Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H11FN2O |
| Molecular Weight | 194.2055 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(F)C=CC=C1[C@H]2COC(N)=N2
InChI
InChIKey=IOHOUWIYOVWGHV-SECBINFHSA-N
InChI=1S/C10H11FN2O/c1-6-7(3-2-4-8(6)11)9-5-14-10(12)13-9/h2-4,9H,5H2,1H3,(H2,12,13)/t9-/m1/s1
| Molecular Formula | C10H11FN2O |
| Molecular Weight | 194.2055 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:55:38 GMT 2023
by
admin
on
Sat Dec 16 18:55:38 GMT 2023
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| Record UNII |
Y2P4KD8GDR
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| Record Status |
Validated (UNII)
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| Record Version |
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RO-5263397
Created by
admin on Sat Dec 16 18:55:38 GMT 2023 , Edited by admin on Sat Dec 16 18:55:38 GMT 2023
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PRIMARY | MedKoo CAT NO.: 522568, CAS NO.: 1357266-05-7Description: RO5263397 is a selective TAAR 1 agonist. RO5263397 was efficacious in reducing cocaine-mediated behaviors. RO5263397 dose-dependently prevented cocaine-induced lowering of ICSS thresholds. TAAR1 stimulation effectively suppresses the rewarding and reinforcing effects of cocaine in self-administration and ICSS models, supporting the candidacy of TAAR1 as a drug discovery target for cocaine addiction. (last updated: 1/6/2016). | ||
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56835991
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admin on Sat Dec 16 18:55:38 GMT 2023 , Edited by admin on Sat Dec 16 18:55:38 GMT 2023
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Y2P4KD8GDR
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admin on Sat Dec 16 18:55:38 GMT 2023 , Edited by admin on Sat Dec 16 18:55:38 GMT 2023
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1357266-05-7
Created by
admin on Sat Dec 16 18:55:38 GMT 2023 , Edited by admin on Sat Dec 16 18:55:38 GMT 2023
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300000042479
Created by
admin on Sat Dec 16 18:55:38 GMT 2023 , Edited by admin on Sat Dec 16 18:55:38 GMT 2023
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ACTIVE MOIETY |
This study examined the effects of a selective TAAR 1 agonist, RO5263397, on cocaine induced behavioral sensitization in rats, a rodent model of drug-induced behavioral plasticity. Daily treatment with 15mg/kg cocaine (i.p., 7 days) induced robust locomotor sensitization in rats. RO5263397 (1-10mg/kg, i.p.) alone did not significantly alter the locomotor activity. Acute treatment with RO5263397 (3.2 and 10mg/kg) did not significantly modify cocaine-induced hyperactivity, however, the induction of locomotor sensitization was significantly blocked after 7 days of daily RO5263397 treatment. More importantly, the expression of locomotor sensitization remained significantly attenuated when rats were re-tested 7 days after the last drug treatment. The marked attenuation of cocaine sensitization was also evidenced by the suppression of the dose-effect function (3.2-32mg/kg) of cocaine sensitization. Together, these data represent the first to report a critical modulatory role of TAAR 1 agonists in cocaine-induced behavioral plasticity, which may be indicative of its potential role for altering other long-lasting behavioral maladaptations of cocaine including drug addiction.
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