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*  Tachykinin peptides
... an antagonist at the neurokinin-2 receptor in various rodent-models". Pharmacol. Biochem. Behav. 89 (1): 36-45. doi:10.1016/j. ... NK1, NK2 and NK3 selectively bind to substance P, neurokinin A, and neurokinin B, respectively. Whilst the receptors are not ... receptors (NK1 receptor antagonists), through which substance P acts, have been proposed to belong to a new class of ... neurokinin A, neurokinin K, and neurokinin gamma) on the expression of male rat sexual behavior". Physiol. Behav. 54 (2): 249- ...
*  Substance P
NK1-receptor, NK1R). It belongs to the tachykinin receptor sub-family of GPCRs. Other neurokinin subtypes and neurokinin ... Hesketh PJ (Jul 2001). "Potential role of the NK1 receptor antagonists in chemotherapy-induced nausea and vomiting". Supportive ... "Absence of the SP/SP receptor circuitry in the substance P-precursor knockout mice or SP receptor, neurokinin (NK)1 knockout ... Its receptor - the neurokinin type 1 - is distributed over cytoplasmic and nuclear membranes of many cell types (neurons, glia ...
*  Vestipitant
... (INN) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It is under ... Reddy, GK; Gralla, RJ; Hesketh, PJ (2006). "Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy- ... NK1 receptor antagonist Aprepitant Casopitant Fosaprepitant L-733,060 Maropitant "International Nonproprietary Names for ... 2008). "Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to ...
*  Tachykinin receptor 1
NK1 receptor antagonist Tachykinin receptor Discovery and development of neurokinin 1 receptor antagonists GRCh38: Ensembl ... NK1 receptor antagonists block responses to a broader range of emetic stimuli than the established 5-HT3 antagonist treatments ... SP binds to all three of the tachykinin receptors, but it binds most strongly to the NK1 receptor. Tachykinin NK1 receptor ... IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Receptors, Neurokinin-1 ...
*  Tradipitant
2008). "Neurokinin 1 receptor antagonism as a possible therapy for alcoholism". Science. 6: 1536-1539. doi:10.2147/SAR.S70350. ... Tradipitant (VLY-686 or LY686017) is an experimental drug that is a neurokinin 1 antagonist. It works by blocking substance P, ... 2010). "Development of the 2nd generation neurokinin-1 receptor antagonist LY686017 for social anxiety disorder". European ... 68 (1): 48-52. doi:10.1016/j.eplepsyres.2005.09.019. PMID 16377153. George, DT; Gilman, J; Hersh, J; et al. ( ...
*  L-733,060
Varty GB, Cohen-Williams ME, Hunter JC (2003). "The antidepressant-like effects of neurokinin NK1 receptor antagonists in a ... application to the asymmetric syntheses of neurokinin substance P receptor antagonist (−)-L-733,061 and (−)-deoxocassine". The ... anxiolytic-like effects of selective neurokinin NK1 receptor antagonists". Neuropsychopharmacology. 27 (3): 371-9. doi:10.1016/ ... L-733,060 is a drug developed by Merck which acts as an orally active, non-peptide, selective antagonist for the NK1 receptor, ...
*  Serlopitant
Payton, S (August 2010). "Urinary Incontinence: Neurokinin Receptor Antagonist Inferior to Tolterodine for OAB". Nature Reviews ... Serlopitant (INN, codenamed VPD-737) is a drug which acts as an NK1 receptor antagonist. It was assessed in clinical trials for ... Serlopitant is now undergoing clinical trials for the treatment of chronic pruritus (itch) NK1 receptor antagonist " ... Placebo Controlled Trial of a Neurokinin-1 Receptor Antagonist for Overactive Bladder". The Journal of Urology. 184 (2): 616-22 ...
*  Befetupitant
NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783- ... Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists ... is a drug developed by Hoffmann-La Roche which acts as a potent and selective antagonist for the NK1 receptor. It was ... 2006 Mar 1;16(5):1362-5. PMID 16332435 Bignami F, Giacomini C, Lorusso A, Aramini A, Rama P, Ferrari G. ...
