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• W2103261380 abstract "No AccessJournal of UrologyCLINICAL UROLOGY: Original Articles1 Jul 2002An Extract From the Bark of Aspidosperma Quebracho Blanco Binds to Human Penile α-Adrenoceptors Herbert Sperling, Annette Lorenz, Susanne Krege, Rainer Arndt, and Martin C. Michel Herbert SperlingHerbert Sperling More articles by this author , Annette LorenzAnnette Lorenz More articles by this author , Susanne KregeSusanne Krege More articles by this author , Rainer ArndtRainer Arndt More articles by this author , and Martin C. MichelMartin C. Michel More articles by this author View All Author Informationhttps://doi.org/10.1016/S0022-5347(05)64852-5AboutFull TextPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail Abstract Purpose: We determined whether an extract from the bark of the tree Aspidosperma quebracho blanco, which is used as a prescription drug to treat erectile dysfunction in some countries, can bind to human penile α1 and α2-adrenoceptors, and cloned human α-adrenoceptor subtypes. Materials and Methods: Competition binding studies were performed with α1 and α2-adrenoceptors with the extract and 4 subfractions prepared from it using [3H]prazosin (New England Nuclear, Dreieich, Germany) and [3H]RX 821002 (2-methoxy-idazoxam) (Amersham, Braunschweig, Germany) as the radioligands, respectively. Results: In a concentration dependent manner the extract inhibited 2-methoxy-idazoxam binding to human penile α2-adrenoceptors. Somewhat less potently it inhibited [3H] prazosin binding to penile α1-adrenoceptors. The extract also inhibited binding to cloned α2-adrenoceptors more potently than to α1-adrenoceptors but did not discriminate among subtypes. Subfraction B was more potent than the others for all cloned α1-adrenoceptor subtypes and much more potent at all penile and all cloned α2-adrenoceptor subtypes. This fraction largely contained yohimbine, whereas the other fractions were devoid of yohimbine. Based on yohimbine competition binding experiments with penile and cloned α1 and α2-adrenoceptors, it appears that the inhibitory effects of the abstract and its subfractions can largely be explained by its yohimbine content. Conclusions: An α-adrenoceptor mediated component of the pro-erectile effects of Aspidosperma quebracho blanco bark extract may predominantly be caused by its yohimbine content. The α-adrenoceptor independent, pro-erectile effects of the extract could not be determined from this study. References 1 : Erectile dysfunction. New Engl J Med2000; 342: 1802. Google Scholar 2 : Oral treatment of erectile dysfunction: from herbal remedies to designer drugs. J Sex Marital Ther1998; 24: 69. Google Scholar 3 : Erfahrungsbericht über Afrodor 2000. Urologe B1991; 31: 24. Google Scholar 4 : Treatment for potency problems with Afrodor 2000. Acta Chir Hung1995; 35: 87. Google Scholar 5 : Secondary erectile dysfunction. Is oral medication in the diagnostic phase indicated? Urologe A1999; 38: 56. Google Scholar 6 : The biochemical and neurologic basis for the treatment of male erectile dysfunction. J Pharmacol Exp Ther2001; 296: 225. Google Scholar 7 : Physiology of penile erection. Physiol Rev1995; 75: 191. Google Scholar 8 : Oral alpha adrenoceptor blockade as a treatment of erectile dysfunction. World J Urol2001; 19: 9. Google Scholar 9 : Alpha-adrenergic receptor blockade by phentolamine increases the efficacy of vasodilators in penile corpus cavernosum. Int J Impot Res2000; 12: S26. Google Scholar 10 : Characterization of α-adrenoceptor subtypes in the corpus cavernosum of patients undergoing sex change surgery. J Urol1999; 162: 1793. Abstract, Google Scholar 11 : Effects of intracavernosal trazodone hydrochloride: animal and human studies. J Urol1990; 144: 1277. Link, Google Scholar 12 : Affinity of trazodone at human penile alpha1- and alpha2-adrenoceptors. BJU Int2000; 85: 959. Google Scholar 13 : Isolation and biological activity of aspidospermine and quebrachamine from an Aspidosperma tree source. J Pharmacol Biomed Anal1994; 12: 1283. Google Scholar 14 : Alpha-adrenoceptor (1) subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells. Biochem Biophys Res Commun2000; 272: 906. Google Scholar 15 : Characterization of alpha2-adrenoceptors mediating contraction of dog saphenous vein: identity with the human alpha 2A subtype. Br J Pharmacol1997; 121: 1721. Google Scholar 16 : Differential alpha1-adrenoceptor labeling by [3H]prazosin and [3H]tamsulosin. Eur J Pharmacol1998; 342: 85. Google Scholar 17 : Comparison of adrenoceptor subtype expression in porcine and human bladder and prostate. Urol Res1997; 25: 199. Google Scholar 18 : Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol1973; 22: 3099. Google Scholar 19 : Saw palmetto extracts potently and noncompetitively inhibit human alpha-adrenoceptors (1) in vitro. Prostate1999; 38: 208. Google Scholar 20 : Yohimbine for erectile dysfunction: a systematic review and meta-analysis of randomized clinical trials. J Urol1998; 159: 433. Link, Google Scholar From the Departments of Urology and Medicine, University of Essen, Essen and Farco-Pharma GmbH, Köln, Germany© 2002 by American Urological Association, Inc.FiguresReferencesRelatedDetails Volume 168Issue 1July 2002Page: 160-163 Advertisement Copyright & Permissions© 2002 by American Urological Association, Inc.Keywordspenisimpotencereceptors, adrenergic, alphaaspidospermayohimbineMetricsAuthor Information Herbert Sperling More articles by this author Annette Lorenz More articles by this author Susanne Krege More articles by this author Rainer Arndt More articles by this author Martin C. Michel More articles by this author Expand All Advertisement PDF downloadLoading ..." @default.
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• W2103261380 title "An Extract From the Bark of Aspidosperma Quebracho Blanco Binds to Human Penile α-Adrenoceptors" @default.
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