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Protriptyline hydrochloride Sale

(Synonyms: 盐酸普罗替林) 目录号 : GC30856

A tricyclic antidepressant

Protriptyline hydrochloride Chemical Structure

Cas No.:1225-55-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥297.00
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5mg
¥270.00
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10mg
¥450.00
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25mg
¥990.00
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50mg
¥1,710.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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)

Chemical Properties

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
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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
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Research Update

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.