*  Aprepitant
Trist, DG; Ratti, E; Bye, A (2013). "Why receptor reserve matters for neurokinin1 (NK1) receptor antagonists". J. Recept. ... May 2004). "Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant". Biological ... Aprepitant is classified as an NK1 antagonist because it blocks signals given off by NK1 receptors. This, therefore, decreases ... It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid ...
*  Vofopitant
... is a drug which acts as an NK1 receptor antagonist. It has antiemetic effects as with other NK1 antagonists, and also shows ... A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept ... NK1 receptor antagonist Gardner CJ, Armour DR, Beattie DT, Gale JD, Hawcock AB, Kilpatrick GJ, Twissell DJ, Ward P. GR205171: a ... novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept ...
*  Maropitant
... is a neurokinin (NK1) receptor antagonist, which was developed by Zoetis specifically for the treatment of motion sickness and ... 2013). "Effect of maropitant, a neurokinin-1 receptor antagonist, on the minimum alveolar concentration of sevoflurane during ... 2011). "Maropitant an NK-1 Antagonist Decreases the Anesthetic Requirements During Visceral Stimulation of the Ovary in Dogs". ...
*  Lanepitant
... (INN, code name LY303870) is a drug developed by Eli Lilly which acts as a selective antagonist for the NK1 receptor ... Pharmacological characterization of LY303870: a novel, potent and selective nonpeptide substance P (neurokinin-1) receptor ... PMID 11290877 Bignami F, Giacomini C, Lorusso A, Aramini A, Rama P, Ferrari G. NK1 receptor antagonists as a new treatment for ... antagonist. J Pharmacol Exp Ther. 1995 Nov;275(2):737-44. PMID 7473161 Goldstein DJ, Offen WW, Klein EG, Phebus LA, Hipskind P ...
*  Sean Ekins
... models for studying nuclear receptor-ligand co-evolution, computational models for PXR agonists and antagonists as well as ... and identification of the cytochrome P-450 inhibitory potency of neurokinin-1 receptor antagonists."[5] U.S. Patent no 6489094 ... J Pharmacol Exp Ther 301, 427-434 Ekins, S.; Erickson, J.A. (2002). "A pharmacophore for human pregnane-X-receptor ligands". ... 2005). "A Novel Method for Visualizing Nuclear Hormone Receptor Networks Relevant to Drug Metabolism". Drug Metab Dispos. 33: ...
*  NK1 receptor antagonist
2002), "The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists", ... Biological research that identified the many functions of tachykinins sparked interest in neurokinin receptor antagonists ... In the 1980s, several peptide antagonists derived from SP were the first NK1 receptor antagonists. However, these compounds, ... SP binds to all three of the tachykinin receptors, but it binds most strongly to the NK1 receptor. Tachykinin NK1 receptor, ...
*  Casopitant
NK1 receptor antagonist Aprepitant Fosaprepitant L-733,060 Maropitant Vestipitant "International Nonproprietary Names for ... Casopitant (INN, tentative trade names Rezonic (U.S.), Zunrisa (Europe)) is an neurokinin 1 receptor (NK1R) antagonist ...
*  Marcos A. Moreno
Todd Vanderah studying Neurokinin Receptor -1 (NK₁R) antagonists and Substance-P (SP) implications in neurological reward ...
*  Burapitant
... a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological ... which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor. While ... a centrally active nonpeptide antagonist of the tachykinin neurokinin 1 receptor: II. Neurochemical and behavioral ... 1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2- ...
*  Cancer and nausea
NK1 receptor antagonists: such as Aprepitant block the NK1 receptor in the brainstem and gastrointestinal tract. Their ... a neurokinin-1 antagonist) given before chemotherapy. A common consequence of cancer treatment is the development of ... This structure contains receptors which form a chemoreceptor trigger zone. Some of the receptors and neurotransmitters involved ... Prokinetic agents such as Metoclopramide Dopamine receptor antagonists such as Phenothiazines (Prochlorperazine and ...
