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5-HT5A
5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the ''HTR5A'' gene. Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes. Function The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization. The 5-HT5A receptor has been shown to be functional in a native expression system. Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B, however while humans possess a gene coding for the 5-HT5B subtype, its cod ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT Receptor
5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gast ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SB-699,551
SB-699551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes. Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage, In animal studies, SB-699551 was found to block cue-mediated responding to LSD, again suggesting an antipsychotic type of activity. It also reduces the viability of certain types of cancer Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b ... cells ''in vitro'', suggesting the 5-HT5A receptor as a possible target for novel chemotherapy drugs. References 5-HT5 antagonists Dimethylamino compounds Carboxamides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-hydroxytryptamine
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methylergometrine
Methylergometrine, also known as methylergonovine and sold under the brand name Methergine, is a medication of the ergoline and lysergamide groups which is used as an oxytocic in obstetrics and in the treatment of migraine. It reportedly produces psychedelic effects similar to those of lysergic acid diethylamide (LSD) at high doses. It is on the World Health Organization's List of Essential Medicines. Medical uses Obstetric use Methylergometrine is a smooth muscle constrictor that mostly acts on the uterus. It is most commonly used to prevent or control excessive bleeding following childbirth and spontaneous or elective abortion, and also to aid in expulsion of retained products of conception after a missed abortion (miscarriage in which all or part of the fetus remains in the uterus) and to help deliver the placenta after childbirth. It is available as tablets or injection ( IM or IV) or in liquid form to be taken orally. Migraine Methylergometrine is sometimes used for both ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olanzapine
Olanzapine (sold under the trade name Zyprexa among others) is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. For schizophrenia, it can be used for both new-onset disease and long-term maintenance. It is taken by mouth or by injection into a muscle. Common side effects include weight gain, movement disorders, dizziness, feeling tired, constipation, and dry mouth. Other side effects include low blood pressure with standing, allergic reactions, neuroleptic malignant syndrome, high blood sugar, seizures, and tardive dyskinesia. In older people with dementia, its use increases the risk of death. Use in the later part of pregnancy may result in a movement disorder in the baby for some time after birth. Although how it works is not entirely clear, it blocks dopamine and serotonin receptors. Olanzapine was patented in 1991 and approved for medical use in the United States in 1996. It is available as a generic medication. In 2020, it was the 164t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lisuride
Lisuride, sold under the brand name Dopergin among others, is a monoaminergic medication of the ergoline class which is used in the treatment of Parkinson's disease, migraine, and high prolactin levels. It is taken by mouth. Side effects of lisuride include nausea and decreased blood pressure, among others. Lisuride acts as a mixed agonist and antagonist of dopamine, serotonin, and adrenergic receptors. Activation of specific dopamine receptors is thought to be responsible for its effectiveness in the treatment of Parkinson's disease and ability to suppress prolactin levels, while interactions with serotonin receptors are thought to be principally involved in its effectiveness for migraine. Medical uses Lisuride is used to lower prolactin and, in low doses, to prevent migraine attacks. The use of lisuride as initial antiparkinsonian medication for Parkinson's disease has been advocated, delaying the need for levodopa until lisuride becomes insufficient for controlling the park ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Valerian (herb)
Valerian (''Valeriana officinalis'', Caprifoliaceae) is a perennial flowering plant native to Europe and Asia. In the summer when the mature plant may have a height of , it bears sweetly scented pink or white flowers that attract many fly species, especially hoverflies of the genus ''Eristalis''. It is consumed as food by the larvae of some Lepidoptera (butterfly and moth) species, including the grey pug. Crude extract of valerian root may have sedative and anxiolytic effects, and is commonly sold in dietary supplement capsules to promote sleep, but there is insufficient clinical evidence that it is effective for this purpose. Its roots and leaves cause a catnip-like response in cats. History Valerian has been used as a herb in traditional medicine since at least the time of ancient Greece and Rome. Hippocrates described its properties, and Galen later prescribed it as a remedy for insomnia. In medieval Sweden, it was sometimes placed in the wedding clothes of the groom to wa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Valerenic Acid
Valerenic acid is a sesquiterpenoid constituent of the essential oil of the valerian plant. Valerian is used as a herbal sedative which may be helpful in the treatment of insomnia. Valerenic acid may be at least partly responsible for valerian's sedative effects, in addition to the other valerenic acids hydroxyvalerenic acid and acetoxyvalerenic acid. Valerian supplements are often standardized to contain a particular amount of valerenic acid by weight (often 0.8%). Valerenic acid acts as a subtype-selective GABAA receptor positive allosteric modulator via a binding site in the transmembrane domain at the β+α− interface. At receptors expressed in Xenopus oocytes (frog eggs) it was shown that only assemblies incorporating β2 or β3 subunits were stimulated by valerenic acid. A study in mice demonstrated that a single amino acid substitution (N265M) in the β3 subunit severely decreases the anxiolytic effect. Modulation of ion channel action was not significantly dep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-Carboxamidotryptamine
5-Carboxamidotryptamine (5-CT) is a tryptamine derivative closely related to the neurotransmitter serotonin. 5-CT acts as a non-selective, high-affinity full agonist at the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 receptors, as well as at the 5-HT2, 5-HT3, 5-HT6 receptors with lower affinity. It has negligible affinity for the 5-HT1E and 5-HT1F receptors. 5-CT binds most strongly to the 5-HT1A receptor and it was once thought to be selective for this site. Recently, a close derivative of 5-CT, AH-494 has been shown to function as an agonist of 5-HT7, although being more selective over 5-HT1A. Structural study indicated residue Ser5x43 might play critical roles in the selectivity of 5-CT across the serotonin receptor family. See also * 2-Methyl-5-hydroxytryptamine * 5-Benzyloxytryptamine * 5-Methoxytryptamine * α-Methyl-5-hydroxytryptamine * Frovatriptan * AH-494 * Acetryptine Acetryptine (INN) (developmental code name W-2965-A), also known as 5-acetyltryp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions are long-acting and last for 2–4 weeks. Common side effects include extrapyramidal symptoms, movement problems, sedation, sleepiness, dizziness, trouble seeing, constipation, and increased weight. Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and hyperglycemia, high blood sugar levels. In older people with psychosis as a result of dementia, it may increase the risk of death. It is unknown if it is safe for use in pregnancy. Its mechanism of action is not entirely clear, but is believed to be related to its action as a dopamine antagonist, dopamine and serotonin antagonist. Study of risperidone began in the late 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Latrepirdine
Latrepirdine (INN, also known as dimebolin and sold as Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. Research was conducted in both Russia and western nations into potential applications as a neuroprotective drug to treat Alzheimer's disease and, possibly, as a nootropic, as well. After a major phase III clinical trial for Alzheimer's disease (AD) treatment failed to show any benefit, three other AD trials continued.Novel Alzheimer's Drug Flops ''MedPage Today'', March 03, 2010 Major industry-based development in this indication essentially stopped after another Phase III trial suffered the same fate in 2012.Sweetlove M: Phase III CONCERT Trial of Latrepirdine. Negative results. Pharm Med 2012;26(2):113-115 Latrepirdine failed in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
