An α1-adrenergic receptor antagonist (pA2 = 6.73-8.15 in various blood vessels from dog

Naftopidil (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
1164469-60-6
Storage:
-20
UN-No:
Non-Hazardous - /

Naftopidil is an α1-adrenergic receptor antagonist that competitively inhibits α-adrenoceptor-mediated contractions induced by noradrenaline with pA2 values of 6.73-8.15 in various blood vessels from dog, rabbit, guinea pig, and rat.{33266} It binds to the cloned human α1-adrenergic receptors with Ki values of 3.7, 20, and 1.2 nM for α1A, α1B and α1D, respectively.{33264} Clinical formulations of naftopidil are used in the treatment of benign prostatic hyperplasia in Japan.{33264} Naftopidil also exhibits antiproliferative activity, inhibiting the growth of androgen-sensitive LNcaP cells and androgen-insensitive PC-3 cancer cell lines with IC50 values of 22.2 and 33.2 µM, respectively.{33265}  

 

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Description

An α1-adrenergic receptor antagonist (pA2 = 6.73-8.15 in various blood vessels from dog, rabbit, guinea pig, and rat); binds to the cloned human α1-adrenergic receptors (Kis= 3.7, 20, and 1.2 nM for α1A, α1B and α1D, respectively); used clinically in the treatment of benign prostatic hyperplasia in Japan; inhibits growth of LNcaP cells and PC-3 cells (IC50s = 22.2 and 33.2 µM, respectively)

Formal name: 4-(2-methoxyphenyl)-α-[(1-naphthalenyloxy)methyl]-1-piperazineethanol, monohydrochloride

Synonyms: 

Molecular weight: 429

CAS: 1164469-60-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Cardiovascular System|Vasculature|Vasodilation

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