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
名称をさらに表示
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
- 形式電荷
- 0
- 複雑度
- 354
実験および物理化学的性質
LogP
1.1
1.49
Human Drugs
Breast Feeding; Lactation; Milk, Human; Adrenergic Beta-Antagonists; Antiglaucoma Agents
Pharmaceuticals
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
化学と産業
薬理情報
ATC Code
S01ED05
C - Cardiovascular system
S - Sensory organs
QS - Sensory organs
QC - Cardiovascular system
Pharmacodynamics
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
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.
FDA Pharmacological Classification
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
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
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).
上流・下流製品情報
上流原料
サプライヤー9 社
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