ノルアドレナリン 化学特性,用途語,生産方法
定義
ノルエピネフリン，あるいはアルテレノールともいう。副腎髄質，クロム親和細胞および交感神経細胞から分泌されて，生体内で神経刺激伝達物質として働いているカテコールアミンの一種。副腎髄質ホルモンであるアドレナリンの前駆質でもある。心筋，睾丸および卵巣ではアドレナリンより多く存在する。血中遊離脂肪酸を上昇させるほか，血圧上昇，中枢神経系の刺激などの作用をする。昇圧剤として臨床面で応用されている。ノルアドレナリンは，アドレナリンの前駆体。血管収縮や血糖量増大などの作用をもつ。交感神経では化学伝達物質として働いている。
解説
ホルモンの一種で，ノルアドレナリンは，ノルエピネフリンnorepinephrineとも呼ぶ。生理活性アミン，カテコールアミンの一種。副腎髄質の腺細胞や神経細胞で生合成される。L‐チロシンからドーパ，ドーパミンを経て合成される。アミノ基へのメチル基転移反応によりアドレナリンを生じる。副腎髄質から分泌されたものはアドレナリンに類似したさまざまの作用をもつ。カテコールアミンノルアドレナリンの植物にも大量に含まれているが，その生理的機能は不明である。株式会社平凡社 世界大百科事典 第２版について 情報
効能
昇圧薬, 血管収縮薬, アドレナリン受容体作動薬
商品名
ノルアドリナリン (アルフレッサファーマ)
化学的特性
solid
使用
Norepinephrine is used for increasing cardiac constriction and for the necessary elevation of blood pressure after sharp decline, which can result from surgical intervention or
trauma.
定義
ChEBI: The R-enantiomer of noradrenaline.
世界保健機関（WHO）
Vasoconstrictor agents have been in use for many years to
prolong duration of action of local anaesthetics, particularly in dentistry.
Combination products containing epinephrine or levarterenol in concentrations of
1:80,000 or less remain widely available. See also WHO comment for epinephrine.
生物学の機能
Most central noradrenergic neurons are located in the
nucleus locus ceruleus of the pons and in neurons of
the reticular formation. Fibers from these nuclei innervate
a large number of cortical, subcortical, and spinomedullary
fields. Many functions have been ascribed to
the central noradrenergic neurons, including a role in affective disorders (see Chapter 33), in learning and
memory, and in sleep–wake cycle regulation.The mammalian
CNS contains both α- and β-adrenoceptors.
一般的な説明
Norepinephrine (NE, Levophed) differs from DA onlyby addition of a 1-OH substituent (β-OH-DA) and from Eonly by lacking the N-methyl group. Like DA, it is polar andrapidly metabolized by both COMT and MAO, resulting inpoor oral bioavailability and short DOA (1 or 2 minutes evenwhen given intravenously). It is a stimulant of α1-, α2-, andβ1-adrenoceptors (notice that lacking the N-methyl group resultsin lacking β2- and β3-activity). It is used to counteractvarious hypotensive crises, because its α-activity raisesblood pressure and as an adjunct treatment in cardiac arrestbecause its β-activity stimulates the heart. It has limitedclinical application caused by the nonselective nature of itsactivities.
危険性
May cause local tissue necrosis, headache,
bradycardia, hypertension; poison; teratogen; mutagen.
薬理学
Norepinephrine is the primary neurotransmitter produced and released by adrenergic neurons, and in literature it is also described as and called () noradrenaline or levarterenol.
This vasopressor catecholamine reduces both the resistance and capacity of blood vessels
by stimulating α-adrenoreceptors and having a direct cardiostimulatory effect, which is
accomplished by activation of β1-adrenoreceptors. Norepinephrine exhibits significantly
less activity than epinephrine as a drug for widening blood vessels through the activation
of β2-adrenoreceptors. Elevation of both stylistic and diastolic blood pressure is a typical
reaction to intravenous introduction of norepinephrine.
安全性プロファイル
Poison by ingestion,
intraperitoneal, subcutaneous, and
intravenous routes. An experimental
teratogen. Experimental reproductive
effects. Human mutation data reported. A
sympathomimetic vasopressor. When heated
to decomposition it emits toxic fumes of
NOx.
純化方法
Recrystallise adrenor from EtOH and store it in the dark under N2. [pKa, Lewis Brit J Pharmacol Chemother 9 488 1954, UV: Bergstr.m et al. Acta Physiol Scand 20 101 1950, Fluorescence: Bowman et al. Science NY 122 32 1955, Tullar J Am Chem Soc 70 2067 1948.] The L-tartrate salt monohydrate has m 102-104.5o, [] D -11o (c 1.6, H2O), after recrystallisation from H2O or EtOH. [Beilstein 13 III 2382.]
ノルアドレナリン 上流と下流の製品情報
原材料
準備製品