• Unlike many tricyclic antidepressants, medifoxamine lacks anticholinergic and alpha blocker properties (very low affinity for the muscarinic acetylcholine receptors and 10-fold lower affinity for the α1-adrenergic receptor relative to 5-HT2 binding sites), and is also apparently inactive as a norepinephrine reuptake inhibitor (although the same source stating this also states that it is inactive as a serotonin reuptake inhibitor, which was subsequently found not to be the case). (wikipedia.org)
  • The serotonin-1A (5-HT1A) receptor is among the most abundant and widely distributed 5-HT receptors in the brain, but is also expressed on serotonin neurons as an autoreceptor where it plays a critical role in regulating the activity of the entire serotonin system. (biomedcentral.com)
  • this is flanked by a series of upstream repressor elements for REST, Freud-1/CC2D1A and Freud-2/CC2D1B factors that not only restrict its expression to neurons, but may also regulate the level of expression of 5-HT1A receptors in various subsets of neurons, including serotonergic neurons. (biomedcentral.com)
  • Elevated 5-HT1A autoreceptor expression would tend to reduce the activity of 5-HT neurons, while reduced post-synaptic 5-HT1A receptors would result in a blunted behavioral response to 5-HT. (biomedcentral.com)
  • RESEARCH:5-HT1A (Serotonin-1A) receptor gene regulation and mental illness:Hypothesis: Down-regulation of the 5-HT1A receptor gene in serotonin neurons is required for the antidepressant actions of therapeutic compounds. (vdocuments.net)
  • regulators of the rat and human 5-HT1A receptor genes using luciferase reporter fusion constructs transfected in cell lines. (vdocuments.net)
  • These studies implicate the 5-HT1A receptor as an important determinant of predisposition to mental illness. (biomedcentral.com)
  • This review examines the evidence that alterations in transcriptional regulation of the 5-HT1A receptor could underlie its dys-regulation in mental illness. (biomedcentral.com)
  • Understanding the proteins that regulate the 5-HT1A promoter will lead to insights on receptor regulation and provide new therapeutic targets relevant to depression, anxiety, obsessive compulsive disorder and other mental illnesses. (vdocuments.net)
  • MDMA, a potent monoamine-releaser with particularly pronounced serotonin- releasing properties, has unique subjective effects that include: marked positive mood, pleasant/unusual bodily sensations and pro-social, empathic feelings. (researchgate.net)
  • Pet1, an obligatory enhancer for serotonergic differentiation, has been identified as a potent activator of 5-HT1A autoreceptor expression. (biomedcentral.com)
  • Taken together, these results highlight an integrated regulation of 5-HT1A autoreceptors that differs in several aspects from regulation of post-synaptic 5-HT1A receptors, and could be selectively targeted to enhance serotonergic neurotransmission. (biomedcentral.com)
  • Over-expression of the 5-HT1A autoreceptor has been implicated in reducing serotonergic neurotransmission, and is associated with major depression and suicide. (biomedcentral.com)
  • 5-MT acts as a full agonist at the 5-HT 1 , 5-HT 2 , 5-HT 4 , 5-HT 6 , and 5-HT 7 receptors. (cloudfront.net)
  • Unlike many tricyclic antidepressants, medifoxamine lacks anticholinergic and alpha blocker properties (very low affinity for the muscarinic acetylcholine receptors and 10-fold lower affinity for the α1-adrenergic receptor relative to 5-HT2 binding sites), and is also apparently inactive as a norepinephrine reuptake inhibitor (although the same source stating this also states that it is inactive as a serotonin reuptake inhibitor, which was subsequently found not to be the case). (wikipedia.org)
  • The catalog of these molecules includes low molecular weight transmitters such as monoamines, acetylcholine, glutamate, gama-aminobutiric acid (GABA), adenosine-5-triphosphate (ATP), and a list of peptides including substance P, brain-derived neurotrophic factor (BDNF), and oxytocin. (frontiersin.org)
  • neurons and the detection of these transmitters in the extracellular fluid in concentrations capable of activating their receptors suggest that the "classical" low molecular weight neurotransmitters previously thought to act exclusively on synapses, also participate in extrasynaptic communication. (frontiersin.org)
  • 5-Methoxytryptamine ( 5-MT ), also known as mexamine , is a tryptamine derivative closely related to the neurotransmitters serotonin and melatonin . (cloudfront.net)
  • The discovery of extrasynaptic receptors by Miledi (1960) , was followed by observations by Dun and Minota (1982) of peripheral neuronal responses that could be attributed to somatic exocytosis of signaling molecules upon electrical stimulation. (frontiersin.org)
  • Co-director of proposal to evaluate PET imaging of the peripheral benzodiazepine receptor as a cellular marker of inflammation in Alzheimer's disease and atherosclerosis. (nih.gov)
  • This article will review neuroactive steroid effects on serotonin and GABA systems, along with the subsequent effects on cognitive functions. (researchgate.net)
  • Estrogen and progesterone have their respective hormone receptors, whereas allopregnanolone acts via the GABA(A) receptor. (researchgate.net)
  • The action of estrogen and progesterone can be direct genomic, indirect genomic, or non-genomic, also influencing several neurotransmitter systems, such as the serotonin and GABA systems. (researchgate.net)
  • In adults, an activation of the GABA-A receptor leads to an inward flow of chloride ions. (researchgate.net)
  • Positive GABA-A receptor modulating stress and sex steroids (steroid-PAMs) such as allopreg-nanolone (ALLO) and medroxyprogesterone acetate can provoke impaired cognition. (researchgate.net)
  • 5-MT has been shown to occur naturally in the body in low levels. (cloudfront.net)
  • Estrogen alone, or in combination with progesterone, affects the brain serotonin system differently in different parts of the brain, which can at least partly explain the opposite effects on mood of those hormones. (researchgate.net)