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Article: AF-2364 [1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide] is a potential male contraceptive: A review of recent data

TitleAF-2364 [1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide] is a potential male contraceptive: A review of recent data
Authors
Keywords1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide
Adherens junction
AF-2364
Junction dynamics
Male contraceptive
Sertoli-germ cell interactions
Testis
Issue Date2005
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/contraception
Citation
Contraception, 2005, v. 72 n. 4, p. 251-261 How to Cite?
AbstractEarlier studies have shown that 1-(2,4-dichlorobenzyl)-1H-indazole-3- carbohydrazide (AF-2364) is a potential male contraceptive when administered orally to adult Sprague-Dawley rats. This compound induces reversible germ cell loss from the seminiferous epithelium by disrupting cell adhesion function between Sertoli and germ cells, in particular, elongating/elongate/round spermatids and spermatocytes but not spermatogonia. Thus, this event is accompanied by a transient loss of fertility in treated rats. Once the drug is metabolically cleared, the remaining spermatogonia can begin repopulating the epithelium, and fertility bounces back. In this review, we summarize recent findings regarding the possible use of this drug for male contraception and its mechanism of action in the rat testis. We also provide an update on the efficacy results of using different treatment regimens in adult rats where AF-2364 was administered by gavage vs. intraperitoneal and intramuscular administration. These results have clearly indicated that AF-2364 is indeed a reversible male contraceptive. Furthermore, the tissue distribution in multiple organs and biological fluids using [3H]-AF-2364 is also reviewed. These data have clearly illustrated the low bioavailability of AF-2364 in rats and that this compound is not specifically taken up by any organs including the testis or the epididymis. These summaries are helpful to investigators in the field who seek to understand the molecular mechanism of action of AF-2364 in the rat testis and to explore its possible use for male contraception. © 2005 Elsevier Inc. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/84861
ISSN
2015 Impact Factor: 2.788
2015 SCImago Journal Rankings: 1.557
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorCheng, CYen_HK
dc.contributor.authorMruk, Den_HK
dc.contributor.authorSilvestrini, Ben_HK
dc.contributor.authorBonanomi, Men_HK
dc.contributor.authorWong, CHen_HK
dc.contributor.authorSiu, MKYen_HK
dc.contributor.authorLee, NPYen_HK
dc.contributor.authorLui, WYen_HK
dc.contributor.authorMo, MYen_HK
dc.date.accessioned2010-09-06T08:57:58Z-
dc.date.available2010-09-06T08:57:58Z-
dc.date.issued2005en_HK
dc.identifier.citationContraception, 2005, v. 72 n. 4, p. 251-261en_HK
dc.identifier.issn0010-7824en_HK
dc.identifier.urihttp://hdl.handle.net/10722/84861-
dc.description.abstractEarlier studies have shown that 1-(2,4-dichlorobenzyl)-1H-indazole-3- carbohydrazide (AF-2364) is a potential male contraceptive when administered orally to adult Sprague-Dawley rats. This compound induces reversible germ cell loss from the seminiferous epithelium by disrupting cell adhesion function between Sertoli and germ cells, in particular, elongating/elongate/round spermatids and spermatocytes but not spermatogonia. Thus, this event is accompanied by a transient loss of fertility in treated rats. Once the drug is metabolically cleared, the remaining spermatogonia can begin repopulating the epithelium, and fertility bounces back. In this review, we summarize recent findings regarding the possible use of this drug for male contraception and its mechanism of action in the rat testis. We also provide an update on the efficacy results of using different treatment regimens in adult rats where AF-2364 was administered by gavage vs. intraperitoneal and intramuscular administration. These results have clearly indicated that AF-2364 is indeed a reversible male contraceptive. Furthermore, the tissue distribution in multiple organs and biological fluids using [3H]-AF-2364 is also reviewed. These data have clearly illustrated the low bioavailability of AF-2364 in rats and that this compound is not specifically taken up by any organs including the testis or the epididymis. These summaries are helpful to investigators in the field who seek to understand the molecular mechanism of action of AF-2364 in the rat testis and to explore its possible use for male contraception. © 2005 Elsevier Inc. All rights reserved.en_HK
dc.languageengen_HK
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/contraceptionen_HK
dc.relation.ispartofContraceptionen_HK
dc.rightsContraception . Copyright © Elsevier Inc.en_HK
dc.subject1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazideen_HK
dc.subjectAdherens junctionen_HK
dc.subjectAF-2364en_HK
dc.subjectJunction dynamicsen_HK
dc.subjectMale contraceptiveen_HK
dc.subjectSertoli-germ cell interactionsen_HK
dc.subjectTestisen_HK
dc.titleAF-2364 [1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide] is a potential male contraceptive: A review of recent dataen_HK
dc.typeArticleen_HK
dc.identifier.openurlhttp://library.hku.hk:4550/resserv?sid=HKU:IR&issn=0010-7824&volume=72&issue=4&spage=251&epage=261&date=2005&atitle=AF-2364+[1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide]+is+a+potential+male+contraceptive:+a+review+of+recent+dataen_HK
dc.identifier.emailSiu, MKY: mkysiu@hkucc.hku.hken_HK
dc.identifier.emailLee, NPY: nikkilee@hku.hken_HK
dc.identifier.emailLui, WY: wylui@hku.hken_HK
dc.identifier.authoritySiu, MKY=rp00275en_HK
dc.identifier.authorityLee, NPY=rp00263en_HK
dc.identifier.authorityLui, WY=rp00756en_HK
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.contraception.2005.03.008en_HK
dc.identifier.pmid16181968en_HK
dc.identifier.scopuseid_2-s2.0-23844478817en_HK
dc.identifier.hkuros118909en_HK
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-23844478817&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume72en_HK
dc.identifier.issue4en_HK
dc.identifier.spage251en_HK
dc.identifier.epage261en_HK
dc.identifier.isiWOS:000232543300003-
dc.publisher.placeUnited Statesen_HK
dc.identifier.scopusauthoridCheng, CY=7404797787en_HK
dc.identifier.scopusauthoridMruk, D=6701823934en_HK
dc.identifier.scopusauthoridSilvestrini, B=7006825900en_HK
dc.identifier.scopusauthoridBonanomi, M=8839441200en_HK
dc.identifier.scopusauthoridWong, CH=8849630400en_HK
dc.identifier.scopusauthoridSiu, MKY=24924018400en_HK
dc.identifier.scopusauthoridLee, NPY=7402722690en_HK
dc.identifier.scopusauthoridLui, WY=35220192400en_HK
dc.identifier.scopusauthoridMo, MY=7006857340en_HK

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