Dabuzalgron (hydrochloride)

Dabuzalgron is a partial agonist of the α_1A-adrenergic receptor (α_1A-AR).¹ It selectively binds to α_1A-ARs over α_1B- and α_1D-ARs in CHO-K1 cells expressing the recombinant human receptors (K_is = 0.041, 1.6, and 6.5 µM, respectively) and selectively induces inositol phosphate accumulation in α_1A-AR-expressing CHO-K1 cells over those expressing α_1B- or α_1D-ARs (EC₅₀s = 0.204, >100, and >100 µM, respectively). Dabuzalgron induces urethral tension in rabbit bladder neck preparations (EC₅₀ = 0.363 µM). Intravenous administration of dabuzalgron increases intraurethral pressure and diastolic arterial pressure in anesthetized micropigs (ED₅₀s = 41 and 36 µg/kg, respectively). Dabuzalgron (300 µg/kg) increases urethral tension but does not affect diastolic arterial pressure or heart rate in conscious micropigs. Oral administration of dabuzalgron (10 µg/kg) decreases cardiac fibrosis and prevents decreases in heart rate and fractional shortening induced by doxorubicin (Item No. 15007) in a mouse model of cardiotoxicity.²

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1. Blue, D.R., Daniels, D.V., Gever, J.R., et al. Pharmacological characteristics of Ro 115-1240, a selective α1A/1L-adrenoceptor partial agonist: A potential therapy for stress urinary incontinence. BJU Int. 93(1), 162-170 (2004).

2. Beak, J., Huang, W., Parker, J.S., et al. An oral selective alpha-1A adrenergic receptor agonist prevents doxorubicin cardiotoxicity. JACC Basic Transl. Sci. 2(1), 39-53 (2017).