| Identification | Back Directory | [Name]
trace amine receptor 1 | [CAS]
1043495-96-0 | [Synonyms]
tar1
rTAR1
TAAR1
TRAR1
snorf33
RO-5256390
RP11-295F4.9
RO-5256390,RO5256390
trace amine receptor 1
trace amine associated receptor 1
Anti-TAAR1 antibody produced in rabbit
Anti-TAAR1/TA1 antibody produced in rabbit
2-Oxazolamine, 4,5-dihydro-4-[(2S)-2-phenylbutyl]-, (4S)-
(4S)-4-((2S)-2-phenylbutyl)-4,5-dihydro-1,3-oxazol-2-ylamine | [Molecular Formula]
C13H18N2O | [MDL Number]
MFCD28405494 | [MOL File]
1043495-96-0.mol | [Molecular Weight]
218.29 |
| Chemical Properties | Back Directory | [Boiling point ]
330.9±25.0 °C(Predicted) | [density ]
1.13±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
8.58±0.70(Predicted) | [color ]
White to off-white | [biological source]
rabbit | [Optical Rotation]
[α]/D 14 to 19°, c =1 in methanol | [InChI]
1S/C13H18N2O/c1-2-10(11-6-4-3-5-7-11)8-12-9-16-13(14)15-12/h3-7,10,12H,2,8-9H2,1H3,(H2,14,15)/t10-,12-/m0/s1 | [InChIKey]
IXDKFUBXESWHSL-JQWIXIFHSA-N | [SMILES]
CC[C@@H](C[C@H]1COC(N)=N1)C2=CC=CC=C2 |
| Hazard Information | Back Directory | [Uses]
RO 5256390 is a trace amine-associated receptor 1(TAAR1) agonist which may be used as treatment of cocaine addiction. | [Biological Activity]
RO5256390 is an agonist of Trace amine-associated receptor 1 (TAAR1)a GPCR primarily found in the brainexpressed in areas where the major monoamine amine transmitters (DA and NE) are also present. RO5256390 is a selective TAAR1 agonist shown to be a negative regulator of dopamine transmission. It has antipsychotic activity in models of schizophreniareduces cocaineμs reinforcng effectsand blocks binge-eating disorder. | [in vivo]
RO5256390 (0-15 μg Intracranial administration for 10 minutes; 0-10 mg/kg Intraperitoneal injection for 30 minutes; Single dose) can block compulsive overeating behavior in rats[2].
RO5256390 (0.03-30 mg/kg; Oral administration; 15-60 minutes) exhibits pro-cognitive and antidepressant-like properties in rodent and primate models. RO5256390 produces a brain activation pattern reminiscent of Olanzapine (HY-14541) in rodents[3]. | Animal Model: | Wistar rats aged 45 days old with binge-like eating[2] | | Dosage: | 0, 1.5, 5 and 15 μg per side;
0, 1, 3, 10 mg/kg | | Administration: | Intracranial administration (ICV); 10 min prior to the operant sessions;
Intraperitoneal injection (i.p.); 30 min prior to the operant sessions | | Result: | Blocked binge-like eating in rats responding 1 h per day for a highly palatable sugary diet.
Selectively reduced the rate and regularity of palatable food responding, but it did not affect either baseline intake or food restriction-induced overeating of the standard chow diet.
Fully blocked compulsive-like eating when the palatable diet was offered in an aversive compartment of a light/dark conflict box, and blocked the conditioned rewarding properties of palatable food, as well as palatable food-seeking behavior in a second-order schedule of reinforcement.
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| Animal Model: | C57BL/6J mice, NMRI mice, Sprague-Dawley rats, Long-Evans rats and Cynomolgus macaques[3] | | Dosage: | 0.03-3 mg/kg; 0.01-1 mg/kg; 1-30 mg/kg; 1-10 mg/kg; 0.3-3 mg/kg | | Administration: | Oral administration (p.o.); 15min, 30 min or 60 min | | Result: | Blocked psychostimulant-induced hyperactivity.
Did not induce cataplexy or weight gain.
Improved cognitive performance in cynomolgus macaques.
Inhibited psychostimulant induced hyperactivity.
Reversed cognitive deficits in rats.
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 19945035818 |
| Website: |
www.topule.com/ |
|