652978-45-5
Chemical Structure
RTI-371
- CAS No.: 652978-45-5
- Formula:C24H25ClN2O
- Molecular Weight:392.92
IUPAC Name: 3-(4-chlorophenyl)-5-((1S,2S,3S,5R)-8-methyl-3-(p-tolyl)-8-azabicyclo[3.2.1]octan-2-yl)isoxazole
InChIKey: MUVQRHMVRFZUGP-WOOVXOMTSA-N
SMILES: [H][C@@]12[C@H]([C@H](C[C@@](N2C)([H])CC1)C3=CC=C(C=C3)C)C4=CC(C5=CC=C(C=C5)Cl)=NO4
Biological Activity: RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC50 = 8.7 nM) and shows high binding affinity for rat DAT with a Ki value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease[1][2].
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RTI-371 | RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC50 = 8.7 nM) and shows high binding affinity for rat DAT with a Ki value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease. | |||||||||||||||||||||
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- [1]. Navarro HA, et al. Positive allosteric modulation of the human cannabinoid (CB) receptor by RTI-371, a selective inhibitor of the dopamine transporter. Br J Pharmacol. 2009 Apr;156(7):1178-84. [Content Brief]
- [2]. Hiranita T, et al. 2-isoxazol-3-phenyltropane derivatives of cocaine: molecular and atypical system effects at the dopamine transporter. J Pharmacol Exp Ther. 2014 May;349(2):297-309. [Content Brief]
Keywords
