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Elzasonan
Elzasonan (CP-448,187) is a selective 5-HT1B and 5-HT1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy. By preferentially blocking 5-HT1B and 5-HT1D autoreceptors, elzasonan is thought to enhance serotonergic innervations originating from the raphe nucleus, thereby improving signaling to limbic regions like the hippocampus and prefrontal cortex and ultimately resulting in antidepressant effects. See also * GR-127,935 * SB-649,915 SB-649,915 is a serotonin reuptake inhibitor and 5-HT1A receptor, 5-HT1A and 5-HT1B receptor, 5-HT1B receptor receptor antagonist, antagonist which is being investigated for its antidepressant effects. Relative to the selective serotonin reuptake ... References {{Serotonergics Abandoned drugs 5-HT1 antagonists 4-Methylpiperazin-1-yl compounds Thiomorpholines Lactams Chloroarenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SB-649,915
SB-649,915 is a serotonin reuptake inhibitor and 5-HT1A receptor, 5-HT1A and 5-HT1B receptor, 5-HT1B receptor receptor antagonist, antagonist which is being investigated for its antidepressant effects. Relative to the selective serotonin reuptake inhibitors (SSRIs), SB-649,915 has a faster onset of action and may also have greater clinical efficacy as well. This can be attributed to blockade of 5-HT1A and 5-HT1B autoreceptors which inhibit serotonin release. See also * Elzasonan * LY-367,265 References {{Serotonin receptor modulators 5-HT1 antagonists Benzoxazines Piperidines Quinolines Selective serotonin reuptake inhibitors Lactams Phenol ethers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1B Receptor
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the ''HTR1B'' gene. The 5-HT1B receptor is a 5-HT receptor subtype. Tissue distribution and function 5-HT1B receptors are widely distributed throughout the central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a terminal receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synapt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GR-127,935
GR-127935 is a drug which acts as a selective antagonist at the serotonin receptors 5-HT1B and 5-HT1D. It has little effect when given by itself but blocks the antiaggressive effect of 5-HT1B agonists, and alters release of serotonin in the brain, as well as reducing drug-seeking behaviour in cocaine addicted rats. See also * Elzasonan Elzasonan (CP-448,187) is a selective 5-HT1B and 5-HT1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy. By preferentially blocking 5-HT1B and 5-HT1D ... References 5-HT1 antagonists 4-Methylpiperazin-1-yl compounds Phenol ethers Benzanilides Oxadiazoles {{nervous-system-drug-stub ... [...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] |
5-HT1 Antagonists
The 5-HT1 receptors are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin (also known as 5-hydroxytryptamine, or 5-HT). The 5-HT1 subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. Receptors of the 5-HT1 type, specifically, the 5-HT1A and 5-HT1D receptor subtypes, are present on the cell bodies. Receptors of the 5-HT1 type, specifically, the 5-HT1B and 5-HT1D receptor subtypes, are also present on the nerve terminals. These receptors are broadly distributed throughout the brain and are recognized to play a significant part in regulating synaptic levels of 5-HT. The receptor subfamily is coupled to Gi/Go and mediate inhibitory neurotransmission Neurotransmission (Latin: ''transmissio'' "passage, crossing" from ''transmittere'' "send, let through") is the process by which signaling molecules called neurotran ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prefrontal Cortex
In mammalian brain anatomy, the prefrontal cortex (PFC) covers the front part of the frontal lobe of the cerebral cortex. It is the association cortex in the frontal lobe. The PFC contains the Brodmann areas BA8, BA9, BA10, BA11, BA12, BA13, BA14, BA24, BA25, BA32, BA44, BA45, BA46, and BA47. This brain region is involved in a wide range of higher-order cognitive functions, including speech formation (Broca's area), gaze ( frontal eye fields), working memory ( dorsolateral prefrontal cortex), and risk processing (e.g. ventromedial prefrontal cortex). The basic activity of this brain region is considered to be orchestration of thoughts and actions in accordance with internal goals. Many authors have indicated an integral link between a person's will to live, personality, and the functions of the prefrontal cortex. This brain region has been implicated in executive functions, such as planning, decision making, working memory, personality expression, moderating ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hippocampus
The hippocampus (: hippocampi; via Latin from Ancient Greek, Greek , 'seahorse'), also hippocampus proper, is a major component of the brain of humans and many other vertebrates. In the human brain the hippocampus, the dentate gyrus, and the subiculum are components of the hippocampal formation located in the limbic system. The hippocampus plays important roles in the Memory consolidation, consolidation of information from short-term memory to long-term memory, and in spatial memory that enables Navigation#Navigation in spatial cognition, navigation. In humans, and other primates the hippocampus is located in the archicortex, one of the three regions of allocortex, in each cerebral hemisphere, hemisphere with direct neural projections to, and reciprocal indirect projections from the neocortex. The hippocampus, as the medial pallium, is a structure found in all vertebrates. In Alzheimer's disease (and other forms of dementia), the hippocampus is one of the first regions of th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Limbic System
The limbic system, also known as the paleomammalian cortex, is a set of brain structures located on both sides of the thalamus, immediately beneath the medial temporal lobe of the cerebrum primarily in the forebrain.Schacter, Daniel L. 2012. ''Psychology''.sec. 3.20 Its various components support a variety of functions including emotion, behavior, long-term memory, and olfaction. The limbic system is involved in lower order emotional processing of input from sensory systems and consists of the amygdala, mammillary bodies, stria medullaris, central gray and dorsal and ventral nuclei of Gudden. This processed information is often relayed to a collection of structures from the telencephalon, diencephalon, and mesencephalon, including the prefrontal cortex, cingulate gyrus, limbic thalamus, hippocampus including the parahippocampal gyrus and subiculum, nucleus accumbens (limbic striatum), anterior hypothalamus, ventral tegmental area, midbrain raphe nuclei, habenular commi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
