Protriptyline hydrochloride
(Synonyms: 盐酸普罗替林) 目录号 : GC30856
A tricyclic antidepressant
Cas No.:1225-55-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Protriptyline is a tricyclic antidepressant.1 It binds to the norepinephrine and serotonin (5-HT) transporters with Kd values of 1.41 and 19.6 nM, respectively. Protriptyline also binds to histamine H1, muscarinic acetylcholine, and α1-adrenergic receptors (Kds = 25, 25, and 130 nM, respectively).2 It inhibits norepinephrine uptake into rat whole brain and hypothalamic synaptosomes (IC50s = 12 and 0.55 μM, respectively) and 5-HT uptake into rat whole brain synaptosomes (IC50 = 5.5 μM).3 Protriptyline (1 mg/kg, i.v.) inhibits food-induced cataplexy in narcoleptic dogs.4 Formulations containing protriptyline have been used in the treatment of depression.
1.Tatsumi, M., Groshan, K., Blakely, R.D., et al.Pharmacological profile of antidepressants and related compounds at human monoamine transportersEur. J. Pharmacol.340(2-3)249-258(1997) 2.Richelson, E., and Nelson, A.Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitroJ. Pharmacol. Exp. Ther.230(1)94-102(1984) 3.Schacht, U., and Heptner, W.Effect of nomifensine (HOE 984), a new antidepressant, on uptake of noradrenaline and serotonin and on release of noradrenaline in rat brain synaptosomesBiochem. Pharmacol.23(24)3413-3422(1974) 4.Foutz, A.S., Delashaw, J.B., Jr., Guilleminault, C., et al.Monoaminergic mechanisms and experimental cataplexyAnn. Neurol.10(4)369-376(1981)
| Cas No. | 1225-55-4 | SDF | |
| 别名 | 盐酸普罗替林 | ||
| Canonical SMILES | CNCCCC1C2=CC=CC=C2C=CC3=CC=CC=C13.[H]Cl | ||
| 分子式 | C19H22ClN | 分子量 | 299.84 |
| 溶解度 | DMSO : ≥ 24 mg/mL (80.04 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3351 mL | 16.6756 mL | 33.3511 mL |
| 5 mM | 0.667 mL | 3.3351 mL | 6.6702 mL |
| 10 mM | 0.3335 mL | 1.6676 mL | 3.3351 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Protriptyline
Protriptyline hydrochloride is a tricyclic antidepressant used to improve mood in people with depression. It is also useful in treating anxiety. It is a more potent antidepressant and has fewer sedative and tranquilizing effects than other TCAs. FDA-approved uses include mental depression, narcolepsy, attention deficit hyperactivity disorder, and headaches. It also has other non-FDA approved indications. This activity outlines the indications, mechanism of action, methods of administration, important adverse effects, contraindications, monitoring, and toxicity of protriptyline, so providers can direct patient therapy in treating conditions for which it is indicated, as part of the interprofessional team.
Protriptyline
Because there is no published experience with protriptyline during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.
Protriptyline
Protriptyline is a tricyclic antidepressant that was previously widely used in the therapy of major depression. Most of the tricyclic antidepressants have been shown to cause a low rate of mild and transient serum enzyme elevations and rare cases of clinically apparent acute cholestatic liver injury. The potential hepatotoxicity specifically of protriptyline, however, has not been well defined.
Protriptyline kinetics
The kinetics of protriptyline were examined in 8 subjects after a single oral dose of 30 mg protriptyline hydrochloride. Peak protriptyline levels ranged from 10.4 to 22.3 ng/ml and were reached 6 to 12 hr after the oral dose. The mean protriptyline half-life (t1/2) was 74.3 hr and ranged from 53.6 to 91.7 hr in individual subjects, confirming the long t1/2 of protriptyline reported by Moody and associates. The estimated first-pass metabolism of protriptyline was relatively small, ranging from 10% to 25% of the oral dose, assuming complete absorption. The mean volume of distribution was 22.5 L/kg and ranged from 15.0 to 31.2 L/kg. No relationship was found between the kinetics of protriptyline and those of doxepin studied previously in 7 of the 8 subjects.
Nedocromil
Because there is no published experience with protriptyline during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.