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WAY-100135
WAY-100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potency (pharmacology), potent 5-HT1A receptor, 5-HT1A receptor receptor antagonist, antagonist, and was originally believed to be highly binding selectivity, selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D, 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B, 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter. However, WAY-100635 turned out to be non-selective as well, having been shown to act additionally as a potent D4 receptor, D4 receptor agonist later on. See also * WAY-100635 References 5-HT1A antagonists Carboxamides N-(2-methoxyphenyl)piperazines Tert-butyl comp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WAY-100635
WAY-100635 is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. It is sometimes referred to as a silent antagonist at the former receptor. It is closely related to WAY-100135. In light of its only recently discovered dopaminergic activity, conclusions drawn from studies that employed WAY-100635 as a selective 5-HT1A antagonist may need to be re-evaluated. Human PET studies In human PET studies WAY-100635 shows high binding in the cerebral cortex, hippocampus, raphe nucleus and amygdaloid nucleus, while lower in thalamus and basal ganglia. One study described a single case with relatively high binding in the cerebellum. In relating its binding to subject variables one Swedish study found WAY-100635 binding in raphe brain region correlating with self-transcendence and spiritual accep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonergic
Serotonergic () or serotoninergic () means "pertaining to or affecting serotonin". Serotonin is a neurotransmitter. A synapse is serotonergic if it uses serotonin as its neurotransmitter. A serotonergic neuron ''produces'' serotonin. A substance is serotonergic if it produces its effects via interactions with the serotonin system, such as by stimulating or blocking neurotransmission. A serotonergic or serotoninergic agent is any chemical that modifies the effects of serotonin in the body. Some different types of serotonergics drugs include the following: * Serotonin receptor agonists and antagonists * Serotonin reuptake inhibitors * Serotonin releasing agent A serotonin releasing agent (SRA) is a type of drug that induces the release of serotonin into the neuronal synaptic cleft. A selective serotonin releasing agent (SSRA) is an SRA with less significant or no efficacy in producing neurotransmitter e ...s See also References Parasympathetic nervous system Neurochemistr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1B
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 postsynaptic 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 synap ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-(2-methoxyphenyl)piperazines
Chemistry * ''n-'', a lowercase prefix in chemistry denoting the straight-chain form of an open-chain compound in contrast to its branched isomer * ''N-'', an uppercase prefix in chemistry denoting that the substituent is bonded to the nitrogen, as in amines Mathematics, science and technology The italicized letter ''n'' is used in mathematics to denote an arbitrary number (usually a non-negative integer). * n-ary associativity, ''n''-ary associativity * n-ary code, ''n''-ary code * n-ary group, ''n''-ary group * n-back, ''n''-back * n-body problem, ''n''-body problem * n-category, ''n''-category * n-category number, ''n''-category number * n-connected space, ''n''-connected space * n-curve, ''n''-curve * n-dimensional space, ''n''-dimensional space * n-dimensional sequential move puzzle, ''n''-dimensional sequential move puzzle * n-electron valence state perturbation theory, ''n''-electron valence state perturbation theory (NEVPT) * n-entity, ''n''-entity * n-flake, ''n''-flake ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Antagonists
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarisation and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A receptor ago ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
D4 Receptor
The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5. The structure of DRD4 was recently reported in complex with the antipsychotic drug nemonapride. As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many neurological and psychiatric conditions including schizophrenia and bipolar disorder, ADHD, addictive behaviors, Parkinson's disease, and eating disorders such as anorexia nervosa. A weak association has been drawn between DRD4 and borderline personality disorder. It is also a target for drugs which treat schizophrenia and Parkinson's disease. The D4 receptor is considered to be D2-like in which the activated receptor inhibits the enzyme adenylate cyclase, thereby reducing the intracellular concentration of the second messenger cyclic AMP. Genetics The human protein is coded by the ''DRD4'' on chromosome 11 located in 11p15. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
British Journal Of Pharmacology
The ''British Journal of Pharmacology'' is a biweekly peer-reviewed medical journal covering all aspects of experimental pharmacology. It is published for the British Pharmacological Society by Wiley-Blackwell. It was established in 1946 as the ''British Journal of Pharmacology and Chemotherapy''. The journal obtained its current title in 1968. The current editor-in-chief is Amrita Ahluwalia. Previous editors-in-chief include Ian McGrath, Humphrey Rang, Alan North, Phil Moore, Bill Large, and Tony Birmingham. A sister journal, also published for the British Pharmacological Society by Wiley-Blackwell is the '' British Journal of Clinical Pharmacology''. The journal publishes research papers, review articles, commentaries and correspondence in all fields of pharmacology. It also publishes themed issues, as well as supplements. ''The Concise Guide to PHARMACOLOGY'' The ''Concise Guide to PHARMACOLOGY'' is a supplement of the ''British Journal of Pharmacology'', replacing the "Guide ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist , competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of ligands acti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
