"目录号: HY-14151
GPCR/G ProteinNeuronal Signaling-
Prucalopride (R093877)是高亲和性5-HT4受体激动剂，对5-HT4a/4b的pKi分别为8.6/8.1，比对其它受体的亲和性高150倍。
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生物活性
Description
Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)Target: 5-HT4 receptorPrucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor [1].
Clinical Trial
Movetis
Constipation
July 1997
Phase 1
Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
Constipation
May 2010
Phase 3
Movetis
Constipation
November 1998
Phase 1
Movetis
Constipation
January 2000
Phase 1
Janssen Pharmaceutica
Chronic Constipation
February 2013
Phase 4
Jinling Hospital, China
Postoperative Ileus
November 2013
Phase 2
Movetis
Constipation
January 2009
Phase 1
Shire
Non-cancer Pain-Opioid Induced Constipation
May 2010
Phase 3
Movetis
Constipation
November 1998
Phase 1
Universitaire Ziekenhuizen Leuven
Gastroparesis
November 2011
Phase 4
Movetis
Chronic Constipation
December 1994
Phase 2
Shandong University-Binzhou People's Hospital-Tai'an People's Hospital-Linyi People's Hospital
Prucalopride Plus Polyethylene Glycol in Bowel Preparation for Colonoscopyp
June 2016
Phase 4
Queen's University-Hotel Dieu Hospital-Janssen Inc.
Bowel Cleansing-Colon Capsule Completion Times
June 2013
Phase 3
Guang'anmen Hospital of China Academy of Chinese Medical Sciences-Ministry of Science and Technology of the People´s Republic of China
Constipation
April 2014
Shire
Healthy
March 2013
Phase 1
Movetis
Constipation
September 1996
Phase 2
Movetis
Constipation
March 1998
Phase 3
Movetis
Constipation
November 1995
Phase 2
University of British Columbia
Gastrointestinal Hemorrhage-Crohn Disease-Celiac Disease-Intestinal Diseases-Inflammatory Bowel Diseases
July 2016
Phase 4
Movetis
Constipation
April 1999
Phase 3
Shire
Constipation
June 2011
Phase 4
University of Auckland, New Zealand
Postoperative Ileus-Colorectal Surgery-Postoperative Complications
January 2017
Phase 3
Movetis
Constipation
April 1998
Phase 3
Norgine
Constipation
November 2010
Phase 3
Movetis
Constipation
March 1995
Phase 2
Movetis
Constipation
April 1997
Phase 2
Shire
Male Subjects With Chronic Constipation
September 2010
Phase 3
Shire
Chronic Constipation
January 2013
Phase 4
Movetis-FOCUS GmbH
Healthy Volunteers
December 2009
Phase 1
Movetis
Chronic Constipation
July 1998
Phase 3
Xian-Janssen Pharmaceutical Ltd.
Constipation
October 2014
Phase 4
University of Calgary-Janssen Inc.
Gastroparesis-Diabetes Mellitus
March 2014
Phase 2-Phase 3
Shire-PRA Health Sciences
Functional Constipation
April 2011
Phase 3
Movetis
Hepatic Impairment
May 2010
Phase 1
Movetis
Constipation
October 1998
Phase 3
Movetis
Constipation
March 1998
Phase 3
Movetis
Chronic Constipation
June 1998
Phase 3
Movetis
Constipation
February 1999
Phase 2
Movetis
Healthy
Phase 1
Universitaire Ziekenhuizen Leuven
Constipation
May 2013
Movetis
Constipation
August 1998
Phase 3
Queen's University-Hotel Dieu Hospital (Gastrointestinal Diseases Research Unit)
Quality of Bowel Preparation for the Colon Capsule-Colon Capsule Completion Rates-Colon Capsule Polyp Detection
July 2012
Phase 3
Janssen Korea, Ltd., Korea
Constipation
August 2012
Phase 4
Katholieke Universiteit Leuven-Universitaire Ziekenhuizen Leuven
Postoperative Ileus
July 2014
Phase 4
Yuhan Corporation
Healthy
August 2013
Phase 1
Yuhan Corporation
Functional Constipation
August 2015
Phase 1-Phase 2
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