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Tampramine
Tampramine (AHR-9,377) is a tricyclic antidepressant (TCA) which was developed in the 1980s but was never marketed. Despite being a TCA, it acts as a selective norepinephrine reuptake inhibitor and has negligible affinity for adrenergic, histaminergic, and muscarinic receptors. It was found to be effective in the forced swim test (FST) model of depression in animal studies but is not known to have ever been trialed in humans. See also * Tricyclic antidepressant Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade. They are named after their chemical structure, which contains ... References {{Tricyclics Abandoned drugs Dimethylamino compounds Pyridobenzodiazepines Tricyclic antidepressants ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tricyclic Antidepressant
Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade. They are named after their chemical structure, which contains three rings of atoms. Tetracyclic antidepressants (TeCAs), which contain four rings of atoms, are a closely related group of antidepressant compounds. Although TCAs are sometimes prescribed for depressive disorders, they have been largely replaced in clinical use in most parts of the world by newer antidepressants such as selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs) and norepinephrine reuptake inhibitors (NRIs). Adverse effects have been found to be of a similar level between TCAs and SSRIs. Medical uses The TCAs are used primarily in the clinical treatment of mood disorders such as major depressive disorder (MDD), dysthymia, and treatment-resistant variants. They are also ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine Reuptake Inhibitor
A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore can increase adrenergic neurotransmission. Medical use NRIs are commonly used in the treatment of conditions like ADHD and narcolepsy due to their psychostimulant effects and in obesity due to their appetite suppressant effects. They are also frequently used as antidepressants for the treatment of major depressive disorder, anxiety and panic disorder. Additionally, many addictive substances such as cocaine and methylphenidate possess NRI activity, though NRIs without combined dopamine reuptake inhibitor (DRI) properties are not significantly rew ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adrenergic
Adrenergic means "working on adrenaline (epinephrine) or noradrenaline (norepinephrine)" (or on their receptors). When not further qualified, it is usually used in the sense of enhancing or mimicking the effects of epinephrine and norepinephrine in the body. * Adrenergic nervous system, a part of the autonomic nervous system that uses epinephrine or norepinephrine as its neurotransmitter Regarding proteins: * Adrenergic receptor, a receptor type for epinephrine and norepinephrine; subtypes include α1, α2, β1, β2, and β3 receptors * Adrenergic transporter (norepinephrine transporter), a protein transporting norepinephrine from the synaptic cleft into nerve cells Regarding pharmaceutical drugs: * Adrenergic receptor agonist, a type of drug activating one or more subtypes of adrenergic receptors ** This includes drugs regulating blood pressure and antiasthmatic drugs. * Adrenergic receptor antagonist, a type of drug blocking one or more subtypes of adrenergic receptor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Histaminergic
Histaminergic means "working on the histamine system", and histaminic means "related to histamine". A histaminergic agent (or drug) is a chemical which functions to directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine antagonists include H1 receptor antagonists, H2 receptor antagonists, and H3 receptor antagonists. See also * Adenosinergic * Adrenergic * Cannabinoidergic * Cholinergic * Dopaminergic * GABAergic * Glycinergic * Melatonergic A melatonergic agent (or drug) is a chemical which functions to directly modulate the melatonin system in the body or brain. Examples include melatonin receptor agonists and melatonin receptor antagonists. See also * Adenosinergic * Adrenergic ... * Monoaminergic * Opioidergic * Serotonergic References Neurochemistry Neurotransmitters {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic
A muscarinic acetylcholine receptor agonist, also simply known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation. Clinical significance M1 M1-type muscarinic acetylcholine receptors play a role in cognitive processing. In Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. As these receptors themselves appear relatively unchanged in the disease process, they have become a potential therapeutic target when trying to improve cognitive function in patients with AD. A number of muscarinic agonists have been developed and are under investigation to treat AD. These agents show promise as they are neurotrophic, decrease amyloid depositions, and improve damage due to oxidative stress. Tau-phosphorylation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and Signal_transduction, transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrophysiology, electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptor, GABA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand (biochemistry), ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G prote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biochemical Pharmacology (journal)
''Biochemical Pharmacology'' is a peer-reviewed medical journal published by Elsevier. It covers research on the pharmacodynamics and pharmacokinetics of drugs and non-therapeutic xenobiotics. The editor-in-chief is Jacques Piette, University of Liege. , accessed on February 11th, 2013 Abstracting and indexing The journal is abstracted and indexed in: According to the '''', the journal received a 2019impact factor
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Forced Swim Test
''Forced'' is a single-player and co-op action role-playing game developed by BetaDwarf, released in October 2013 for Windows, OS X and Linux through the Steam platform as well as Wii U. It is about gladiators fighting for their freedom in a fantasy arena where they are assisted by a spirit-like character called Balfus. Gameplay consists of selecting a weapon class and abilities to combat the various enemies of each arena, while solving puzzles using the help of Balfus. BetaDwarf was formed by a small group of students in 2011, who began developing the game in an unused classroom in Aalborg University – Copenhagen, Denmark. They were removed months later and launched a successful Kickstarter campaign involving an Imgur picture which documented their progress. ''Forced'' received moderate to favorable reviews with most critics praising its competitive gameplay and puzzle-system. The game's weak plot, technical glitches and excess difficulty were the negative highlights. It won th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Major Depression
Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Introduced by a group of US clinicians in the mid-1970s, the term was adopted by the American Psychiatric Association for this symptom cluster under mood disorders in the 1980 version of the ''Diagnostic and Statistical Manual of Mental Disorders'' (DSM-III), and has become widely used since. The disorder causes the second-most years lived with disability, after lower back pain. The diagnosis of major depressive disorder is based on the person's reported experiences, behavior reported by family or friends, and a mental status examination. There is no laboratory test for the disorder, but testing may be done to rule out physical conditions that can cause similar symptoms. The most common time of onset is in a person's 20s, with females affec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tricyclic Antidepressant
Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade. They are named after their chemical structure, which contains three rings of atoms. Tetracyclic antidepressants (TeCAs), which contain four rings of atoms, are a closely related group of antidepressant compounds. Although TCAs are sometimes prescribed for depressive disorders, they have been largely replaced in clinical use in most parts of the world by newer antidepressants such as selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs) and norepinephrine reuptake inhibitors (NRIs). Adverse effects have been found to be of a similar level between TCAs and SSRIs. Medical uses The TCAs are used primarily in the clinical treatment of mood disorders such as major depressive disorder (MDD), dysthymia, and treatment-resistant variants. They are also ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
