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5-HT1F
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it. Agonists * 5-''n''-Butyryloxy-DMT: >60-fold selectivity versus 5-HT1E receptor * BRL-54443 - mixed 5-HT1E/1F agonist * Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist * LY-334,370 - as well as related benzamides * LY-344,864 (N- 3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl4-fluorobenzamide) * Naratriptan - mixed 5-HT1B/1D/1F agonist * Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan molecule Antagonists MLS000756415 See also * 5-HT1 receptor * 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 multiple tissues including the Central nervous system, central and peripheral nervous systems ... References Further reading * * * * * * * * External links * * Seroton ... [...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 multiple tissues including the Central nervous system, central and peripheral nervous systems. They mediate both Neurotransmitter#Excitatory and inhibitory, excitatory and inhibitory Synaptic transmission, neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural Ligand (biochemistry), ligand. The serotonin receptors modulate the release of many neurotransmitters, including glutamic acid, glutamate, gamma-Aminobutyric acid, 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, cogn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1 Receptor
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] |
BRL-54443
BRL-54443 is a drug which acts as a selective agonist for the 5-HT1E and 5-HT1F serotonin receptor subtypes. See also * CP-94253 * RS134-49 * RU-24969 * Sertindole * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ... * VU6067416 References 5-HT1E agonists 5-HT1F agonists Hydroxyarenes Piperidinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eletriptan
Eletriptan, sold under the brand name Relpax and used in the form of eletriptan hydrobromide, is a second-generation triptan medication intended for treatment of migraine headaches. It is used as an abortive medication, blocking a migraine attack which is already in progress. Eletriptan is marketed and manufactured by Pfizer Inc. Approval and availability Eletriptan was approved by the US Food and Drug Administration (FDA) in December 2002, for the acute treatment of migraine with or without aura in adults. It is available only by prescription in the United States, Canada and Australia. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. It is available in 20 mg and 40 mg strengths. Eletriptan was covered by and ; both now expired. Mechanism of action Eletriptan is believed to reduce swelling of the blood vessels surrounding the brain. This swelling is associated with the head pain of a m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY334370
LY-334370 is a selective 5-HT1F receptor agonist which was under development by Eli Lilly and Company for the treatment of migraine headaches. The drug showed efficacy in a phase II clinical trial but further development was halted due to toxicity detected in animals. See also * CP-135807 * Lasmiditan * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ... References External links * 5-HT1F agonists Abandoned drugs Benzamides Drugs developed by Eli Lilly and Company 4-Fluorophenyl compounds Piperidinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lasmiditan
Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute (active but short-term) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not useful for prevention. It is taken by mouth. Common side effects include sleepiness, dizziness, tiredness, and numbness. Lasmiditan was approved in the United States in October 2019 and became available in February 2020. It was developed by Eli Lilly. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. Pharmacology Mechanism of action Lasmiditan is a serotonin receptor agonist that, like the unsuccessful LY-334,370, selectively binds to the 5-HT1F receptor subtype. A number of triptans have been shown to act on this subtype as well, but only after their affinity for 5-HT1B and 5-HT1D has been made responsible for their anti-migraine activity. The lack of affinity for these receptors might result in fewer side effects re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ditan
Ditans are a class of abortive medication for the treatment of migraines. The first ditan, Eli Lilly's lasmiditan, was approved by the FDA in 2019. Ditans selectively bind to the 5-HT1F receptor subtype. A number of triptans have been shown to act on this subtype as well, but only after their affinity for 5-HT1B and 5-HT1D has been made responsible for their anti-migraine activity. The lack of affinity for these receptors might result in fewer side effects related to vasoconstriction compared to triptans in susceptible patients, such as those with ischemic heart disease, Raynaud's phenomenon or after a myocardial infarction A myocardial infarction (MI), commonly known as a heart attack, occurs when Ischemia, blood flow decreases or stops in one of the coronary arteries of the heart, causing infarction (tissue death) to the heart muscle. The most common symptom .... A 1998 review has found such side effects to rarely occur in most patients taking triptans. One clini ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naratriptan
Naratriptan (trade names include Amerge) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. It is a selective 5-HT1 receptor subtype agonist. It was patented in 1987 and approved for medical use in 1997. Medical uses Naratriptan is used for the treatment of the acute migraine attacks and the symptoms of migraine, including severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound or light. Efficacy A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at marketed doses and that naratriptan, although less effective than sumatriptan and rizatriptan was more effective than placebo in reducing migraine symptoms at two hours and efficacy was demonstrated in almost two thirds of subjects after four hours of treatment. Side effects Side effects are similar to other triptan medications, with the incidence of side effects reportedly being lower than suma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metabolic reactions, DNA replication, Cell signaling, responding to stimuli, providing Cytoskeleton, structure to cells and Fibrous protein, organisms, and Intracellular transport, transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the Nucleic acid sequence, nucleotide sequence of their genes, and which usually results in protein folding into a specific Protein structure, 3D structure that determines its activity. A linear chain of amino acid residues is called a polypeptide. A protein contains at least one long polypeptide. Short polypeptides, containing less than 20–30 residues, are rarely considered to be proteins and are commonly called pep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protein-coding genes and non-coding genes. During gene expression (the synthesis of Gene product, RNA or protein from a gene), DNA is first transcription (biology), copied into RNA. RNA can be non-coding RNA, directly functional or be the intermediate protein biosynthesis, template for the synthesis of a protein. The transmission of genes to an organism's offspring, is the basis of the inheritance of phenotypic traits from one generation to the next. These genes make up different DNA sequences, together called a genotype, that is specific to every given individual, within the gene pool of the population (biology), population of a given species. The genotype, along with environmental and developmental factors, ultimately determines the phenotype ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamide
Benzamide is an organic compound with the chemical formula of C7H7NO. It is the simplest amide derivative of benzoic acid. In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large varie ... found in the herbs of '' Berberis pruinosa''. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
