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Vol. 83, No. 6, 2009
Issue release date: June 2009
Section title: Original Paper
Pharmacology 2009;83:367–378
(DOI:10.1159/000218739)

Bladder-Relaxant Properties of the Novel Benzofuroindole Analogue LDD175

dela Peña I.C.a · Yoon S.Y.a · Kim S.M.a · Lee G.S.a · Ryu J.H.b · Park C.-S.c · Kim Y.C.c · Cheong J.H.a
aDepartment of Pharmacology, Sahmyook University, Seoul, bDepartment of Oriental Pharmaceutical Science, Kyunghee University, Seoul, and cDepartment of Life Science, Gwangju Institute of Science and Technology, Gwangju, Korea

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Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 10/6/2008
Accepted: 2/20/2009
Published online: 5/18/2009
Issue release date: June 2009

Number of Print Pages: 12
Number of Figures: 10
Number of Tables: 1

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA

Abstract

The present study describes the bladder-relaxant properties of LDD175 (4-chloro-7-trifluoromethyl-10H-benzo[4,5]furo [3,2-b]indole-1-carboxylic acid), a novel benzofuroindole compound. LDD175 had no significant effect on the spontaneous and electrically evoked bladder contractions, but produced concentration-dependent relaxation in strips precontracted by 1 μmol/l acetylcholine (pEC50 = 5.9 ± 0.2, Emax = 90.3 ± 2.6%; 100 μmol/l, n = 6). In high K+- (20 and 80 mmol/l) stimulated samples, LDD175 caused a concentration-dependent relaxant activity which was significant in 20 mmol/l K+ (pEC50 = 5.6 ± 0.2, Emax = 63.1 ± 4.8%, n = 6), but not in 80 mmol/l K+ (pEC50 = 5.1 ± 0.3, Emax = 12.7 ± 2.5%, n = 6). Iberiotoxin (100 nmol/l), a specific BKCa blocker, attenuated the compound’s relaxative effect (vehicle = 65.7 ± 9.2% vs. iberiotoxin 28.0 ± 3.5%, respectively, n = 3), but not tetraethylammonium chloride (10 mmol/l), a nonselective K+ channel blocker, barium chloride (10 mmol/l), a conventional KIR blocker, and glibenclamide (1 mmol/l), a KATP blocker. LDD175 was evaluated in both endothelium-intact and denuded rat aorta contracted with high K+. In these preparations, LDD175 did not produce significant inhibition. Administered intravenously to conscious restrained rats, LDD175 (10 mg/kg) did not alter the rat’s hemodynamic activity (i.e. blood pressure and heart rate). When tested in the spontaneously hypertensive rats (SHR) for its influence on their voiding behavior, LDD175 (5 and 10 mg/kg) significantly reduced voiding frequency and lengthened void intervals of the animals. These observations: (1) reveal the BKCa channel potentiation of LDD175; (2) support previous claims concerning the bladder (vs. vascular) selectivity of benzofuroindole compounds; (3) demonstrate the efficacy of LDD175 in the animal model of bladder overactivity (SHR). Therefore, the compound may be potentially useful in the treatment of bladder overactivity.

© 2009 S. Karger AG, Basel


  

Author Contacts

Dr. Jae Hoon Cheong
College of Pharmacy, Sahmyook University
26-21 Kongkreung-dong, Nowongu
Seoul 139-742 (Korea)
Tel. +82 2339 1605, Fax +82 2339 1617, E-Mail cheongjh@syu.ac.kr

  

Article Information

Received: October 6, 2008
Accepted: February 20, 2009
Published online: May 18, 2009
Number of Print Pages : 12
Number of Figures : 10, Number of Tables : 1, Number of References : 54

  

Publication Details

Pharmacology (International Journal of Experimental and Clinical Pharmacology)

Vol. 83, No. 6, Year 2009 (Cover Date: June 2009)

Journal Editor: Donnerer J. (Graz), Billingsley M.L. (Hershey, Pa.), Maeyama K. (Matsuyama)
ISSN: 0031-7012 (Print), eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA


Article / Publication Details

First-Page Preview
Abstract of Original Paper

Received: 10/6/2008
Accepted: 2/20/2009
Published online: 5/18/2009
Issue release date: June 2009

Number of Print Pages: 12
Number of Figures: 10
Number of Tables: 1

ISSN: 0031-7012 (Print)
eISSN: 1423-0313 (Online)

For additional information: http://www.karger.com/PHA


Copyright / Drug Dosage

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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in goverment regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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