Search results for "Monoamine neurotransmitter"
showing 9 items of 29 documents
Wasp venom injected into the prey's brain modulates thoracic identified monoaminergic neurons.
2005
The wasp Ampulex compressa injects a cocktail of neurotoxins into the brain of its cockroach prey to induce an enduring change in the execution of locomotory behaviors. Our hypothesis is that the venom injected into the brain indirectly alters the activity of monoaminergic neurons, thus changing the levels of monoamines that tune the central synapses of locomotory circuits. The purpose of the present investigation was to establish whether the venom alters the descending control, from the brain, of octopaminergic neurons in the thorax. This question was approached by recording the activity of specific identified octopaminergic neurons after removing the input from the brain or after a wasp s…
Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhe…
2010
Vascular adhesion protein-1 (VAP-1) belongs to the semicarbazide-sensitive amine oxidases (SSAOs) that convert amines into aldehydes. SSAOs are distinct from the mammalian monoamine oxidases (MAOs), but their substrate specificities are partly overlapping. VAP-1 has been proposed as a target for anti-inflammatory drug therapy because of its role in leukocyte adhesion to endothelium. Here, we describe the synthesis and in vitro activities of novel series of VAP-1 selective inhibitors. In addition, the molecular dynamics simulations performed for VAP-1 reveal that the movements of Met211, Ser496, and especially Leu469 can enlarge the ligand-binding pocket, allowing larger ligands than those s…
Studies of the Hypothalamus-Pituitary-Adrenocortical System: An Example of Progress in Psychoneuroendocrinology
1986
Psychobiological study of affective disorders has passed through several phases during the last three decades. With the discovery of thymoleptic drugs and our partial understanding of their pharmacological properties, a dominant theme in psychiatric research came to be the pathophysiology underlying depressive illness. Since enhancement of monoamine neurotransmission was found to be a common characteristic of most antidepressants, several attempts were made to test the hypothesis of a defective cerebral monoamine transmission as the prime cause of depression. In this context, neuroendocrinology became an area that was of particular interest to investigators, for several reasons. Basic resea…
Dietary l-tryptophan leaves a lasting impression on the brain and the stress response
2017
AbstractComparative models suggest that effects of dietary tryptophan (Trp) on brain serotonin (5-hydroxytryptamine; 5-HT) neurochemistry and stress responsiveness are present throughout the vertebrate lineage. Moreover, hypothalamic 5-HT seems to play a central role in control of the neuroendocrine stress axis in all vertebrates. Still, recent fish studies suggest long-term effects of dietary Trp on stress responsiveness, which are independent of hypothalamic 5-HT. Here, we investigated if dietary Trp treatment may result in long-lasting effects on stress responsiveness, including changes in plasma cortisol levels and 5-HT neurochemistry in the telencephalon and hypothalamus of Atlantic sa…
Association study of affective disorders with genetic polymorphisms of monoamine oxidases
2000
Introduction: Monoamine oxidases (MAO) catalyze the oxidative deamination of monoamines like norepinephrine, serotonin and dopamine. The existing MAOs (A and B) have distinct although partially overlapping biological functions and distributions in the brain. MAO A is mainly expressed in catecholaminergic neurons. Thirty-fold differences in enzyme activity of MAO A can be found in cultured cells from different individuals suggesting a genetic determination of enzyme activity. Indeed, a point mutation in the coding region of the gene which creates a restriction site for Fnu4HI alters the activity. Moreover, the pharmacological inhibition of monoamine oxidase A activity is one of the most effe…
Synthesis and monoamine uptake inhibition of conformationally constrained 2β-carbomethoxy-3β-phenyl tropanes
2009
A series of 2beta-carbomethoxy-3beta-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity.
Role of hydrophobicity on the monoamine receptor binding affinities of central nervous system drugs: a quantitative retention-activity relationships …
2004
Abstract Biological action and activity reflect an aspect of the fundamental physicochemical properties of the bioactive compounds. As an alternative to classical QSAR studies, in this work different quantitative retention–activity relationships (QRAR) models are proposed, which are able to describe the role of hydrophobicity on the binding affinity to different brain monoamine receptors (H 1 -histamine, α 1 -noradrenergic and 5-HT 2 -serotonergic) of different families of psychotherapeutic drugs. The retention of compounds is measured in a biopartitioning micellar chromatography (BMC) system using Brij-35 mobile phases. The adequacy of the QRAR models developed is due to the fact that both…
The Role of Monoamines in the Development of Cold-Induced Edema
1976
Our results show that even the experimentally induced high concentrations of exogenous 5-HT in the brain tissue during the early phase of edema formation are not able to increase the amount of fluid accumulation in the normal and injured brain tissue. The changes of the endogenous 5-HT levels in the blood and the brain tissue result in similar hemispheric water and RISA differences between the injured and uninjured half of the brain. Moreover, 5-HT concentrations elevated by 100% failed to produce detectable edema in the normal brain tissue of the rat.
Polymorphisms in the Serotonin (5-Hydroxytryptamine (5-HT)) Type 2A Receptor (5-HTR2A) Gene, Other Related Genes and Anthropometry
2012
Serotonin or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter, which helps to regulate many physiological processes such as sleep, appetite, eating disorders, thermoregulation, hormone secretion, mood, anxiety, etc. The serotonin and related genes, such as the 5-HT2A receptor gene (HTR2A), the 5-HT transporter gene (SLC6A4), the 5-HT2C receptor gene (HTR2C), or the 5-HT1A receptor (HTR1A) gene, are re-emerging as powerful candidates for studying the association between food intake and anthropometry. Variations in all of these genes need to be studied to better understand the effects of serotonin and its receptors on anthropometry. The most widely studied polymorphism is the −1438G…