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8-OH-DPAT
8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to be discovered. Originally believed to be selective for the 5-HT1A receptor, 8-OH-DPAT was later found to act as a 5-HT7 receptor agonist and serotonin reuptake inhibitor/releasing agent as well. In animal studies, 8-OH-DPAT has been shown to possess antidepressant, anxiolytic, serenic, anorectic, antiemetic, hypothermic, hypotensive, bradycardic, hyperventilative, and analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ... effects. See also * 5-OH-DPAT * 7-OH-DPAT * Bay R 1531 * MDAT * UH-301 References External links * Yves ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Receptor
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 ag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Agonists
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 r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
7-OH-DPAT
7-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with reasonable selectivity for the D3 receptor subtype, and low affinity for serotonin receptors, unlike its structural isomer 8-OH-DPAT. 7-OH-DPAT is self-administered in several animal models, and is used to study addiction to cocaine. See also * 5-OH-DPAT * 8-OH-DPAT * PD-128,907 * Rotigotine Rotigotine, sold under the brand name Neupro among others, is a dopamine agonist of the non-ergoline class of medications indicated for the treatment of Parkinson's disease and restless legs syndrome. It is formulated as a once-daily transdermal ... * UH-232 References Phenols Dopamine agonists Aminotetralins {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT7 Agonists
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the ''HTR7'' gene, which in humans is transcribed into 3 different splice variants. Function When the 5-HT7 receptor is activated by serotonin, it sets off a cascade of events starting with release of the stimulatory G protein Gs from the GPCR complex. Gs in turn activates adenylate cyclase which increases intracellular levels of the second messenger cAMP. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT7 Receptor
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the ''HTR7'' gene, which in humans is transcribed into 3 different splice variants. Function When the 5-HT7 receptor is activated by serotonin, it sets off a cascade of events starting with release of the stimulatory G protein Gs from the GPCR complex. Gs in turn activates adenylate cyclase which increases intracellular levels of the second messenger cAMP. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
UH-301
(S)-UH-301 is a drug and research chemical widely used in scientific studies. It acts as a selective 5-HT1A receptor silent antagonist. It is structurally related to 8-OH-DPAT. UH-301 was found to produce a head-twitch response in mice which is usually typical of 5-HT2A agonist drugs, and has subsequently been used to investigate how 5-HT1A receptor activity modulates 5-HT2A receptors downstream. See also * 4-HO-DPT * Robalzotan Robalzotan (NAD-299, AZD-7371) is a selective antagonist at the 5-HT1A receptor. It was shown to completely reverse the autoreceptor-mediated inhibition of serotonin release induced by the administration of selective serotonin reuptake inhibit ... * UH-232 References 5-HT1A antagonists Phenols Fluoroarenes Aminotetralins {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bay R 1531
Bay R 1531 is a tricyclic tryptamine derivative which acts as a selective serotonin receptor 5-HT1A agonist. It was researched unsuccessfully for the treatment of stroke but remains in use for scientific research. See also * 8-OH-DPAT * RDS-127 * RU-28306 * LY-293,284 * NDTDI NDTDI is a tricyclic tryptamine derivative which is thought to act as a serotonin receptor agonist, though its pharmacology has not been studied in detail. It is a structurally simplified analogue of LSD and is reported to retain similar effect ... References {{Tryptamines Serotonin receptor agonists Tryptamines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-OH-DPAT
5-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with selectivity for the D2 receptor and D3 receptor subtypes. Only the (''S'')-enantiomer is active as an agonist, with the (''R'')-enantiomer being a weak antagonist at D2 receptors. Radiolabelled 11C-5-OH-DPAT is used as an agonist radioligand for mapping the distribution and function of D2 and D3 receptors in the brain, and the drug is also being studied in the treatment of Parkinson's disease. See also * 7-OH-DPAT * 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonists to be discove ... References Phenols Dopamine agonists Aminotetralins {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aminotetralin
2-Aminotetralin (2-AT), also known as 1,2,3,4-tetrahydronaphthalen-2-amine (THN), is a stimulant drug with a chemical structure consisting of a tetralin group combined with an amine. 2-AT is a rigid analogue of phenylisobutylamine and fully substitutes for d-amphetamine in rat discrimination tests, although at one eighth the potency. It has been shown to inhibit the reuptake of serotonin and norepinephrine, and likely induces their release Release may refer to: * Art release, the public distribution of an artistic production, such as a film, album, or song * Legal release, a legal instrument * News release, a communication directed at the news media * Release (ISUP), a code to iden ... as well. It is also likely to act on dopamine on account of its full substitution of d-amphetamine in rodent studies. Chemical derivatives A number of derivatives of 2-aminotetralin exist, including: See also * 2-Aminodilin * 2-Aminoindane References {{DEFAULTSORT:Ami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Research Chemical
Research chemicals are chemical substances used by scientists for medical and scientific research purposes. One characteristic of a research chemical is that it is for laboratory research use only; a research chemical is not intended for human or veterinary use. This distinction is required on the labels of research chemicals, and is what exempts them from regulation under parts 100-740 in Title 21 of the Code of Federal Regulations ( 21CFR). Background Pharmacological research chemicals Research chemicals are fundamental in the development of novel pharmacotherapies. Common medical laboratory uses include ''in vivo'' and animal testing to determine therapeutic value, toxicology testing by contract research organization In the life sciences, a contract research organization (CRO) is a company that provides support to the pharmaceutical, biotechnology, and medical device industries in the form of research services outsourced on a contract basis. A CRO may provid ...s to d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradycardia
Bradycardia (also sinus bradycardia) is a slow resting heart rate, commonly under 60 beats per minute (BPM) as determined by an electrocardiogram. It is considered to be a normal heart rate during sleep, in young and healthy or elderly adults, and in athletes. In some people, bradycardia below 60 BPM may be associated with fatigue, weakness, dizziness, sweating, and fainting. The term "relative bradycardia" is used to refer to a heart rate slower than an individual's typical resting heart rate. Athletes may have athletic heart syndrome, which includes bradycardia as part of the cardiovascular adaptations to training and participation. The word "bradycardia" is from the Greek βραδύς ''bradys'' "slow", and καρδία ''kardia'' "heart". Classification Sinus Atrial bradycardias are divided into three types. The first, respiratory sinus arrhythmia, is usually found in young and healthy adults. Heart rate increases during inhalation and decreases during exhalation. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Releasing Agents
A serotonin releasing agent (SRA) is a type of drug that induces the releasing agent, 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 wikt:efflux, efflux at other types of monoamine neurons. SSRAs have been used clinically as appetite suppressants, and they have also been proposed as novel antidepressants and anxiolytics with the potential for a faster onset of action and superior efficacy relative to the selective serotonin reuptake inhibitors (SSRIs). A closely related type of drug is a serotonin reuptake inhibitor (SRI). Examples and use of SRAs Substituted amphetamine, Amphetamines like MDMA, 3,4-Methylenedioxy-N-ethylamphetamine, MDEA, methylenedioxyamphetamine, MDA, and MBDB, among other relatives (see substituted methylenedioxyphenethylamine, MDxx), are recreational drugs termed entactogens. They act as serotonin-norepinephrine-dopamine releasing ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
