either subjected to peroxidation or not.Materials and methodsH9C2 were treated with asenapine alone or in presence of intracellular kinases blockers, serotoninergic and dopaminergic antagonists, and voltage Ca2+ channels inhibitors. Experiments were also performed in H9C2 treated with hydrogen peroxide. NO release and intracellular Ca2+ were measured through specific probes.ResultsIn H9C2, asenapine differently modulated NO release and Ca2+ movements depending on the peroxidative condition. The Ca2+ pool mobilized by asenapine mainly originated from the extracellular space and was slightly affected by thapsigargin. Moreover, the effects of asenapine were reduced or prevented by kinases blockers, dopaminergic and serotoninergic receptors inhibitors and voltage Ca2+ channels blockers.ConclusionsOn the basis of our findings we can conclude that asenapine by interacting with its specific receptors, exerts dual effects on NO release and Ca2+ homeostasis in H9C2; this would be of particular clinical relevance, when considering their role in cardiac function modulation.Disclosure of interestThe authors have not supplied their declaration of competing interest.

ChemInform Abstract: Novel (R)-2-Amino-5-fluorotetralins: Dopaminergic Antagonists and Inverse Agonists.

ChemInform ◽  
2010 ◽  
Vol 28 (7) ◽  
pp. no-no
Author(s):  
AA. MALMBERG ◽  
B. BACKLUND HOEOEK ◽  
A. M. JOHANSSON ◽  
U. HACKSELL
Keyword(s):  
Inverse Agonists ◽  
Dopaminergic Antagonists

scholarly journals Vitex agnus castus and Some Female Disorders: A Review

2021 ◽  
Author(s):  
Muna O. Alamoudi ◽  
Yousef F. Bakrshoom
Keyword(s):  
Polycystic Ovary ◽  
Potential Effect ◽  
Arab Countries ◽  
Deciduous Tree ◽  
Beneficial Effects ◽  
Natural Medicine ◽  
The People ◽  
Agnus Castus ◽  
Fat Liver ◽  
Dopaminergic Antagonists

Vitex agnus castus L., is a deciduous tree which has been utilized in ancient Greece, Iran, Egypt and Rome for over 2500 years for a large variety of female reproductive system health difficulties. In Saudi Arabia, many women have menstrual cycle disturbances and menopausal dysfunction and many have polycystic ovary syndrome at young age. Using Vitex is not in Saudi tradition like other Arab countries. Recently, just few people used this herb for treating some infertility problems. A variety of beneficial effects of this curative herb have been reported in clinical studies, including antioxidant, anti-inflammatory, hypolipidemic, anti-diabetic, hormonal modulatory, anti-nociceptive and opioidergic activities, preventing oxidative stress and nonalcoholic fat liver disease. Adverse effects of the plant are mild and reversible. The advantages of this herb as natural medicine attract the people and make it one of best choose and utilize widely in women disorders specially that related with menopauses. Its constituents could interact with dopaminergic antagonists and exhibited progesteronic and estrogenic activities. This brief review introduces this plant to Saudi society and others to expand it usage and discusses the potential effect of the plant to cure some of the women disorders displaying its main ingredients and the side effects.

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