126766-43-6
Chemical Structure
GR103545 fumarate
- CAS No.: 126766-43-6
- Formula:C23H29Cl2N3O7
- Molecular Weight:530.40
IUPAC Name: methyl (R)-4-(2-(3,4-dichlorophenyl)acetyl)-3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate fumarate
InChIKey: ABTNETSDXZBJTE-WMQZXYHMSA-N
SMILES: OC(/C=C/C(O)=O)=O.ClC(C=C1CC(N2[C@@H](CN(CC2)C(OC)=O)CN3CCCC3)=O)=C(C=C1)Cl
Biological Activity: GR103545 fumarate 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 fumarate selectively binds to KORs in the brain. GR103545 fumarate induces antinociceptive effects. GR103545 fumarate can be used in research related to neurological disorders such as depression and Alzheimer's disease[1][2][3].
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GR103545 fumarate | GR103545 fumarate 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 fumarate selectively binds to KORs in the brain. GR103545 fumarate induces antinociceptive effects. GR103545 fumarate can be used in research related to neurological disorders such as depression and Alzheimer's disease. | |||||||||||||||||||||
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- [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]
- [2]. Birch PJ, et al. Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective κ-opioid receptor agonists. Bioorganic & Medicinal Chemistry Letters. 1992;2(10):1275-1278.
- [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]
Keywords
