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Tachykinin Receptor 3
Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the ''TACR3'' gene. Function This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B. Selective ligands A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications. Agonists * Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK3 * Senktide – 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6 Antagonists * Elinzanetant (BAY-3427080 GSK-1144814, NT-814) * Fezolinetant (ESN-364) * Osanetant (SR-142, ... [...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 residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, responding to stimuli, providing structure to cells and organisms, and transporting molecules from one location to another. Proteins differ from one another primarily in their sequence of amino acids, which is dictated by the nucleotide sequence of their genes, and which usually results in protein folding into a specific 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 peptides. The individual amino acid residues are bonded together by peptide bonds and adjacent amino acid residues. The sequence of amino acid residue ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a basic unit of heredity and 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 noncoding genes. During gene expression, the DNA is first copied into RNA. The RNA can be directly functional or be the intermediate template for a protein that performs a function. The transmission of genes to an organism's offspring is the basis of the inheritance of phenotypic traits. These genes make up different DNA sequences called genotypes. Genotypes along with environmental and developmental factors determine what the phenotypes will be. Most biological traits are under the influence of polygenes (many different genes) as well as gen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachykinin
Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue. The tachykinin family is characterized by a common C-terminal sequence, Phe-X- Gly-Leu- Met-NH2, where X is either an Aromatic or an Aliphatic amino acid. The genes that produce tachykinins encode precursor proteins called preprotachykinins, which are chopped apart into smaller peptides by posttranslational proteolytic processing. The genes also code for multiple splice forms that are made up of different sets of peptides. Tachykinins excite neurons, evoke behavioral responses, are potent vasodilators, and contract (directly or indirectly) many smooth muscles. Tachykinins are from ten to twelve residues long. The two human tachykinin genes are called TAC1 and TAC3 for historical reasons, and are equivalent to Tac1 and Tac2 of the mouse, respectively. TAC1 encodes neurokinin A (formerly known a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone. Additionally, NKB is associated with pregnancy in females and maturation in young adults. Reproductive function is highly dependent on levels of both neurokinin B and also the G-protein coupled receptor ligand kisspeptin. The first NKB studies done attempted to resolve why high levels of the peptide may be implicated in pre-eclampsia during pregnancy. NKB, kisspeptin, and dynorphin together are found in the arcuate nucleus (ARC) known as the KNDy subpopulation. This subpopulation is targeted by many steroid hormones and works to form a network that feeds back to GnRH pulse generator. Synthesis Neurokinin B is found in humans as a ten-peptide chain (decapeptide) attached to a terminal amide group. The peptide formula is H-Asp-Met-His-Asp-Phe-Phe-Val-Gly-Leu-Met-NH2 (DMHDFFVGLM-NH2). Neuroki ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone. Additionally, NKB is associated with pregnancy in females and maturation in young adults. Reproductive function is highly dependent on levels of both neurokinin B and also the G-protein coupled receptor ligand kisspeptin. The first NKB studies done attempted to resolve why high levels of the peptide may be implicated in pre-eclampsia during pregnancy. NKB, kisspeptin, and dynorphin together are found in the arcuate nucleus (ARC) known as the KNDy subpopulation. This subpopulation is targeted by many steroid hormones and works to form a network that feeds back to GnRH pulse generator. Synthesis Neurokinin B is found in humans as a ten-peptide chain (decapeptide) attached to a terminal amide group. The peptide formula is H-Asp-Met-His-Asp-Phe-Phe-Val-Gly-Leu-Met-NH2 (DMHDFFVGLM-NH2). Neuroki ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elinzanetant
Elinzanetant (developmental code names BAY-3427080 GSK-1144814, NT-814) is an orally active small-molecule neurokinin/tachykinin NK1 receptor and NK3 receptor antagonist which is under development by Bayer, GlaxoSmithKline, and NeRRe Therapeutics for the treatment of hot flashes and "sex hormone disorders". It has been found to relieve hot flashes in postmenopausal women and to dose-dependently suppress luteinizing hormone, estradiol, and progesterone levels in premenopausal women. As of August 2021, elinzanetant is in phase 2 clinical trials for hot flashes and "sex hormone disorders". It was also under development for the treatment of schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ... and opioid-related disorders, but development was discontinued for these uses. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fezolinetant
Fezolinetant (; former developmental code name ESN-364) is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which is under development by Ogeda (formerly Euroscreen) for the treatment of sex hormone-related disorders. As of May 2017, it has completed phase I and phase IIa clinical trials for hot flashes in postmenopausal women. Phase IIa trials in polycystic ovary syndrome patients are ongoing. In April 2017, it was announced that Ogeda would be acquired by Astellas Pharma. Fezolinetant shows high affinity for and potent inhibition of the NK3 receptor ''in vitro'' (Ki = 25 nM, = 20 nM). Loss-of-function mutations in ''TACR'' and ''TACR3'', the genes respectively encoding neurokinin B and its receptor, the NK3 receptor, have been found in patients with idiopathic hypogonadotropic hypogonadism. In accordance, NK3 receptor antagonists like fezolinetant have been found to dose-dependently suppress luteinizing hormone (LH) secretion, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Osanetant
Osanetant (developmental code name SR-142,801) is a Tachykinin receptor 3, neurokinin 3 receptor receptor antagonist, antagonist which was developed by Sanofi-Synthélabo and was being researched for the treatment of schizophrenia but was discontinued. It was the first non-peptide NK3 antagonist developed in the mid-1990s. Professor David J. Anderson, Director and Leadership Chair of the Tianqiao and Chrissy Chen Institute for Neuroscience at California Institute of Technology, has advocated that osanetant be explored as a treatment for pain, anxiety, and aggression in humans and companion animals experiencing bereavement or social isolation, citing research suggesting that osanetant has an excellent safety profile and suppresses negative effects of social isolation in mice through an evolutionarily-conserved mechanism and without acting as a depressant. Another potential application for osanetant is in the treatment of drug addiction, as it has been found to block the effects o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pavinetant
Pavinetant (, ; developmental code names MLE-4901, AZD-4901, AZ-12472520, AZD-2624), is a small-molecule, oral administration, orally active, binding selectivity, selective tachykinin receptor 3, neurokinin-3 (NK3) tachykinin receptor 3, receptor receptor antagonist, antagonist which was under development by AstraZeneca and Millendo Therapeutics for the treatment of hot flashes and polycystic ovary syndrome (PCOS). It was also under investigation for the treatment of schizophrenia, but development was discontinued for this indication due to lack of effectiveness. In November 2017, development of the medication for hot flashes and PCOS was also terminated after its developer assessed the clinical risks and benefits. See also * Tachykinin receptor 3#Agonists, Tachykinin receptor 3 § Agonists References External links Pavinetant - AdisInsight Abandoned drugs Carboxamides NK3 receptor antagonists Quinolines Sulfonamides {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Talnetant
Talnetant (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for several functions (primarily treatment of irritable bowel syndrome, despite a 2007 study finding no statistically significant improvement in rectal hypersensitivity over placebo). Its use as a potential antipsychotic drug for the treatment of schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ... has also been discontinued. See also * Tachykinin receptor 3 § Agonists References Antipsychotics NK3 receptor antagonists Quinolinols Carboxamides {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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