The effects of pargyline and 2-phenylethylamine on D1-like dopamine receptor binding.

J Neural Transm (Vienna)

Department of Chemistry, Brandon University, Brandon, MB, R7A 6A9, Canada.

Published: July 2011


Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

2-Phenylethylamine (PE) potentiates neuronal responses to dopamine by an unknown post-synaptic mechanism. Here, whether PE modifies D1-like receptor binding was examined. An unexpected effect of the monoamine oxidase inhibitor pargyline was observed, which did not involve competition for ligand binding. PE did not affect ligand binding in the presence or absence of pargyline. It is concluded that the effect of pargyline does not involve elevation of endogenous PE, and PE effects on dopaminergic neurotransmission are not due to altered D1-like receptor binding.

Download full-text PDF

Source
http://dx.doi.org/10.1007/s00702-010-0561-xDOI Listing

Publication Analysis

Top Keywords

receptor binding
12
d1-like receptor
8
ligand binding
8
binding
5
effects pargyline
4
pargyline 2-phenylethylamine
4
2-phenylethylamine d1-like
4
d1-like dopamine
4
dopamine receptor
4
binding 2-phenylethylamine
4

Similar Publications

Splenic erythrophagocytosis is regulated by ALX/FPR2 signaling.

Haematologica

September 2025

Center for Cardiometabolic Science, Christina Lee Brown Envirome Institute, Division of Environmental Medicine, Department of Medicine, University of Louisville, Louisville, Kentucky,.

Maintaining a healthy pool of circulating red blood cells (RBCs) is essential for adequate perfusion, as even minor changes in the population can impair oxygen delivery, resulting in serious health complications including tissue ischemia and organ dysfunction. This responsibility largely falls to specialized macrophages in the spleen, known as red pulp macrophages, which efficiently take up and recycle damaged RBCs. However, questions remain regarding how these macrophages are acutely activated to accommodate increased demand.

View Article and Find Full Text PDF

The estrogen receptor (ER or ERα) remains the primary therapeutic target for luminal breast cancer, with current treatments centered on competitive antagonists, receptor down-regulators, and aromatase inhibitors. Despite these options, resistance frequently emerges, highlighting the need for alternative targeting strategies. We discovered a novel mechanism of ER inhibition that targets the previously unexplored interface between the DNA-binding domain (DBD) and ligand-binding domain (LBD) of the receptor.

View Article and Find Full Text PDF

Abnormal immune responses are common clinical features in septic patients. γδ T cells, as innate immune cells, play an important role in host defense, immune surveillance and homeostasis. However, the immune characteristics of γδ T cells in pediatric sepsis remains remain poorly understood.

View Article and Find Full Text PDF

The ryanodine receptors (RyRs) represent an optimal target for insecticide development. To explore novel structures of RyRs agonists, a series of compounds containing 1,2,4-oxadiazole were designed and synthesized based on the RyRs structure. The compounds were confirmed by H and C nuclear magnetic resonance as well as high-resolution mass spectrometry.

View Article and Find Full Text PDF

In this review, the primary aim is to examine non-azole ring systems that have analgesic activity and, where applicable, to establish structure - activity relationships (SARs) with the nine major pathways, prostaglandin synthesis inhibition, opioid receptor modulation, sodium channel blockade, enhancement of serotonin and norepinephrine levels, cannabinoid receptor (CBR) binding, N-methyl-D-aspartate (NMDA) receptor antagonism, transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonism, and P2X purinergic receptor blockade, have been described for pain relief. Analgesic effects have been observed in compounds containing ring systems such as piperidine, piperazine, pyridine, pyridazine, pyrazine, morpholine, thiomorpholine, pyran, thiopyran, indane, benzofuran, benzothiophene, quinoline, quinazoline, and chromene. These ring systems were classified in the whole study, first according to their molecular weights and then by bioisosteric similarity as same as first part.

View Article and Find Full Text PDF