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Chemical Structure| 14919-77-8 Chemical Structure| 14919-77-8

Structure of Benserazide HCI
CAS No.: 14919-77-8

Chemical Structure| 14919-77-8

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Benserazide HCl is a aromatic L-amino acid decarboxylase (AAAD) or DOPA decarboxylase inhibitor.

Synonyms: Serazide; Ro 4-4602; Benserazide(hydrochloride)

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Product Details of Benserazide HCI

CAS No. :14919-77-8
Formula : C10H16ClN3O5
M.W : 293.70
SMILES Code : NC(CO)C(NNCC1=CC=C(O)C(O)=C1O)=O.Cl
Synonyms :
Serazide; Ro 4-4602; Benserazide(hydrochloride)
MDL No. :MFCD00078571
InChI Key :ULFCBIUXQQYDEI-UHFFFAOYSA-N
Pubchem ID :26964

Safety of Benserazide HCI

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • decarboxylase

In Vitro:

Cell Line
Concentration Treated Time Description References
LoVo 3 μM, 10 μM, 30 μM, 100 μM 48 hours Did not inhibit LoVo cell proliferation Pharmacol Res. 2016 Nov;113(Pt A):18-37.
HT29 3 μM, 10 μM, 30 μM, 100 μM 48 hours Inhibited HT29 cell proliferation, cytotoxic at 100 μM Pharmacol Res. 2016 Nov;113(Pt A):18-37.
HCT116 10 μM, 30 μM, 100 μM 48 hours Inhibited HCT116 cell proliferation, completely at 30 μM Pharmacol Res. 2016 Nov;113(Pt A):18-37.
Enterococcus faecalis 1.5 mM 24 hours To evaluate the inhibitory effects of human AADC inhibitors on PEA production in En. faecalis. Benserazide significantly inhibited PEA production in En. faecalis. Gut Microbes. 2022 Jan-Dec;14(1):2128605.
LO2 cells 0-500 μM 48 hours Evaluate the cytotoxicity of Benserazide on LO2 cells, showing IC50 value >500 μM J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
HCT116 cells 0-500 μM 48 hours Evaluate the cytotoxicity of Benserazide on HCT116 cells, showing IC50 value of 181.4 ± 11.5 μM J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
SW480 cells 0-500 μM 48 hours Evaluate the cytotoxicity of Benserazide on SW480 cells, showing IC50 value of 143.0 ± 7.0 μM J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
CB-17/SCID mice SW480 cells xenograft model Intraperitoneal injection 300 and 600 mg/kg Once daily for 16 days Evaluate the inhibitory effect of Benserazide on tumor growth, showing significant suppression at 300 and 600 mg/Kg doses, reducing tumor size and weight by 30.1% and 60.3% respectively J Exp Clin Cancer Res. 2017 Apr 20;36(1):58.
Nude mice Human colon cancer cell xenograft model Subcutaneous injection 50 mg/kg/day Once daily for the duration of the experiment Prevented tumor growth Pharmacol Res. 2016 Nov;113(Pt A):18-37.
Mice Mouse pain models Intraperitoneal (i.p.) or intracerebroventricular (i.c.v.) injection 1 mg/kg (i.p.) or 25 μg/mouse (i.c.v.) Single administration To investigate the effect of benserazide on L-DOPS-induced antinociception. Results showed that systemic benserazide (i.p.) did not affect the antinociceptive effect of L-DOPS, while i.c.v. benserazide significantly suppressed the antinociceptive effect of L-DOPS. Br J Pharmacol. 1994 Feb;111(2):503-8
Mice Parkinsonian mouse model Subcutaneous injection 15 mg/kg Once daily for 2 weeks To inhibit the breakdown of L-dopa in the periphery and evaluate its effect on abnormal involuntary movements (AIMs). Results showed that AIMs developed similarly in α6(-/-) and wildtype mice with combined L-dopa and benserazide treatment, but declined to ~50% in α6(-/-) mice with continued treatment. Neuropharmacology. 2012 Sep;63(3):450-9
Rat Healthy rats Intraperitoneal injection 15 mg/kg bodyweight Single dose, PET scans performed 1 hour after injection To evaluate the impact of peripheral aromatic L-amino acid decarboxylase (AADC) inhibition on brain uptake. Results showed that brain uptake of 3-L-[18F]FPhe was significantly increased with benserazide pretreatment, while 3-D-[18F]FPhe was unaffected. Cancers (Basel). 2021 Nov 30;13(23):6030
Mice 6-hydroxydopamine (6-OHDA)-induced hemiparkinsonian model Intraperitoneal injection 12 mg/kg Once daily for 10 days To evaluate the effect of Benserazide in combination with L-DOPA on dyskinesia in a Parkinson's disease mouse model. Results showed that Benserazide combined with L-DOPA alleviated dyskinetic symptoms. J Neurosci. 2012 Apr 25;32(17):5900-10

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

17.02mL

3.40mL

1.70mL

34.05mL

6.81mL

3.40mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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