ArticleBritish journal of pharmacology1999
In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 86 citations in OpenAlex.
- Evaluation of oral ro70-0004/003, an alpha1A-adrenoceptor antagonist, in the treatment of male erectile dysfunction.International journal of impotence research · 2001Trial
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- Roles for αThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2021Article
- The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D-adrenoceptors.Pharmacology research & perspectives · 2020Article
- A novel postsynaptic signal pathway of sympathetic neural regulation of murine colonic motility.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Norepinephrine Has Dual Effects on Human Colonic Contractions Through Distinct Subtypes of Alpha 1 Adrenoceptors.Cellular and molecular gastroenterology and hepatology · 2020Article
- Isoproterenol acts as a biased agonist of the alpha-1A-adrenoceptor that selectively activates the MAPK/ERK pathway.PloS one · 2015Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Article
- Size-dependent heterogeneity of contractile Ca2+ sensitization in rat arterial smooth muscle.The Journal of physiology · 2012Article
- Phenotype pharmacology of lower urinary tract α(1)-adrenoceptors.British journal of pharmacology · 2012Review
- Adrenoceptor activity of muscarinic toxins identified from mamba venoms.British journal of pharmacology · 2011Article
- Investigation of the distribution and function of alpha-adrenoceptors in the sheep isolated internal anal sphincter.British journal of pharmacology · 2010Article
- Subtypes of functional alpha1-adrenoceptor.Cellular and molecular life sciences : CMLS · 2010Review
- Alpha1A/B-knockout mice explain the native alpha1D-adrenoceptor's role in vasoconstriction and show that its location is independent of the other alpha1-subtypes.British journal of pharmacology · 2009Article
- The alpha 1B/D-adrenoceptor knockout mouse permits isolation of the vascular alpha 1A-adrenoceptor and elucidates its relationship to the other subtypes.British journal of pharmacology · 2009Article
- Characterization of the alpha1-adrenoceptor subtype mediating contractions of the pig internal anal sphincter.British journal of pharmacology · 2008Article
- Role of alpha1-adrenoceptor subtypes in the effects of methylenedioxy methamphetamine (MDMA) on body temperature in the mouse.British journal of pharmacology · 2008Article
- Alpha(1A)-adrenoceptors mediate contractions to phenylephrine in rabbit penile arteries.British journal of pharmacology · 2007Article
- Alpha1-, alpha2- and beta-adrenoceptors in the urinary bladder, urethra and prostate.British journal of pharmacology · 2006Review
Corrections and comments
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Authors and funding
16 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
It has been hypothesized that in patients with benign prostatic hyperplasia, selective antagonism of the alpha1A-adrenoceptor-mediated contraction of lower urinary tract tissues may, via a selective relief of outlet obstruction, lead to an improvement in symptoms. The present study describes the alpha1-adrenoceptor (alpha1-AR) subtype selectivities of two novel alpha1-AR antagonists, Ro 70-0004 (aka RS-100975) and a structurally-related compound RS-100329, and compares them with those of prazosin and tamsulosin. Radioligand binding and second-messenger studies in intact CHO-K1 cells expressing human cloned alpha1A-, alpha1B- and alpha1D-AR showed nanomolar affinity and significant alpha1A-AR subtype selectivity for both Ro 70-0004 (pKi 8.9: 60 and 50 fold selectivity) and RS-100329 (pKi 9.6: 126 and 50 fold selectivity) over the alpha1B- and alpha1D-AR subtypes respectively. In contrast, prazosin and tamsulosin showed little subtype selectivity. Noradrenaline-induced contractions of human lower urinary tract (LUT) tissues or rabbit bladder neck were competitively antagonized by Ro 70-0004 (pA2 8.8 and 8.9), RS-100329 (pA2 9.2 and 9.2), tamsulosin (pA2 10.4 and 9.8) and prazosin (pA2 8.7 and 8.3 respectively). Affinity estimates for tamsulosin and prazosin in antagonizing alpha1-AR-mediated contractions of human renal artery (HRA) and rat aorta (RA) were similar to those observed in LUT tissues, whereas Ro 70-0004 and RS-100329 were approximately 100 fold less potent (pA2 values of 6.8/6.8 and 7.3/7.9 in HRA/RA respectively). The alpha1A-AR subtype selectivity of Ro 70-0004 and RS-100329, demonstrated in both cloned and native systems, should allow for an evaluation of the clinical utility of a 'uroselective' agent for the treatment of symptoms associated with benign prostatic hyperplasia.
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