ADRA1D receptor antagonist 1 free base

ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

ADRA1D receptor antagonist 1 (free base) (10 µg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats[1]. ADRA1D receptor antagonist 1 (free base) (4.4 µg/kg; i.v.; single) inhibits bladder contraction with an IC 30 value of 15 nM in rats[1]. Animal Model: Rats with cyclophosphamide-induced cystitis[1]. Dosage: 10 µg/kg Administration: Oral administration; single Result: Increased voiding intervals. Animal Model: Rats with BOO (bladder outlet obstruction)[1]. Dosage: 4.4 µg/kg Administration: Intravenous injection; single Result: Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.