基本情報
- CAS
65-29-2- 標準SMILES
CC[N+](CC)(CC)CCOc1cccc(OCC[N+](CC)(CC)CC)c1OCC[N+](CC)(CC)CC.[I-].[I-].[I-]- InChIKey
REEUVFCVXKWOFE-UHFFFAOYSA-K- 分子式
- C30H60I3N3O3
- 平均分子量
- 891.5 g/mol
- 単同位体質量
- 891.1769
概要
A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
名称と識別子
- 優先名称
- Gallamine Triethiodide
- IUPAC
- 2-[2,3-bis[2-(triethylazaniumyl)ethoxy]phenoxy]ethyl-triethylazanium triiodide
- 現地名
- ガラミントリエチオダイド
- 英語名
- Gallamine triethiodide
- 分子式
- C30H60I3N3O3
- 分子量
- 891.53
名称と別名
GALLAMINE TRIETHIODIDE65-29-2FlaxedilBenzcurine iodideRemyolanSyncurarineRelaxanSincurarineRetensinTricuranGallaminii iodidumGallamine-3ETI
名称をさらに表示
シンクラリンベンズクリンヨージドレミヨラン1,2,3-トリス{2'-(トリエチルアンモニウム)エトキシ}ベンゼントリアイオダイド2,2',2''-[(1,2,3-ベンゼントリイル)トリス(オキシ)]トリス[N,N,N-トリエチルエタンアミニウム]·トリヨージドパレキシルトリエトヨウ化ガラミンガラフレックスレテンシンフラキセジルフィロラキソンミオワズGガラミントリエチオジドガラミントリエトヨージドレラキサンフラセジルガラミントリエチオダイドgallaminef2559rp3697gallaminflacedil
Gallamine triiodoethylateFourneau 2559Gallamine iodideGallamina triodoetilatoGallamini triethiodidumTriethiodure de gallamineGallamin triethiodideGallamone triethiodide
物性
構造計算による物性
- 極性表面積
- 27.7 Ų
- 水素結合供与体数
- 0
- 水素結合受容体数
- 6
- 回転可能結合数
- 21
- 重原子数
- 39
- 形式電荷
- 0
- 複雑度
- 489
実験および物理化学的性質
OdorODORLESS
Color/Form
WHITE AMORPHOUS POWDER
White crystals from acetone/water
Solubility
Soluble
Freely sol in water, alcohol, dil acetone; sparingly sol in anhyd acetone, ether, benzene, chloroform
Very soluble in water and ethanol; slightly soluble in ethyl ether and acetone.
Human Drugs
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
DecompositionWhen heated to decomposition it emits very toxic fumes of ammonia, nitroxides, and iodine.
Melting Point
152-153
147.5 °C
Other Experimental PropertiesHYGROSCOPIC
物理化学的性質
- 融点
- 235 °C · 235 °C (dec.) (lit.)
- 比重(密度)
- 1.4288 · 1.4288 (estimate)
- 貯蔵温度
- 2 · 2-8°C
- 溶解性
安全と法規制
安全情報は参考情報です。供給元の安全データシート（SDS）、適用法令、専門家による評価に代わるものではありません。
GHS分類
GHS Classification
Warning
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 39 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
危険有害性情報
Regulatory InformationEthanaminium, 2,2',2''-[1,2,3-benzenetriyltris(oxy)]tris[N,N,N-triethyl-, triiodide: Does not have an individual approval but may be used under an appropriate group standard
Other Safety InformationIMAP assessments - Ethanaminium, 2,2',2''-[1,2,3-benzenetriyltris(oxy)]tris[N,N,N-triethyl-, triiodide: Human health tier I assessment
FDA Requirements
Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).
Hazard Classes and CategoriesAcute Tox. 4 (100%)
安全と保護具
Disposal Methods
SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.
化学と産業
薬理情報
Pharmacodynamics
Gallamine Triethiodide is a nondepolarizing neuromuscular blocking drug (NDMRD) used as an adjunct to anesthesia to induce skeletal muscle relaxation. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. Muscle groups differ in their sensitivity to these types of relaxants with ocular muscles (controlling eyelids) being most sensitive, followed by the muscles of the neck, jaw, limbs and then abdomen. The diaphragm is the least sensitive muscle to NDMRDs. Although the nondepolarizing neuromuscular blocking drugs do not have the same adverse effects as succinylcholine, their onset of action is slower. They also have a longer duration of action, making them more suitable for maintaining neuromuscular relaxation during major surgical procedures.
Mechanism of Action
It competes with acetylcholine (ACh) molecules and binds to muscarinic acetylcholine receptors on the post-synaptic membrane of the motor endplate. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. It blocks the action of ACh and prevents activation of the muscle contraction process. It can also act on nicotinic presynaptic acetylcholine receptors which inhibits the release of ACh.
GALLAMINE TRIETHIODIDE...PRODUCES SKELETAL MUSCLE RELAXATION BY COMBINING WITH RECEPTOR SITE AT NEUROMUSCULAR JUNCTION & BLOCKING ACTION OF NEUROTRANSMITTER ACETYLCHOLINE.
IN RAT PHRENIC NERVE-DIAPHRAGM GALLAMINE HAD NO SIGNIFICANT EFFECTS ON ELECTROGENIC PROPERTIES OF EXCITABLE MEMBRANES OF MOTOR NERVE TERMINALS & MUSCLE FIBERS; IT DEPRESSED RESPONSE OF POSTSYNAPTIC RECEPTORS TO ACTION OF ACETYLCHOLINE.
AT NEUROMUSCULAR JUNCTIONS IN MICE AND FROGS, FOLLOWING STEP CHANGES OF MEMBRANE POTENTIAL FROM -70 TO -130 MV, GALLAMINE (5 UMOL) IN THE PRESENCE OF ACETYLCHOLINE (3 UMOL) CAUSED AN INITIAL RAPID DECR IN CURRENT FOLLOWED BY OPENING OF CHANNELS AT A SLOWER RATE THAN WITH ACETYLCHOLINE ALONE. WHEN THE INTERNAL POTENTIAL WAS REDUCED TO -70 MV, THERE WAS A RAPID INCR IN CURRENT AT FIRST, FOLLOWED BY THE USUAL DECR WHICH WAS AGAIN SLOWER THAN NORMAL. THUS, GALLAMINE MAY PRODUCE A POTENTIAL-DEPENDENT BLOCK OF OPEN ION CHANNELS.
Biological Half-Life135 minutes /From table/
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