2. Neuronal Signaling
  3. Cholinesterase (ChE) Amyloid-β
  4. Protriptyline

Protriptyline is a potent tricyclic antidepressant (TCA). Protriptyline inhibits AChE activity with an IC50 value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline can be used for the study of depression and Alzheimers disease.

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Protriptyline

Protriptyline Chemical Structure

CAS No. : 438-60-8

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AChE BChE

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Description

Protriptyline is a potent tricyclic antidepressant (TCA). Protriptyline inhibits AChE activity with an IC50 value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline can be used for the study of depression and Alzheimers disease[1][2][3].

IC50 & Target[1]

AChE

0.06 mM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.0017 μM
Compound: Protriptyline
Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting
Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting
[PMID: 22420844]
CHO IC50
2.8 nM
Compound: Protriptyline
Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells
Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells
[PMID: 26988801]
CHO IC50
2.8 x 10-9 M
Compound: Protriptyline
Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
HCC1954 EC50
> 10 μM
Compound: Protriptyline
Antiproliferative activity against human HCC1954 cells assessed as cell viability incubated for 72 hrs Alamar blue assay
Antiproliferative activity against human HCC1954 cells assessed as cell viability incubated for 72 hrs Alamar blue assay
[PMID: 31757681]
HCC1954 EC50
> 10 μM
Compound: Protriptyline
Induction of morphological changes in human HCC1954 cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
Induction of morphological changes in human HCC1954 cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
[PMID: 31757681]
T47D EC50
7.7 μM
Compound: Protriptyline
Induction of morphological changes in human T47D cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
Induction of morphological changes in human T47D cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method
[PMID: 31757681]
T47D EC50
> 10 μM
Compound: Protriptyline
Antiproliferative activity against human T47D cells assessed as cell viability incubated for 72 hrs Alamar blue assay
Antiproliferative activity against human T47D cells assessed as cell viability incubated for 72 hrs Alamar blue assay
[PMID: 31757681]
In Vitro

Protriptyline (0-70 μM; 24 hours; PC3 cells) causes cytotoxicity in PC3 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Protriptyline Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: PC3 cells
Concentration: 50, 60 and 70 μM
Incubation Time: 24 hours
Result: Decreased cell viability in a concentration-dependent manner.
In Vivo

Protriptyline (10 mg/kg; i.p.; for 21 days; rat model of AD) improves spatial learning and retention memory in STZ treated rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat model of AD[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; for 21 days.
Result: Reduced pTau, Aβ42 and BACE-1 levels, neurodegeneration, oxidative stress and glial activation. Improved p-ERK/ERK ratio and enhanced BDNF and CREB levels by reducing NFκB and GFAP expression.
Clinical Trial
Molecular Weight

263.38

Formula

C19H21N
CAS No.
SMILES

CNCCCC1C2=CC=CC=C2C=CC3=CC=CC=C13
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Protriptyline Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Protriptyline438-60-8Cholinesterase (ChE)Amyloid-ββ-amyloid peptideAβAbetaalzheimersAβ Self-AssemblyAChEInhibitorinhibitorinhibit

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