Protriptyline Hydrochloride

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Cat Number

API0231626

CAS Number

1225-55-4

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Product Detail Description Scientific Support Customer Q&A

CAS Number

1225-55-4

EINECS

214-956-3

Storage

Store at room temperature

Synonyms

Protriptyline HCl; Concordin; Maximed; Triptil hydrochloride; MK-240; NSC-169912; DTXSID8046951

Molecular Formula

C19H22ClN

Molecular Weight

299.8

Smiles

CNCCCC1C2=CC=CC=C2C=CC3=CC=CC=C13.Cl

Appearance

White to off-white powder

Boiling Point

407.7℃ at 760 mmHg

Relative Density

1.026

General Description

Protriptyline hydrochloride is a secondary amine tricyclic antidepressant with activating properties, unlike the sedating effects of other TCAs. It is one of the least sedating agents in its class. The drug has a long half-life and is typically dosed once or twice daily.

Mechanism of Action

Protriptyline potently inhibits norepinephrine reuptake at the presynaptic terminal, with weaker inhibition of serotonin reuptake. This increases noradrenergic transmission in the brain, improving energy, motivation, and mood. The drug also blocks histamine H1, muscarinic cholinergic, and alpha-1 adrenergic receptors, though to a lesser extent than amitriptyline. Its activating effect is attributed to minimal histamine blockade.

Application

Protriptyline is indicated for major depressive disorder, particularly in patients with psychomotor retardation, apathy, or anergy. It is also used off-label for narcolepsy (to reduce cataplexy and excessive daytime sleepiness) and for attention-deficit/hyperactivity disorder (ADHD) in children.

Screening 140 FDA‑approved nervous system drugs using docking studies against acetylcholinesterase, β‑secretase (BACE‑1), and amyloid β aggregation identified the tricyclic antidepressant protriptyline as a potent inhibitor of all three targets. Biophysical assays, kinetics, molecular dynamics simulations, and atomic force microscopy confirmed strong inhibitory activity. Protriptyline also inhibited glycation‑induced amyloid aggregation. The authors conclude that protriptyline is a promising multi‑target directed ligand for Alzheimer’s disease and warrants further investigation.

Fig. 1 Protriptyline inhibits AChE activity. (Bansode SB, et al., 2014)

References

Bansode SB, et al. Molecular investigations of protriptyline as a multi-target directed ligand in Alzheimer's disease. PLoS One. 2014;9(8):e105196.

Does Protriptyline Hydrochloride require protection from light during storage?

Yes, it is photosensitive. Prolonged light exposure can cause discoloration and degradation of the dibenzocycloheptene ring. Store in light-resistant containers.

What is the recommended storage temperature for Protriptyline Hydrochloride?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate oxidative degradation.

Is Protriptyline Hydrochloride hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity, it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity dibenzosuberone monitored during stability?

This oxidative degradation product is quantified using a stability-indicating HPLC method, ensuring it remains below USP limits.