Imipramine (hydrochloride)
(Synonyms: 盐酸丙咪嗪) 目录号 : GC12885A tricyclic antidepressant
Cas No.:113-52-0
Sample solution is provided at 25 µL, 10mM.
Imipramine (hydrochloride) is a tricyclic antidepressant and is mainly used in the treatment of major depression and enuresis [1].
Antidepressants are antagonists of many neurotransmitter receptors in human brain [3].
Imipramine is the first tricyclic antidepressant that acts mainly as an inhibitor of serotonin and norepinephrine transporters [2]. In radioligand binding assays, imipramine inhibited serotonin and norepinephrine transporters with KD values of 1.4 and 37 nM, respectively [2]. Imipramine is also inhibited histamine H1 receptor, muscarinic acetylcholine receptor and α1-adrenergic receptor with Kd values of 37, 46, and 32 nM, respectively [4].
In rodents, imipramine abolished the depressive syndrome produced by the acute administration of reserpine. Imipramine also possessed central anticholinergic activity and attenuate the activity of the centrally acting muscarinic agents tremorine and oxotremorine. Imipramine inhibited the presynaptic uptake of NA and 5-HT, and relatively weak against DA [1].
References:
[1]. Spencer PS. Review of the pharmacology of existing antidepressants. Br J Clin Pharmacol. 1977;4Suppl 2:57S-68S.
[2]. Tatsumi M, Groshan K, Blakely RD, et al. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58.
[3]. Cusack B, Nelson A, Richelson E. Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65.
Animal experiment: |
Rats: The Wistar (WIS) and Wistar Kyoto (WKY) rats are divided into four groups: (1) a control WIS rat group, (2) an imipramine-treated WIS rat group, (3) a control WKY rat group and (4) an imipramine-treated WKY rat group. Distilled water (10 mL/kg) or imipramine solution (10 mg/10 mL/kg) is orally administered for 28 days except on the day of the open field test, when nothing is administered in order to avoid the acute effect of single administration on the open field test[5]. Mice: C57BL/6 mice subjected to repeated social defeat (RSD), home cage control (HCC) are randomLy selected into four groups: RSD/imipramine, RSD/vehicle, HCC/imipramine, and HCC/vehicle. Mice in the RSD/imipramine received daily intraperitoneal (i.p.) injections of imipramine (20 mg/kg) for 24 days after the 6 cycles of RSD. HCC/imipramine received daily i.p. imipramine at the same dose while RSD/vehicle and HCC/vehicle groups received i.p. injections of vehicle (sodium chloride, 0.9%) for 24 days at the same time point[3]. |
References: [1]. Balkovetz DF, et al. Evidence for an imipramine-sensitive serotonin transporter in human placental brush-border membranes. J Biol Chem. 1989 Feb 5;264(4):2195-8. |
Cas No. | 113-52-0 | SDF | |
别名 | 盐酸丙咪嗪 | ||
化学名 | 10,11-dihydro-N,N-dimethyl-5H-dibenz[b,f]azepine-5-propanamine, monohydrochloride | ||
Canonical SMILES | CN(C)CCCN1C2=C(C=CC=C2)CCC3=C1C=CC=C3.Cl | ||
分子式 | C19H24N2 • HCl | 分子量 | 316.9 |
溶解度 | ≥ 12.5mg/mL in DMSO | 储存条件 | Store at -20°C,protect from light |
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制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1556 mL | 15.7778 mL | 31.5557 mL |
5 mM | 0.6311 mL | 3.1556 mL | 6.3111 mL |
10 mM | 0.3156 mL | 1.5778 mL | 3.1556 mL |
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