| Identification | Back Directory | [Name]
reserpine hydrochloride | [CAS]
16994-56-2 | [Synonyms]
Reserpine HCl
reserpine hydrochloride | [EINECS(EC#)]
241-074-6 | [Molecular Formula]
C33H41ClN2O9 | [MDL Number]
MFCD23379918 | [MOL File]
16994-56-2.mol | [Molecular Weight]
645.14 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
≥25 mg/mL in DMSO; insoluble in H2O; ≥2.74 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). | [Biological Activity]
reserpine hydrochloride (serpalan) is an indole alkaloid antipsychotic and antihypertensive drug that irreversibly blocks the vesicular monoamine transporter (vmat). | [in vivo]
Reserpine can be used in animal modeling to create gastrointestinal ulcer and depression models. Withdrawal from chronic (14 days) but not acute reserpine (48 hours) significantly decreases immobility time (F2,18=3.68, p<0.05) and increases climbing time (F2,18=4.48, p<0.02) in rats, without altering swimming time in the forced swim test (FST) (F2,18=1.78; NS) compared to control animals. A dose of 5 mg/kg body weight of Reserpine significantly increases the urinary excretion of vanillylmandelic acid (VMA). Animals treated with Reserpine excrete more 5-hydroxyindoleacetic acid (5-HIAA) than controls. Reserpine treatment results in dose-dependent hypotension. Compared to controls, doses of 0.5, 1, 5, 10, and 15 μg/kg of Reserpine significantly (p<0.01) reduce blood pressure[1][3].
Induction of Gastric Ulcer[4][5][6] Background
Peripheral cholinergic and adrenergic mechanisms are involved in the ulceration induced by reserpine. The ulcerogenic activity of reserpine was significantly reduced by α-adrenoceptor antagonists (phenoxybenzamine (HY-B0431) and phentolamine (HY-12717)) but not by the β-adrenoceptor blocker, propranolol (HY-B0573B)[6].
Specific Modeling Methods
Rat: Wistar Rats ? male ? 200-290 g[4]
Administration: 5 mg/kg ? ip ? 18 h before sacrifice
Mice: ICR mice ? male ? 7 weeks old[5]
Administration: 10 mg/kg ? ip ? once daily for 3 days
Note
(1)Rats were fasted with water ad libitum for 48 h prior to experimentation. Rats were housed and experiments were conducted in a temperature-controlled room (23 ± 1°C).
(2)The level of cancer induction was identified by specific biochemical markers such as serum gastrin level, TBARS, and glutathione followed by histopathological analysis at two-time periods for 8 and 16 week.
Modeling Indicators Individual phenotypic changes: induced marked gastric glandular ulceration and elicited the release of free /~-glucuronidase from lysosomes in the gastric mucosa.
Molecular changes: In the reserpine-induced gastric ulcer control mice, the gastric secretion volume was increased, the pH value (1.04) was decreased, the serum cytokine levels of IL-6, IL-12, TNF-α and IFN-γ was increased.
Correlated Product(s): / Opposite Product(s): /
Induction of Depression[7][8] Background
Reserpine is an irreversible inhibitor of vesicular monoamine transporter 2, which regulates the accumulation of monoamines into the synaptic vesicles and their reuptake from the synapses. Therefore, Reserpine inhibits monoamine pre-synaptic reuptake and storage, leading to monoamine depletion and depressive disorders[7].
Specific Modeling Methods
Rat: Wistar Rats ? male ? 120-150 g[7]
Administration: 0.5 mg/kg ? ip ? once per day for 14 days
Mice: C57BL/6 mice ? male ? 7 weeks old[8]
Administration: 0.5 mg/kg ? ip ? once per day for 10 days
Note
(1) Reserpine was diluted in glacial acetic acid to a final concentration of 0.5% acetic acid in distilled water.
Modeling Indicators Individual phenotypic changes: showed a significant decrease in spontaneous locomotor activity in the activity cage, decrease in latency to immobility, and increase in the immobility duration in forced swimming test (FST), indicating motor impairment and worsened depressive phenotype.
Molecular changes: Reserpine administration significantly increased cortical contents of MDA (malondialdehyde), reduced GSH (glutathione), increased TNF-ɑ and reduced BDNF (brain derived neurotropic factor). Showed a significant decrease in cortical nor-epinephrine (NE), serotonin (5-HT), and dopamine (DA)
Correlated Product(s): / Opposite Product(s): / | [storage]
4°C, protect from light | [References]
[1] Antkiewicz-Michaluk L, et al. Withdrawal from repeated administration of a low dose of reserpine induced opposing adaptive changes in the noradrenaline and serotonin system function: a behavioral and neurochemical ex vivo and in vivo studies in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Mar 3;57:146-54. DOI:10.1016/j.pnpbp.2014.10.009
[2] Hong B, et al. Reserpine Inhibit the JB6 P+ Cell Transformation Through Epigenetic Reactivation of Nrf2-Mediated Anti-oxidative Stress Pathway. AAPS J. 2016 May;18(3):659-69. DOI:10.1208/s12248-016-9901-6
[3] Sreemantula S, et al. Reserpine methonitrate, a novel quaternary analogue of reserpine augments urinary excretion of VMA and 5-HIAA without affecting HVA in rats. BMC Pharmacol. 2004 Nov 16;4:30. DOI:10.1186/1471-2210-4-30
[4] Pfeiffer CJ, et al. Reserpine-induced gastric ulcers: protection by lysosomal stabilization due to zinc. Eur J Pharmacol. 1980 Feb;61(4):347-53. DOI:10.1016/0014-2999(80)90073-4
[5] Li GJ, et al. Preventive Effect of Polysaccharide of Larimichthys crocea Swim Bladder on Reserpine Induced Gastric Ulcer in ICR Mice. Korean J Physiol Pharmacol. 2014 Apr;18(2):183-90. DOI:10.4196/kjpp.2014.18.2.183
[6] Gupta MB, et al. Mechanism of ulcerogenic activity of reserpine in albino rats. Eur J Pharmacol. 1974 Jul;27(2):269-71. DOI:10.1016/0014-2999(74)90159-9
[7] Park BK, et al. Antidepressant-Like Effects of Gyejibokryeong-hwan in a Mouse Model of Reserpine-Induced Depression. Biomed Res Int. 2018 Jun 26;2018:5845491. DOI:10.1155/2018/5845491
[8] El-Marasy SA, et al. Anti-depressant effect of cerebrolysin in reserpine-induced depression in rats: Behavioral, biochemical, molecular and immunohistochemical evidence. Chem Biol Interact. 2021 Jan 25;334:109329. DOI:10.1016/j.cbi.2020.109329 |
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