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编 号：F743010
分子式：C15H13ClN4O
分子量：300.74
分子式：C15H13ClN4O
分子量：300.74
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CAS No: 1191908-24-3
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生物活性：
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.
体内研究：
ADRA1D receptor antagonist 1 (free base) (10 μg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats.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.Animal Model:Rats with cyclophosphamide-induced cystitis.
Dosage:10 μg/kg
Administration:Oral administration; single
Result:Increased voiding intervals.
Animal Model:Rats with BOO (bladder outlet obstruction).
Dosage:4.4 μg/kg
Administration:Intravenous injection; single
Result:Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.
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.
体内研究：
ADRA1D receptor antagonist 1 (free base) (10 μg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats.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.Animal Model:Rats with cyclophosphamide-induced cystitis.
Dosage:10 μg/kg
Administration:Oral administration; single
Result:Increased voiding intervals.
Animal Model:Rats with BOO (bladder outlet obstruction).
Dosage:4.4 μg/kg
Administration:Intravenous injection; single
Result:Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.
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