1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. Glycine Receptor (GlyR) 5-HT Receptor
  3. PSN09

PSN09 is a blood-brain barrier-permeable agonist of PSAM4-GlyR and PSAM4-5-HT3 receptors with high affinity. 18F-labeled PSN09 serves as a radiotracer for PET imaging in non-human primates.

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PSN09

PSN09 Chemical Structure

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Description

PSN09 is a blood-brain barrier-permeable agonist of PSAM4-GlyR and PSAM4-5-HT3 receptors with high affinity. 18F-labeled PSN09 serves as a radiotracer for PET imaging in non-human primates[1].

IC50 & Target[1]

5-HT3 Receptor

 

In Vitro

PSN09 potently binds to PSAM4-GlyR in transfected HEK-293 cells, with a Ki of 1.86 nM[1].
PSN09 potently binds to PSAM4-5-HT3 in transfected HEK-293 cells, with a Ki value of 5.67 nM[1].
PSN09 (0.1-100 μM) potently activates PSAM4-GlyR in transfected HEK-293 cells, with an EC50 of 8.3 nM[1].
PSN09 (0.1-100 μM) potently activates PSAM4-5-HT3 in transduced HEK-293 cells, with an EC50 of 16.8 nM[1].

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

In Vivo

PSN09 (1 mg/kg; i.v.; single dose) activates PSAM4-GlyR, thereby inducing neuronal inhibition in transduced rhesus monkeys[1].

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

Animal Model: Monkey transduced with PSAM4-GlyR (11-year-old male, Lenti-hSyn-PSAM4-GlyR injected into left amygdala)[1]
Dosage: 1 mg/kg
Administration: i.v.; single dose; administered 10 minutes before [18F]FDG injection
Result: Did not significantly alter [18F]FDG arterial input functions.
Reduced MRGlu in the target transduced left amygdala by 19%, and decreased the target-to-mirror MRGlu ratio by 3%.
Molecular Weight

335.37

Formula

C20H18FN3O

SMILES

FC1=CC=C(C=C1)COC2=NC3=CC4=C(C5CNCC4C5)C=C3N=C2

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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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.

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Product Name:
PSN09
Cat. No.:
HY-181351
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