囊泡单胺转运蛋白 2 (VMAT2) 被丝氨酸抑制。大鼠纹状体中多巴胺 D1 受体的密度受丝氨酸显着影响 (F2,12=8.81, p<0.01)。急性和慢性利血平戒断不会改变多巴胺 D1 和 D2 受体的亲和力 (Kd) [1]。利血平给药一天后，JB6 P+和HepG2-C8细胞中的IC50值分别为43.9和54.9 μM。在5至50μM的浓度范围内，丝氨酸以剂量依赖性方式刺激荧光素酶活性；在低于 5 μM 的剂量下没有观察到明显的诱导。结果表明，利血平（2.5 至 10 μM）还可增强 Nrf2、HO-1 和 NQO1 蛋白表达。处理 7 天后，JB6 P+ 细胞中 DNMT1、DNMT3a 和 DNMT3b mRNA 表达被浓度范围为 2.5 至 10 μM 的丝氨酸以浓度依赖性方式降低。当用10 μM利血平处理时，DNMT3a的表达显着不同（p<0.05）[2]。

利血平可用于动物建模以开发胃肠道模型。

Absorption, Distribution and Excretion
Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.
In man, after oral admin of 0.25 mg (3)H-reserpine, tritium was rapidly absorbed into the blood, reaching a peak within 1-2 hr. Radioactivity was tightly bound to red blood cells and remained constant over a 96 hr period. ... Six percent of the dose was excreted in the urine by 24 hr, mainly as trimethoxybenzoic acid; but radioactivity was still detectable in plasma, urine, and feces 11-12 days after drug admin.
PARENTERAL ADMIN OF RESERPINE PRODUCES GREATER CONCN IN NEONATAL RAT BRAIN THAN IN ADULT ANIMALS ... PARALLELED BY GREATER DEPLETION OF NOREPINEPHRINE IN INFANT THAN IN ADULT BRAIN. THIS MAY BE DUE TO LESSER CAPACITY OF RAT NEONATES TO METABOLIZE RESERPINE ... MIGHT ALSO EXPLAIN HIGHER PLASMA & TISSUE LEVELS IN HUMAN ADULTS.
RESERPINE LEAVES BLOOD WITHIN FEW MIN AFTER IV INJECTION & ACCUMULATES IN FATTY TISSUES ... MAX CONCN IN 4-6 HR. LIVER ALSO ACCUMULATES RESERPINE. MOST OF SINGLE DOSE HAS LEFT FAT & LIVER IN 48 HR. BRAIN RETAINS ... RESERPINE & ... METABOLITES ... 5 DAYS AFTER SINGLE DOSE.
... CLAIMED TO BE ADEQUATELY ABSORBED FROM GI TRACT, BUT DIFFERENCE IN EFFICACY OF ORAL & IV DOSES RAISES DOUBTS ABOUT ADEQUACY OF ABSORPTION. ... HAS LONG LATENCY OF ONSET & PROLONGED DURATION OF ACTION.
For more Absorption, Distribution and Excretion (Complete) data for RESERPINE (8 total), please visit the HSDB record page.

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Metabolism / Metabolites
YIELDS 3,4,5-TRIMETHOXYBENZOIC ACID IN RAT, CAT, MOUSE;
YIELDS METHYL RESERPATE IN RAT, CAT;
IDENTIFIED METABOLIC PRODUCTS ARE RESERPIC ACID, SYRINGIC ACID, & SYRINGOYL METHYL RESERPATE.
In rats, orally administered reserpine is rapidly hydrolysed to methyl reserpate; and in mice, orally or intravenously administered reserpine is metabolized to trimethoxybenzoic acid. In rats, methyl reserpate appears to be formed in the intestinal mucosa. Trimethoxybenzoic acid is rapidly eliminated in the urine of mice.

Route of Elimination: Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.

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Biological Half-Life
In man, after oral /dose/ of 0.25 mg (3)H-reserpine ... disappearance of radioactivity in plasma was biphasic: first component had half-life of 4.5 hr, and the second, 271 hr.

Hepatotoxicity
Serum aminotransferase elevations during reserpine therapy are uncommon, but specific rates of such elevations in comparison to placebo treatment have not been reported. Despite many decades of use, reserpine has been implicated in few instances of clinically apparent acute liver injury, and none of them were particularly convincing. Published cases were marked by jaundice and abdominal pain arising a year after starting reserpine, but in combination with other known hepatotoxic agents (dihydrazine, phenobarbital, quinidine). The few cases that have been reported were self-limiting and resolved within a few months of stopping therapy. The last case of suspected reserpine associated liver injury was published more than 50 years ago.
Likelihood score: E (unlikely cause of clinically apparent liver injury).

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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Because no information is available on the use of reserpine during breastfeeding and it might adversely affect the breastfed infant, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
◉ Effects in Breastfed Infants
Although not well documented, reserpine is said to cause nasal stuffiness and increased tracheobronchial secretions in breastfed infants.
◉ Effects on Lactation and Breastmilk
Reserpine has reportedly caused galactorrhea and has been used to increase breastmilk production, although it is obsolete for this use.

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Protein Binding
62%

[1]. 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.

[2]. 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.

[3]. 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.

[4]. Reserpine-induced gastric ulcers: protection by lysosomal stabilization due to zinc. Eur J Pharmacol. 1980 Feb;61(4):347-53.

[5]. 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.

