RS 100329 HCl

Names

[ Name ]:
RS 100329 HCl

[Synonym ]:
2,4(1H,3H)-Pyrimidinedione, 5-methyl-3-[3-[4-[2-(2,2,2-trifluoroethoxy)phenyl]-1-piperazinyl]propyl]-, hydrochloride (1:1)
5-Methyl-3-(3-{4-[2-(2,2,2-trifluoroethoxy)phenyl]-1-piperazinyl}propyl)-2,4(1H,3H)-pyrimidinedione hydrochloride (1:1)
5-Methyl-3-(3-{4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl}propyl)pyrimidine-2,4(1H,3H)-dione hydrochloride (1:1)

Biological Activity

[Description]:

RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia[1][2].

[Related Catalog]:

Research Areas >> Endocrinology

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

[Target]

pKi: 9.6 (α1A-adrenoceptor), 7.9 (α1D-adrenoceptor) and 7.5 (α1B-adrenoceptor)[2]

[In Vitro]

RS100329 hydrochloride (human lower urinary tract (LUT) tissues) contractions to Norepinephrine (HY-13715) is antagonized in a surmountable and concentration-dependent manner[2].

[In Vivo]

RS100329 hydrochloride (0.01-0.1 mg/kg; i.v.; Sprague Dawley rats) reduces baseline urethral pressure and inhibit reflex urethral contractions[1]. Animal Model: Sprague Dawley rats (300-390 g)[1] Dosage: 0.01-0.1 mg/kg Administration: Intravenous injection Result: Caused a fall in baseline urethral pressure reaching a maximum of 23%.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₆ClF₃N₄O₃

[ Molecular Weight ]:
462.894

[ Exact Mass ]:
462.164551

[ Storage condition ]:
-20°C

Related Compounds

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