The effect of prolonged administration of antagonists on rat striatal dopamine D2 receptor binding and mRNA content was examined. Both haloperidol (2 and 4 mg/kg) and sulpiride (10 mg/kg) induced a significant rise in total D2 and D2(444) mRNA level and in Bmax. Regulation of messenger RNA accumulation is thus an important determinant of dopamine D2 receptor density.
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http://dx.doi.org/10.1016/0922-4106(91)90092-v | DOI Listing |
The kinetically-derived maximal dose (KMD) is defined as the maximum external dose at which kinetics are unchanged relative to lower doses, e.g., doses at which kinetic processes are not saturated.
View Article and Find Full Text PDFPharmacol Biochem Behav
January 2025
In vivo Electrophysiology Research Group, Department of Physiology and Neurobiology, Eötvös Loránd University, Hungary. Electronic address:
Dopaminergic system gains importance in homeostatic sleep regulation, but the role of different dopamine receptors is not well-defined. 72 h rat electrocorticogram and sleep recordings were made after single application of dopaminergic drugs in clinical use or at least underwent clinical trials. The non-selective agonist apomorphine evoked short pharmacological sleep deprivation with intense wakefulness followed by pronounced sleep rebound.
View Article and Find Full Text PDFAm J Emerg Med
January 2025
Pharmacy Department, Wesley Medical Center, 550 N Hillside St, Wichita, KS 67214, United States of America.
Introduction: Droperidol is a dopamine-2 receptor antagonist in the class of butyrophenone antipsychotics with antiemetic, sedative, analgesic, and anxiolytic properties. In the postoperative setting, droperidol provides an opioid sparing effect and decreases nausea/vomiting. Another butyrophenone antipsychotic, haloperidol, has been shown to reduce morphine milliequivalents (MME) administered when used for abdominal pain in the emergency department (ED).
View Article and Find Full Text PDFACS Chem Neurosci
January 2025
Departments of Psychiatry and Neurology, Division of Molecular Therapeutics, New York State Psychiatric Institute, Columbia University Medical Center, New York, New York 10032, United States.
Voluntary movement, motivation, and reinforcement learning depend on the activity of ventral midbrain neurons, which extend axons to release dopamine (DA) in the striatum. These neurons exhibit two patterns of action potential activity: low-frequency tonic activity that is intrinsically generated and superimposed high-frequency phasic bursts that are driven by synaptic inputs. acute striatal brain preparations are widely employed to study the regulation of evoked DA release but exhibit very different DA release kinetics than recordings.
View Article and Find Full Text PDFJ Clin Med
December 2024
Global Andrology Forum, Moreland Hills, OH 44022, USA.
Hormonal factors play an essential role as an underlying causative factor of oligoasthenoteratozoospermia (OAT), and these patients can benefit from hormonal medications that modulate the hypothalamic-pituitary-gonadal axis. This review aims to outline the various medications used as hormonal therapy in treating infertile men with OAT. This manuscript focuses on essential hormonal evaluation, identifying men who would benefit from treatment, selecting the appropriate medication, determining the duration of therapy, and evaluating hormonal treatment outcomes.
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