[6]. Mechanism of ulcerogenic activity of reserpine in albino rats. Eur J Pharmacol. 1974 Jul;27(2):269-71.

[7]. Antidepressant-Like Effects of Gyejibokryeong-hwan in a Mouse Model of Reserpine-Induced Depression. Biomed Res Int. 2018 Jun 26;2018:5845491.

[8]. 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.

Reserpine can cause cancer according to California Labor Code.
Reserpine appears as white or cream to slightly yellow crystals or crystalline powder. Odorless with a bitter taste. (NTP, 1992)
Reserpine is an alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. It has a role as an antihypertensive agent, a first generation antipsychotic, an adrenergic uptake inhibitor, an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor, an environmental contaminant, a xenobiotic and a plant metabolite. It is an alkaloid ester, a methyl ester and a yohimban alkaloid. It is functionally related to a reserpic acid.
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use. The FDA withdrew its approval for the use of all oral dosage form drug products containing more than 1 mg of reserpine.
Reserpine is a Catecholamine-depleting Sympatholytic. The physiologic effect of reserpine is by means of Decreased Sympathetic Activity.
Reserpine is an oral antihypertensive medication that acts through inhibitor of alpha-adrenergic transmission and was one of the first antihypertensive agents introduced into clinical practice. Despite widescale use for many years, reserpine has not been shown to cause clinically apparent liver injury.
Reserpine has been reported in Rauvolfia yunnanensis, Rauvolfia serpentina, and other organisms with data available.
Reserpine is an alkaloid, derived from the roots of Rauwolfia serpentine and vomitoria, and an adrenergic uptake inhibitor with antihypertensive effects. Reserpine is lipid soluble and can penetrate blood-brain barrier. This agent binds and inhibits catecholamine pump on the storage vesicles in central and peripheral adrenergic neurons, thereby inhibiting the uptake of norepinephrine, dopamine serotonin into presynaptic storage vesicles. This results in catecholamines and serotonin lingering in the cytoplasm where they are destroyed by intraneuronal monoamine oxidase, thereby causing the depletion of catecholamine and serotonin stores in central and peripheral nerve terminals. Depletion results in a lack of active transmitter discharge from nerve endings upon nerve depolarization, and consequently leads to a decreased heart rate and decreased arterial blood pressure as well as sedative effects.
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
See also: Chlorothiazide; reserpine (component of); Reserpine hydrochloride (is active moiety of); Hydroflumethiazide; reserpine (component of) ... View More ...

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Drug Indication
For the treatment of hypertension

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Mechanism of Action
Reserpine's mechanism of action is through inhibition of the ATP/Mg²⁺ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
... DEPLETES OR RELEASES SEROTONIN (5-HYDROXYTRYPTAMINE), DOPAMINE ... NOREPINEPHRINE FROM ... BRAIN & ... BODY ... DEFICIENCY OF DOPAMINE IN BRAIN ... IN STRIATUM, SUBSTANTIA NIGRA ... PALLIDUM. ... HYPOTHERMIC EFFECT ... RELATED TO SEROTONIN DEPLETION OF HYPOTHALAMIC REGION. HYPOTHALMUS CONTAINS ... HIGHEST CONCN OF SEROTONIN. ...
ANTIHYPERTENSIVE ACTION ... DERIVES FROM ADRENERGIC NEURONAL BLOCKADE CONSEQUENT TO DEPLETION OF CATECHOLAMINE-CONTAINING GRANULES OF POSTGANGLIONIC SYMPATHETIC NEURON. MECHANISM OF CENTRAL EFFECTS IS UNKNOWN. IT DEPLETES BOTH BRAIN SEROTONIN & CATECHOLAMINES.
... REPORTED TO INHIBIT GROWTH OF LEUKEMIA IN L1210 CELLS IN MALE MICE ... AND TO SUPPRESS GROWTH OF SARCOMA 37 IN MICE. ... RESERPINE DID NOT AFFECT GROWTH OF TRANSPLANTED MAMMARY ADENOCARCINOMAS IN C3H MICE. IT BLOCKS RELEASE OF PROLACTIN-INHIBITING FACTOR & THUS RAISES SERUM PROLACTIN LEVELS.
Peripheral-Acting Adrenergic Antagonist /from table/
For more Mechanism of Action (Complete) data for RESERPINE (8 total), please visit the HSDB record page.

608.273

50-55-5

Reserpine hydrochloride;16994-56-2;Reserpine-d9;84759-11-5

5770

White to light yellow solid powder

1.3±0.1 g/cm3

700.1±60.0 °C at 760 mmHg

265ºC (dec.)

377.2±32.9 °C

0.0±2.2 mmHg at 25°C

1.620

4.05

117.78

1

10

10

44

1000

6

O(C([H])([H])[H])[C@@]1([H])[C@@]([H])(C([H])([H])[C@]2([H])C([H])([H])N3C([H])([H])C([H])([H])C4C5C([H])=C([H])C(=C([H])C=5N([H])C=4[C@@]3([H])C([H])([H])[C@]2([H])[C@]1([H])C(=O)OC([H])([H])[H])OC([H])([H])[H])OC(C1C([H])=C(C(=C(C=1[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])=O

QEVHRUUCFGRFIF-MDEJGZGSSA-N

InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1

methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-(3,4,5-trimethoxybenzoyl)oxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate

SerpasilReserpine Serpalan Reserpine phosphateRaudixin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~25 mg/mL (~41.07 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (4.11 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (4.11 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。