In vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M. Cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM In vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs. Cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis.
|Formulation||10% gelatin solution|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
High-resolution manometric evaluation of the effects of cisapride and metoclopramide hydrochloride administered orally on lower esophageal sphincter pressure in awake dogs.
Kempf J, et al. Am J Vet Res. 2014 Apr;75(4):361-6. PMID: 24669921.
Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride.
Matsunaga Y, et.al. J Pharmacol Exp Ther. 2011 Mar;336(3):791-800. PMID: 21123674.
|Related 5-HT Receptor Products|
|Ziprasidone HCl monohydrate
Ziprasidone(CP88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.
Venlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.