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Chemical Structure| 501925-31-1 Chemical Structure| 501925-31-1

Structure of PNU-120596
CAS No.: 501925-31-1

Chemical Structure| 501925-31-1

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PNU-120596 is a a type II positive allosteric modulator of α7 nAChRs with an EC50 of 0.2 μM.

Synonyms: NSC 216666

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Product Details of PNU-120596

CAS No. :501925-31-1
Formula : C13H14ClN3O4
M.W : 311.72
SMILES Code : O=C(NC1=CC(Cl)=C(C=C1OC)OC)NC2=NOC(C)=C2
Synonyms :
NSC 216666
MDL No. :MFCD00095313
InChI Key :CEIIEALEIHQDBX-UHFFFAOYSA-N
Pubchem ID :311434

Safety of PNU-120596

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • nAChR

    α7 nAChR, EC50:216 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Hippocampal CA1 interneurons 1 μM 3 h PNU-120596 did not significantly delay COGD-induced depolarization/injury of hippocampal CA1 interneurons. PMC3753841
Hippocampal CA1 pyramidal neurons 1 μM 3 h PNU-120596 significantly delayed anoxic depolarization/injury of hippocampal CA1 pyramidal neurons subjected to COGD. PMC3753841
Human chromaffin cells 10 µM Potentiated the nicotinic current and exocytosis elicited by ACh PMC3312488
Bosc-23 cells 10 µM To investigate the potentiation of α7 acetylcholine receptor single-channel currents by PNU-120596, results showed that PNU-120596 significantly enhanced the open time of the channels in the presence of calcium. PMC11335256

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Middle cerebral artery occlusion (MCAO) model Subcutaneous and intravenous 30 mg/kg (s.c.), 1 mg/kg (i.v.) Single dose, 3 h pre-MCAO and 30 min post-MCAO PNU-120596 significantly reduced the cortical/subcortical infarct volume when administered 3 h pre-MCAO and 30 min post-MCAO. PMC3753841
Rats MCAO model Intravenous (i.v.) and subcutaneous (s.c.) 2.3 mg/kg (i.v.), 11.1 mg/kg (s.c.1), 5.5 mg/kg (s.c.2-3) I.v. at 90 minutes, s.c.1 at 5 hours, s.c.2 at 24 hours, s.c.3 at 48 hours, lasting for 72 hours To test the therapeutic efficacy of PNU-120596 in the MCAO model, results showed that extending treatment duration enhances the therapeutic efficacy of PNU-120596 and reduces relapses PMC6218269
Mice Chronic Intermittent Ethanol model Intraperitoneal injection 3 or 8 mg/kg Single dose To evaluate the effect of PNU-120596 on the Ro 61-8048-induced reduction in ethanol consumption, results showed that PNU-120596 prevented the Ro 61-8048-induced decrease in ethanol consumption and preference. PMC9314579
Mice Carrageenan-induced inflammatory pain model and chronic constriction injury (CCI) neuropathic pain model Intraperitoneal injection 1, 2, 4, 8 mg/kg Single injection, lasting up to 6 hours PNU-120596 significantly reduced carrageenan-induced thermal hyperalgesia and edema, and exhibited long-lasting anti-hyperalgesic and anti-allodynic effects in the CCI model. PMC3521074
Rats Young rats and aged cognitively-impaired rats Intraperitoneal injection 0.1–10 mg/kg Single administration To evaluate the effects of PNU-120596 on memory task performance, which was not significant when administered alone but was effective in combination with a subthreshold dose of donepezil. PMC3562411
Sprague Dawley rats Cognitive impairment model Intraperitoneal injection 3 mg/kg Twice a week for 5 weeks PNU-120596 reversed scopolamine-induced cognitive impairment and restored memory function to normal levels. PMC3640667

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.04mL

3.21mL

1.60mL

32.08mL

6.42mL

3.21mL

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

References

 

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