미라베그론

한글명:미라베그론

카스 번호223673-61-8

상품명:Mirabegron

CBNumberCB22493967

분자식C21H24N4O2S

포뮬러 무게396.51

MOL 파일223673-61-8.mol

동의어(한글)

미라베그론

화학적 성질

녹는점	138-140°C
끓는 점	690.0±55.0 °C(Predicted)
밀도	1.313
저장 조건	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
용해도	클로로포름(약간 용해됨, 가열), 메탄올(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.51±0.70(Predicted)
색상	흰색에서 연한 노란색
InChIKey	PBAPPPCECJKMCM-IBGZPJMESA-N
SMILES	S1C=C(CC(NC2=CC=C(CCNC[C@H](O)C3=CC=CC=C3)C=C2)=O)N=C1N
CAS 데이터베이스	223673-61-8

그림문자(GHS)

미라베그론 화학적 특성, 용도, 생산

개요
Betanis (Mirabegron) was approved in July 2011 by the Japanese Ministry of Health, Labour, and Welfare for the treatment of urgency, urinary frequency, and urinary urge urinary incontinence associated with overactive bladder (OAB). Mirabegron is synthesized by coupling 4-nitrophenethyl amine to (R)-2-hydroxy-2-phenylacetic acid. The resulting amide is reduced to an amine. The nitro group is then reduced and the resulting aniline is coupled to 2-(2-aminothiazol-4-yl) acetic acid to give mirabegron. Mirabegron has an EC₅₀ of 22 nM (intrinsic activity=0.8) for β3-AR with no detectable activity for β1- andβ2-AR (EC₅₀>10,000 nM). In an anesthetized rat rhythmic bladder contraction model in which bladder contractions are induced by saline, mirabegron at 3 mg/kg iv decreased the frequency of rhythmic bladder contraction without suppressing contraction amplitude. These data suggest that the activation of β3-AR increases bladder capacity without influencing the frequency of bladder contraction.
화학적 성질
White to Off-White Solid
용도
Potent bladder relaxant and reagent for diabetes remedy.;Labeled Mirabegron, intended for use as an internal standard for the quantification of Mirabegron by GC- or LC-mass spectrometry.
정의
ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive ladder syndrome.
Clinical Use
Mirabegron is an orally active β3-adrenoceptor agonist currently in development by Astellas Pharma for the treatment of overactive bladder (OAB). The drug is a nanomolar EC50 antagonist against human β3-AR biochemical assays with good selectivity over b1- and β2-ARs. Mirabegron demonstrates a novel mechanism by targeting the β3-AR for bladder relaxation to help manage OAB symptoms such as increased urinary urgency and frequency and urgency incontinence. However, mirabegron is a cytochrome P450 2D6 inhibitor, and it raises a concern for drug–drug interaction with concomitant administration of other cytochrome P450 2D6 substrates.

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