WebApr 30, 2024 · In 2003, aprepitant (EMEND, Merck Sharp & Dohme B.V.) became the first tachykinin-1 receptor (TAC1R, aka neurokinin-1 receptor NK-1R) antagonist approved for the prevention of acute and delayed chemotherapy-induced nausea and vomiting, a side-effect that can affect more than 99% of patients treated with cisplatin . WebTachykinin regulation of cholinergic transmission in the limbic/prefrontal territory of the rat dorsal striatum: implication of new neurokinine 1-sensitive receptor binding site and interaction with enkephalin/mu opioid receptor transmission.
Biological and Pharmacological Aspects of the NK1-Receptor - Hindawi
WebApr 1, 2008 · George et al. (2008) investigated the role of the neurokinin-1 receptor, a mediator of behavioral stress responses, in alcohol dependence ( 103780) and treatment. In preclinical studies, mice genetically deficient in NK1R showed a marked decrease in voluntary alcohol consumption and had an increased sensitivity to the sedative effects of … WebThe tachykinin NK(1) receptor antagonist SR140333 dose-dependently (0.05 to 0.5 mg kg(-1)) suppressed the local (intestine) and remote (lung) increases in vascular permeability and neutrophil recruitment following mild I/R injury. A structurally-distinct NK(1) receptor antagonist, CP99,994, but not tachykinin NK(2) or NK(3) receptor antagonists ... immatriculation tc
24807 - Gene ResultTacr1 tachykinin receptor 1 [ (Norway rat)]
WebThe tachykinin receptor agents are ligands for a class of G-protein-coupled receptors referred to as tachykinin or neurokinin receptors. Prototypic agonists include the peptide … The tachykinin receptor 1 (TACR1) also known as neurokinin 1 receptor (NK1R) or substance P receptor (SPR) is a G protein coupled receptor found in the central nervous system and peripheral nervous system. The endogenous ligand for this receptor is Substance P, although it has some affinity for other … See more Tachykinins are a family of neuropeptides that share the same hydrophobic C-terminal region with the amino acid sequence Phe-X-Gly-Leu-Met-NH2, where X represents a hydrophobic residue that is either an See more This receptor is considered an attractive drug target, particularly with regards to potential analgesics and anti-depressants. It is also a potential treatment for alcoholism and See more • NK1 receptor antagonist • Tachykinin receptor • Discovery and development of neurokinin 1 receptor antagonists See more • "Tachykinin Receptors: NK1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. See more Many selective ligands for NK1 are now available, several of which have gone into clinical use as antiemetics. • GR-73632 - potent and selective agonist, EC50 2nM, 5-amino acid polypeptide chain. CAS# 133156-06-6 • See more • Burcher E (June 1989). "The study of tachykinin receptors". Clinical and Experimental Pharmacology & Physiology. 16 (6): 539–543. doi:10.1111/j.1440-1681.1989.tb01602.x See more WebSep 14, 2005 · Rat/mouse hemokinin 1 (r/m HK-1) is a novel tachykinin peptide whose biological functions are not fully understood. This work was designed to observe the effects of r/m HK-1 in pain modulation at supraspinal level in mice using tail-flick test. ... When r/m HK-1 co-injected (i.c.v.) with SR140333 (a selective NK(1) receptor antagonist ... list of shipping lines