"目录号: HY-15310
Ivermectin是广泛使用于人类和动物的抗寄生虫剂。它是P2X4和α7nAChRs的正异构效应物。
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生物活性
Description
Ivermectin is a widely used antiparasitic agent in human and veterinary medicine. It is a positive allosteric effector ofP2X4and the α7 neuronal nicotinic acetylcholine receptor (nAChRs).
In Vitro
Ivermectin (IVM) is a specific positive allosteric effector of heterologously expressed P2X4and possibly of heteromeric P2X4/ P2X6channels. In the submicromolar range (EC50=250 nM) the action of IVM is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4channel currents evoked by ATP. IVM also markedly increases the potency of ATP and that of the normally low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X4channels[1]. IVM activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis. The major mode of action of IVM is most likely the disruption of ingestive activity of the parasite, resulting in starvation[2]. Preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human α7 nicotinic acetylcholine receptors reconstituted in Xenopus laevis oocytes and K-28 cells[3]. Ivermectin activates the rat recombinant α1β2γ2sGABAAreceptor. Activation of the channel with 10 mM GABA results in currents rising within 1 ms to their maximal amplitudes. The EC50value for GABA is 7.5 μM[4].
Clinical Trial
University of California, San Diego-Galderma
Rosacea
July 2016
Phase 1-Phase 2
Rabin Medical Center
Demodicidosis-Rosacea
February 2014
Phase 3
Centre d'Appui à la lutte contre la Maladie-Malaria Research and Training Center, Bamako, Mali-World Health Organization
Lymphatic Filariasis
May 2001
Phase 4
Johnson & Johnson Consumer and Personal Products Worldwide
Healthy
September 2005
Phase 1
Johnson & Johnson Consumer and Personal Products Worldwide
Healthy
March 2005
Phase 1
Johnson & Johnson Consumer and Personal Products Worldwide
Healthy
February 2005
Phase 1
University Hospital, Basel, Switzerland
Malaria
November 2016
Phase 1
Centro per le Malattie Tropicali-European Commission
Strongyloidiasis
March 2013
Phase 3
World Health Organization
Onchocerciasis
April 2009
Phase 3
Robert Colebunders-Universiteit Antwerpen
Ivermectin-Onchocerciasis-Epilepsy
April 1, 2017
Phase 4
University of California, Los Angeles
Alcohol Use Disorder
February 2014
Phase 1-Phase 2
Mahidol University-Atlantic Laboratory Ltd
Chronic Strongyloidiasis
July 2008
Phase 3
Topaz Pharmaceuticals Inc
Head Lice
March 2010
Phase 3
Topaz Pharmaceuticals Inc
Pediculus Humanus Capitis (Head Lice)
March 2009
Phase 2
Johnson & Johnson Consumer and Personal Products Worldwide
Lice Infestations
February 2004
Phase 3
Topaz Pharmaceuticals Inc
Head Lice
March 2010
Phase 3
Colorado State University-Institut de Recherche en Sciences de la Sante, Burkina Faso-Centre Muraz-Ministère de la Santé du Burkina Faso
Malaria-Lymphatic Filariasis
June 2015
Phase 2-Phase 3
National Institute of Allergy and Infectious Diseases (NIAID)-National Institutes of Health Clinical Center (CC)
Loiasis
April 2012
Phase 4
Topaz Pharmaceuticals Inc
Head Lice
October 2009
Phase 2
Mahidol University-Ministry of Health, Thailand
Dengue Fever
February 2014
Phase 2-Phase 3
Liverpool School of Tropical Medicine-Kenya Medical Research Institute-Centers for Disease Control and Prevention
Malaria
July 2015
Phase 2
University Hospital, Bordeaux
Scabies
January 2016
Phase 3
Universidad Nacional de Colombia
Chronic Blepharitis
October 2014
Phase 3
Assistance Publique - Hôpitaux de Paris
Gale-Severe Forms of Scabies-Oral Parasitic Drug-Ivermectin
March 2017
Phase 3
Topaz Pharmaceuticals Inc
Head Lice
September 2009
Phase 1
University Hospitals Cleveland Medical Center
Lymphatic Filariasis
May 2014
Phase 2
London School of Hygiene and Tropical Medicine-Emory University
Lymphatic Filariasis
January 2009
London School of Hygiene and Tropical Medicine-Atoifi Adventist Hospital, Solomon Islands-Kirby Institute-Murdoch Childrens Research Institute
Scabies-Yaws-Impetigo
July 2016
Phase 4
University Hospitals Cleveland Medical Center-Washington University School of Medicine
Wuchereria Bancrofti Infection
April 2016
Phase 1
Actavis Inc.
Moderate to Severe Papulopustular Rosacea
June 2016
Phase 3
Galderma R&D
Papulopustular Rosacea
April 2012
Phase 3
London School of Hygiene and Tropical Medicine-Radboud University-Centre National de Recherche et de Formation sur le Paludisme, Burkina Faso
Malaria
January 2013
Phase 1-Phase 2
University Ghent
Scabies
July 2004
Phase 2
Emory University
Trachoma-Lymphatic Filariasis
February 2014
Phase 4
Noguchi Memorial Institute for Medical Research-Ghana Health Services
Lymphatic Filariasis-Helminth Infection
May 19, 2017
Phase 4
Centers for Disease Control and Prevention-Universidad del Valle, Guatemala
Ascariasis-Trichuriasis-Hookworm Infection-Strongyloidiasis-Pediculosis
February 2005
Galderma
Rosacea
May 15, 2017
Phase 4
Edward Via Virginia College of Osteopathic Medicine
Scabies
May 2007
Galderma
Rosacea
December 2015
Phase 4
Washington University School of Medicine-The Task Force for Global Health-Murdoch Children's Research Institute
Lymphatic Filariases-Scabies-Impetigo-Soil Transmitted Helminths
July 13, 2017
Washington University School of Medicine
Lymphatic Filariasis-Onchocerciasis-Soil Transmitted Helminth (STH) Infections
February 2014
Washington University School of Medicine
Lymphatic Filariasis-Onchocerciasis-Soil Transmitted Helminth (STH) Infections
March 2012
Centre d'Appui à la lutte contre la Maladie-International Trachoma Initiative
Parasitic Diseases-Bacterial Diseases
February 2010
World Health Organization
Onchocerciasis
September 2006
Phase 2
Universidad Nacional de Salta-Fundación Mundo Sano-Albert B. Sabin Vaccine Institute
Helminthiasis-Strongyloides Stercoralis Infection
December 2010
National Institute of Allergy and Infectious Diseases (NIAID)-National Institutes of Health Clinical Center (CC)
Lymphatic Filariasis
February 22, 2006
Phase 2
