Гидрохлорид Доксепин химические свойства, назначение, производство
Описание
Doxepin is a tricyclic antidepressant that binds to the serotonin (5-HT) transporter (SERT) and norepinephrine transporter (NET; Kds = 68 and 29.5 nM, respectively). It is a histamine H1 receptor antagonist (Ki = 1.23 nM). Doxepin selectively binds to SERT and NET over the dopamine transporter (DAT; Kd = 12,100 nM) and inhibits histamine H1 over H2, H3, and H4 receptors (Kis = 170, 39,810, and 15,135 nM, respectively). It also binds to the 5-HT2 receptor, as well as to muscarinic acetylcholine and α1-adrenergic receptors (α1-ARs; Kds = 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.
Химические свойства
White Solid
Использование
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.
Показания
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.).
Общее описание
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.
Гидрохлорид Доксепин препаратная продукция и сырье
сырьё
н-Бутиллитий
Диметиламин
Трифенилфосфин
Бромистый водород
10-Хлор-10, 11-дигидро-дибенз(b,f)тиепин
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-(гидроксиметил)бензойная кислота
2 - (феноксиметил) бензойной кислоты
(E)-11-(3-chloropropylidene)-6,11-dihydrodibenzo[b,e]oxepine
ХЛОР[3-(ДИМЕТИЛАМИНО)ПРОПИЛ]МАГНИЙ
Дибенз [b, e] оксепин-11 (6H) -он
Фенол
Methyl 2-chloromethylbenzoate
Фталид
1,2-фталовый дикарбоксальдегид
препарат