Target Validation Information
TTD ID T81183
Target Name Adrenergic receptor Alpha-1 (ADRA1)
Type of Target
Successful
Drug Potency against Target Carvedilol Drug Info Ki = 0.4 nM [2]
Prazosin Drug Info pKi = 6.11 [1]
Tamsulosin Drug Info pKi = 9.13 [4]
Action against Disease Model Tamsulosin Drug Info IC50 on tension responses to electrical field stimulation (0.3 ms duration, 80 V and 20 Hz) in h uMan hyperplastic prostate: 0.193nM [3]
References
REF 1 Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes. Curr Top Med Chem. 2007;7(2):163-86.
REF 2 Recent advances in identification and characterization of beta-adrenoceptor agonists and antagonists. Curr Top Med Chem. 2007;7(2):207-16.
REF 3 Inhibition by tamsulosin of tension responses of human hyperplastic prostate to electrical field stimulation. Eur J Pharmacol. 1996 Jun 3;305(1-3):177-80.
REF 4 Tamsulosin: assessment of affinity of 3H-prazosin bindings to two alpha1-adrenoceptor subtypes (alpha1H and alpha1L) in bovine prostate and rat heart and brain. Gen Pharmacol. 1998 Oct;31(4):597-600.

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