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Prucalopride

普卡比利,R-93877,Resolor,Resotran,R93877,R 93877,

Prucalopride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。

目录号
EY0703
EY0703
EY0703
纯度
99.41%
99.41%
99.41%
规格
5 mg
10 mg
50 mg
原价
350
575
930
售价
350
575
930
库存
现货
现货
现货
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  • 生物活性

    Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Briejer MR, et al. Eur J Pharmacol, 2001, 423(1), 71-83.
    [2] Bouras EP, et al. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Gut. 1999 May;44(5):682-6.
    [3] Emmanuel AV, et al. Randomised clinical trial: the efficacy of prucalopride in patients with chronic intestinal pseudo-obstruction--a double-blind, placebo-controlled, cross-over, multiple n = 1 study. Aliment Pharmacol Ther. 2012 Jan;35(1):48-55.

    分子式
    C18H26ClN3O3    		 分子量
    367.87    		 CAS号
    179474-81-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    60 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    40 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01674192 Constipation Drug: prucalopride Movetis Phase 1 1997-07-01 2012-08-27
    NCT01116206 Constipation Drug: Prucalopride|Drug: Placebo Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 3 2010-05-01 2017-03-17
    NCT01670669 Constipation Drug: prucalopride Movetis Phase 1 1998-11-01 2012-08-20
    NCT00488215 Constipation Drug: prucalopride|Other: Placebo Movetis Phase 1 2000-01-01 2008-05-28
    NCT01692132 Chronic Constipation Drug: Prucalopride Janssen Pharmaceutica Phase 4 2013-02-01 2015-11-30
    NCT02004652 Postoperative Ileus Drug: Prucalopride|Drug: Placebo Jinling Hospital, China Phase 2 2013-11-01 2016-09-29
    NCT00903747 Constipation Drug: prucalopride|Drug: moxifloxacin|Drug: placebo Movetis Phase 1 2009-01-01 2009-05-15
    NCT01117051 Non-cancer Pain|Opioid Induced Constipation Drug: placebo|Drug: prucalopride Shire Phase 3 2010-05-01 2014-06-06
    NCT01674166 Constipation Drug: prucalopride Movetis Phase 1 1998-11-01 2012-08-27
    NCT02510976 Gastroparesis Drug: prucalopride|Drug: placebo Universitaire Ziekenhuizen Leuven Phase 4 2011-11-01 2015-12-14
    NCT00576511 Chronic Constipation Drug: prucalopride|Drug: placebo Movetis Phase 2 1994-12-01 2008-05-28
    NCT02781493 Prucalopride Plus Polyethylene Glycol in Bowel Preparation for Colonoscopyp Drug: 2 mg Prucalopride plus 2 L Polyethylene Glycol regimen|Drug: 2 mg Placebo plus 2 L Polyethylene Glycol regimen Shandong University|Binzhou People's Hospital|Tai'an People's Hospital|Linyi People's Hospital Phase 4 2016-06-01 2016-05-25
    NCT01864915 Bowel Cleansing|Colon Capsule Completion Times Drug: Prucalopride|Procedure: Colon Capsule Queen's University|Hotel Dieu Hospital|Janssen Inc. Phase 3 2013-06-01 2017-02-14
    NCT02047045 Constipation Procedure: acupuncture|Drug: Prucalopride Guang'anmen Hospital of China Academy of Chinese Medical Sciences|Ministry of Science and Technology of the People麓s Republic of China 2014-04-01 2016-10-05
    NCT01807000 Healthy Drug: Radiolabeled Prucalopride Succinate Shire Phase 1 2013-03-01 2014-08-22
    NCT00596596 Constipation Drug: prucalopride|Drug: prucalopride|Drug: 2 mg prucalopride|Drug: 4 mg prucalopride|Other: Placebo Movetis Phase 2 1996-09-01 2008-05-28
    NCT00488137 Constipation Drug: Prucalopride|Other: Placebo|Drug: Prucalopride Movetis Phase 3 1998-03-01 2013-09-25
    NCT00631813 Constipation Drug: Prucalopride|Drug: Prucalopride|Drug: Prucalopride|Drug: Placebo Movetis Phase 2 1995-11-01 2008-05-28
    NCT02947269 Postoperative Ileus|Colorectal Surgery|Postoperative Complications Drug: Prucalopride|Drug: Placebo Oral Capsule University of Auckland, New Zealand Phase 3 2017-01-01 2016-10-25
    NCT02806206 Gastrointestinal Hemorrhage|Crohn Disease|Celiac Disease|Intestinal Diseases|Inflammatory Bowel Diseases Drug: Prucalopride|Drug: Placebo University of British Columbia Phase 4 2016-07-01 2016-07-13

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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