(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
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Chiu G, Li S, Connolly PJ, Pulito V, Liu J, Middleton SA
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3930-4. Epub 2007 May 3.
- PubMed ID
- 17517507 [ View in PubMed]
- Abstract
Although alpha(1) adrenergic receptor blockers can be very effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS), their usage is limited by CV-related side-effects that are caused by the subtype non-selective nature of the current drugs. To overcome this problem, it was hypothesized that a alpha(1a/1d) subtype selective antagonist would bring more benefit for the therapy of BPH/LUTS. In developing such selective alpha(1a/1d) ligands, a series of (phenylpiperidinyl)cyclohexylsulfonamides has been synthesized and evaluated for binding to three cloned human alpha(1)-adrenergic receptor subtypes. Many compounds showed equal affinity for both alpha(1a) and alpha(1d) subtypes with good selectivity versus the alpha(1b) subtype.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Tamsulosin Alpha-1A adrenergic receptor Ki (nM) 0.19 N/A N/A Details Tamsulosin Alpha-1B adrenergic receptor Ki (nM) 2 N/A N/A Details Tamsulosin Alpha-1D adrenergic receptor Ki (nM) 0.2 N/A N/A Details