GR103545
GR103545 is a κ opioid receptor (KOR) selective PET radiotracer and functional agonist with blood-brain barrier permeability and comparable peripheral and central antinociceptive efficacy, with an IC50 of 0.02 nM for KOR agonistic activity. GR103545 selectively binds to KORs in the brain. GR103545 induces antinociceptive effects. GR103545 can be used in research related to neurological disorders such as depression and Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 126766-42-5
- Formula: C19H25Cl2N3O3
- Molecular Weight:414.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Opioid Receptor Isoforms
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Biological Activity
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κ Opioid Receptor/KOR 0.02 nM (IC50) |
GR103545 (compound 2) (in vitro rabbit vas deferens tissue) acts as potent competitive kappa opioid receptor (KOR) agonist with IC50 = 0.02 nM and Log D = 3.14; its s.c./i.c.v. antinociceptive potency ratio is 1.5, showing strong blood-brain barrier penetration[2].
11C-GR103545 (i.v.; bolus injection) exhibits specific, KOR-selective binding in healthy rhesus monkey brain with high BPND values but slow tissue kinetics that delay equilibrium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 2-4 months of age, ~500 g weight)[1]
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Dosage:~1 mCi
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Administration:i.v.; single bolus injection
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Result:Recorded mean baseline BPND values across KOR-abundant brain nuclei ranging 0.55-0.66.
Found average SUV reductions of 60%, 86% and 77% in KOR-rich brain areas after i.v. pre-treatment with racemic GR103545, naloxone and LY2795050 separately.
Identified dose-dependent BPND suppression by i.v. salvinorin A with a KOR occupancy EC50 of 0.36 mg/kg.
Documented time-variant baseline BPND suppression ratios of 55%, 51%, 60% and 88% at 1 min, 1 h, 2.5 h and 5 h post 0.60 mg/kg i.v. salvinorin A injection.
Chemical Information
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CAS No. 126766-42-5
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Molecular Weight 414.33
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Formula C19H25Cl2N3O3
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SMILES
ClC(C=C1CC(N2[C@@H](CN(CC2)C(OC)=O)CN3CCCC3)=O)=C(C=C1)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Placzek MS, et al. Immediate and Persistent Effects of Salvinorin A on the Kappa Opioid Receptor in Rodents, Monitored In Vivo with PET. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2015 Dec;40(13):2865-72. [Content Brief]
[3]. Li S, et al. Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2019 Jul;60(7):1023-1030. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GR103545 Related Classifications
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