カルテオロール

Carteolol

HCID 2583

基本情報

CAS
51781-06-7
標準SMILES
CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2
InChIKey
LWAFSWPYPHEXKX-UHFFFAOYSA-N
分子式
C16H24N2O3
平均分子量
292.37 g/mol
単同位体質量
292.17869263

概要

Carteolol is a quinolone and a secondary alcohol. It has a role as a beta-adrenergic antagonist, an antihypertensive agent, an anti-arrhythmia drug, an antiglaucoma drug and a sympatholytic agent. It is a conjugate base of a carteolol(1+).

名称と識別子

優先名称
Carteolol
IUPAC
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
現地名
カルテオロール
英語名
Carteolol
分子式
C16H24N2O3
分子量
292.37

名称と別名

CARTEOLOL51781-06-7Carteololum8NF31401XG2(1H)-Quinolinone, 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-3,4-dihydro-CHEBI:3437DTXSID30227465-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydroquinolin-2-onecarteololo5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2-ol5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2-ol5-(3-(tert-butylamino)-2-hydroxypropoxy)-1,2,3,4-tetrahydroquinolin-2-one
名称をさらに表示
5-(2-ヒドロキシ-3-tert-ブチルアミノプロポキシ)-3,4-ジヒドロ-2(1H)-キノロン5-[[(S)-3-(tert-ブチルアミノ)-2-ヒドロキシプロピル]オキシ]-3,4-ジヒドロキノリン-2(1H)-オン(-)-カルテオロール5-[3-(tert-ブチルアミノ)-2-ヒドロキシプロポキシ]-3,4-ジヒドロカルボスチリル5-[3-(tert-ブチルアミノ)-2-ヒドロキシプロポキシ]-3,4-ジヒドロキノリン-2(1H)-オンカルテオロール(+)-カルテオロール5-[3-[(1,1-ジメチルエチル)アミノ]-2-ヒドロキシプロポキシ]-3,4-ジヒドロキノリン-2(1H)-オン5-[[(R)-3-(tert-ブチルアミノ)-2-ヒドロキシプロピル]オキシ]-3,4-ジヒドロキノリン-2(1H)-オン5-[3-(tert-ブチルアミノ)-2-ヒドロキシプロポキシ]-1,2,3,4-テトラヒドロキノリン-2-オン5-[(2S)-3-(tert-ブチルアミノ)-2-ヒドロキシプロポキシ]-1,2,3,4-テトラヒドロキノリン-2-オン5-[(2R)-3-(tert-ブチルアミノ)-2-ヒドロキシプロポキシ]-1,2,3,4-テトラヒドロキノリン-2-オンC06874dl-CarteololCarteolol USP/EP/BPCarteolol Impurities1808Carteolol (base and/or unspecified salts)5-[3-(tert-Butylamino)-2-hydroxypropoxy]-3,4-dihydrocarbostyril5-(2-Hydroxy-3-tert-butylaminopropoxy)-3,4-dihydro-2(1H)-quinolone5-[3-(tert-Butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one
RefChem:58563DTXCID202746C07AA15S01ED05Carteololum [INN-Latin]5-(3-(tert-Butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-oneCarteolol (INN)

データベース識別子

CAS
51781-06-7
PubChem CID
2583
DTXSID
DTXSID3022746
ChEMBL
CHEMBL839
ChEBI
CHEBI:3437
UNII
8NF31401XG
Nikkaji
J13.087G

物性

構造計算による物性

XLogP
1
極性表面積
70.6 Ų
水素結合供与体数
3
水素結合受容体数
4
回転可能結合数
6
重原子数
21

実験および物理化学的性質

LogP · 2 件

1.1

1.49

Solubility4.21e-01 g/L
Human Drugs · 2 件

Breast Feeding; Lactation; Milk, Human; Adrenergic Beta-Antagonists; Antiglaucoma Agents

Pharmaceuticals

Physical DescriptionSolid

物理化学的性質

沸点
434.3 °C · 434.3°C (rough estimate)
比重(密度)
1.0574 · 1.0574 (rough estimate)
屈折率
1.58 · 1.5800 (estimate)
酸解離定数(Pka)
13.84 · 13.84±0.20(Predicted)
CAS データベース
51781 · 51781-06-7

安全と法規制

毒性情報

Effects During Pregnancy and Lactation◉ Summary of Use during Lactation

化学と産業

薬理情報

ATC Code · 5 件

S01ED05

C - Cardiovascular system

S - Sensory organs

QS - Sensory organs

QC - Cardiovascular system

Pharmacodynamics · 1 件

Carteolol is a beta1 and beta2 (non-selective) adrenergic receptor-blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Carteolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Carteolol reduces intraocular pressure with little or no effect on pupil size or accommodation in contrast to the miosis which cholinergic agents are known to produce.

Mechanism of Action · 1 件

The primary mechanism of the ocular hypotensive action of carteolol in reducing intraocular pressure is most likely a decrease in aqueous humor production. This process is initiated by the non-selective beta1 and beta2 adrenergic receptor blockade.

Metabolism/MetabolitesHepatic.
FDA Pharmacological Classification · 5 件

8NF31401XG

CARTEOLOL

Mechanisms of Action [MoA] - Adrenergic beta-Antagonists

Established Pharmacologic Class [EPC] - beta-Adrenergic Blocker

Carteolol is a beta-Adrenergic Blocker. The mechanism of action of carteolol is as an Adrenergic beta-Antagonist.

MeSH Pharmacological Classification · 4 件

Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.

Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade.

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.

Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.

用途と製造

Use ClassificationPharmaceuticals

応用分野

用途β受容体遮断薬(Ⅱ群薬)抗不整脈薬

使用Antiadrenergic (β-receptor).

サプライヤー9 社

北京华美互利生物化工010-56205725 · [email protected]
銳迪國際科技有限公司18024082417 · [email protected]
南京生利德生物科技有限公司025-57798810 18652991625 · [email protected]
南京伶亚生物医药科技有限公司18068075658 · [email protected]
深圳市华信医药科技有限公司15671363360 · [email protected]

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