ドキセピン塩酸塩（異性体混合物） 化学特性,用途語,生産方法
外観
白色〜ほとんど白色, 結晶〜粉末
溶解性
水に溶ける。
用途
三環系抗うつ作用化合物です。 モノアミン神経伝達物質再取り込み阻害作用 を示します。
用途
三環系抗うつ作用化合物です。
モノアミン神経伝達物質再取り込み阻害作用
を示します。
効能
抗うつ薬, ヒスタミン受容体拮抗薬, セロトニン・ノルアドレナリン再取り込み阻害薬
説明
Doxepin is a tricyclic antidepressant that binds to the serotonin (5-HT) transporter (SERT) and norepinephrine transporter (NET; K
ds = 68 and 29.5 nM, respectively). It is a histamine H
1 receptor antagonist (K
i = 1.23 nM). Doxepin selectively binds to SERT and NET over the dopamine transporter (DAT; K
d = 12,100 nM) and inhibits histamine H
1 over H
2, H
3, and H
4 receptors (K
is = 170, 39,810, and 15,135 nM, respectively). It also binds to the 5-HT
2 receptor, as well as to muscarinic acetylcholine and α
1-adrenergic receptors (α
1-ARs; K
ds = 27, 23, and 23.5 nM, respectively). Doxepin (10 mg/kg, i.p.) decreases allodynia and hyperalgesia in a mouse model of chronic constriction injury-induced neuropathic pain. It increases the distance traveled in the center of the open field test and reduces immobility time in the forced swim test in a mouse model of depression induced by chronic stress when administered orally at a dose of 15 mg/kg. Formulations containing doxepin have been used in the treatment of depression and insomnia.
化学的特性
White Solid
使用
Doxepin hydrochloride is a tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.It is a antidepressant used clinically to treat anxiety and depression.
適応症
Doxepin (Sinequan, Adapin) is a tricyclic antidepressant with potent H1
and H2 antagonistic effects. It also has antimuscarinic, antiserotonic, and
anti-α-adrenergic activity. Use of 10 to 50 mg PO t.i.d. to q.i.d. has been
shown to be effective in the treatment of primary acquired, chronic idiopathic
urticaria, idiopathic cold urticaria, and for patients with anxiety or depression
associated with their urticaria. Sedation and dry mouth are the most common
side effects. Doxepin may interact with other drugs that are metabolized by the cytochrome P-450 system (ketoconazole, itraconazole, erythromycin,
clarithromycin, etc.).
一般的な説明
Doxepin, 3-dibenz[b,e]-oxepin-11(6H)ylidine-N,N-dimethyl-1-propanamine hydrochloride, N,N-dimethyl-3-(dibenz[b,e]oxepin-11(6H)-ylidene)propylamine (Sinequan, Adapin), isan oxa congener of amitriptyline, as can be seen from itsstructure.
The oxygen is interestingly placed and should influenceoxidative metabolism as well as postsynaptic and presynapticbinding affinities. The (Z)-isomer is the more active, althoughthe drug is marketed as the mixture of isomers. Thedrug overall is a NE and 5-HT reuptake blocker with significantanticholinergic and sedative properties. It can be anticipatedthat the nor- or des- metabolite will contribute to theoverall activity pattern.
ドキセピン塩酸塩（異性体混合物） 上流と下流の製品情報
原材料
ブチルリチウム
ジメチルアミン
トリフェニルホスフィン
臭化水素酸
10-Chloro-10, 11-dihydro-dibenz(b,f)thiepin
Benzoic acid, 2-(phenoxymethyl)-, methyl ester
11-(3-Bromopropylidene)-6,11-dihydrodibenzo[b,e]oxepine
Dibenz[b,e]oxepin-11-ol, 11-[3-(1,1-dimethylethoxy)propyl]-6,11-dihydro-
2-(ヒドロキシメチル)安息香酸
2-フェノキシメチル安息香酸
(E)-11-(3-chloropropylidene)-6,11-dihydrodibenzo[b,e]oxepine
CHLORO[3-(DIMETHYLAMINO)PROPYL]MAGNESIUM
ジベンゾ[b,e]オキセピン-11(6H)-オン
フェノール
2-(クロロメチル)安息香酸メチル
フタリド
o-フタルアルデヒド
準備製品