LY-2940094
LY-2940094 Basic information
- Product Name:
- LY-2940094
- Synonyms:
-
- LY-2940094
- CS-2822
- LY-2940094 tartrate
- LY-2940094 tartrate，BTRX-246040
- (2-(4-((2'-Chloro-4',4'-difluoro-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]-1-yl)methyl)-3-methyl-1H-pyrazol-1-yl)pyridin-3-yl)methanol (2R,3R)-2,3-dihydroxysuccinate
- CAS:
- 1307245-87-9
- MF:
- C26H29ClF2N4O8S
- MW:
- 631.04
- Mol File:
- 1307245-87-9.mol
LY-2940094 Usage And Synthesis
Uses
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models[1].
in vivo
LY2940094 (3, 10, or 30 mg/kg; orally daily for 4 days) dose-dependently reduces homecage ethanol self-administration in Indiana Alcohol-Preferring (P) and Marchigian Sardinian Alcohol-Preferring (msP) rats, without affecting food/water intake or locomotor activity[1].
| Animal Model: | Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g)[1] |
| Dosage: | 3, 10, or 30 mg/kg |
| Administration: | P.o.; daily for 4 days |
| Result: | Reduced homecage ethanol self-administration. |
References
[1] Rorick-Kehn LM, et al. A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models. Alcohol Clin Exp Res. 2016 May;40(5):945-54. DOI:10.1111/acer.13052
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