*  Neurokinin A
Administration of DNK333 (a dual tachykinin receptor NK1/NK2 antagonist) have shown protective activity against neurokinin A ... Journal Maggi C, Patacchini R, Rovero P, Giachetti A (1993). "Tachykinin receptors and tachykinin receptor antagonists". J ... "A novel tachykinin NK2 receptor antagonist prevents motility-stimulating effects of neurokinin A in small intestine". Br J ... show the highest concentration of NK-2 receptors. NK-2 receptor antagonists have been theorized to have antidepressant benefits ...
*  Rolapitant
... selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets". ... which acts as a selective NK1 receptor antagonist (antagonist for the NK1 receptor). It has been approved as a medication for ... to block the closely related receptor NK2 or any other of 115 tested receptors and enzymes, more than 1000-fold therapeutic ... The approved antiemetic combination consists of rolapitant plus dexamethasone and a 5-HT3 antagonist. Under the US approval, ...
*  Tachykinin receptor 2
"Tachykinin antagonists inhibit nerve-mediated contractions in the circular muscle of the human ileum. Involvement of neurokinin ... Site-directed mutagenesis and identification of neurokinin A binding residues in the human neurokinin 2 receptor". The Journal ... "Crosstalk between neurokinin receptors is relevant to hematopoietic regulation: cloning and characterization of neurokinin-2 ... "C-terminal truncation of the neurokinin-2 receptor causes enhanced and sustained agonist-induced signaling. Role of receptor ...
*  Talnetant
... (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for ... Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. ... Receptor Antagonist SB-223412 (Talnetant): Potential Therapeutic Utility in the Treatment of Schizophrenia. ... Tachykinin receptor 3 § Agonists "UPDATE 1-GlaxoSmithKline prunes new drug pipeline". Reuters. Oct 15, 2007. Evangelista S. ...
*  Rostral ventromedial medulla
GABAA receptor involvement was demonstrated by intrathecal administration of gabazine, a GABAA antagonist, in animals receiving ... Pretreatment with a neurokinin 1 (NK1) antagonist prevented the antinociception induced by SP injection, but the NK1 antagonist ... Intra-RVM administration of AP5 or MK-801, NMDA receptor antagonists, resulted in a reversal of the mechanical sensitivity ... To test the effects of an NK1 antagonist during injury states, an NK1 antagonist was microinjected into the RVM after ...
*  Ezlopitant
Giardina GA, Gagliardi S, Martinelli M (August 2003). "Antagonists at the neurokinin receptors--recent patent literature". ... Ezlopitant (INN, code name CJ-11,974) is an NK1 receptor antagonist. It has antiemetic and antinociceptive effects. Pfizer was ... NK1 receptor antagonist Maropitant (tert-butyl instead of isopropyl) "International Nonproprietary Names for Pharmaceutical ... Tsuchiya M, Sakakibara A, Yamamoto M (January 2005). "A tachykinin NK1 receptor antagonist attenuates the 4 beta-phorbol-12- ...
*  Tachykinin receptor 3
NK3 receptor antagonists are being investigated as treatments for various indications. Neurokinin B - endogenous peptide ligand ... This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B. A number of selective ligands ... "Entrez Gene: TACR3 tachykinin receptor 3". Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research ... "Functional expression of a novel human neurokinin-3 receptor homolog that binds [3H]senktide and [125I-MePhe7]neurokinin B, and ...
*  Index of biochemistry articles
... receptor (biochemistry) - receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant ... neurokinin-2 receptor - neuron - neuronal cell adhesion molecule - neuropeptide - neuropeptide receptor - neuropeptide Y - ... G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ... CXCR4 receptor - cyclic AMP receptor - cyclic AMP receptor protein - cyclic AMP-responsive DNA-binding protein - cyclic ...