SML3477
RO5166017
≥95% (HPLC)
Sinónimos:
(4S)-2-Amino-N-ethyl-4,5-dihydro-N-phenyl-4-oxazolemethanamine, (S)-4-((Ethyl(phenyl)amino)methyl)-4,5-dihydrooxazol-2-amine
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About This Item
Fórmula empírica (notación de Hill):
C12H17N3O
Número de CAS:
Peso molecular:
219.28
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist with antipsychotic-like efficacy in vivo.
RO5166017 is an orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist (mouse/rat/human/monkey Ki = 1.9/2.7/31/24 nM, cAMP EC50 = 3.3/14/55/97 nM using respective HEK293 transfectants; GIRK EC50 = 8 nM with mTAAR1-expressing Xenopus oocytes; neurons firing frequency IC50 = 1.73/2.99 nM in mouse VTA/DRN slices) with good selectivity over TAAR4 and 123 other proteins. RO5166017 reduces spontaneous hyperlocomotion in Dat-/- mice (0.5 mg/kg ip.), as well as hyperlocomotion induction by cocaine or NMDAR agonist L-687,414 in wild-type (0.01-0.3 mg/kg po.), but not Taar1-knockout mice.
RO5166017 is an orally active, high-affinity, potent and selective trace amine-associated receptor 1 (TAAR1) agonist (mouse/rat/human/monkey Ki = 1.9/2.7/31/24 nM, cAMP EC50 = 3.3/14/55/97 nM using respective HEK293 transfectants; GIRK EC50 = 8 nM with mTAAR1-expressing Xenopus oocytes; neurons firing frequency IC50 = 1.73/2.99 nM in mouse VTA/DRN slices) with good selectivity over TAAR4 and 123 other proteins. RO5166017 reduces spontaneous hyperlocomotion in Dat-/- mice (0.5 mg/kg ip.), as well as hyperlocomotion induction by cocaine or NMDAR agonist L-687,414 in wild-type (0.01-0.3 mg/kg po.), but not Taar1-knockout mice.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity
Proceedings of the National Academy of Sciences of the USA, 108(20), 8485-8490 (2011)
Role of trace amine-associated receptor 1 in nicotine's behavioral and neurochemical effects
Neuropsychopharmacology, 43(12), 2435-2444 (2018)
F G Revel et al.
Molecular psychiatry, 18(5), 543-556 (2012-05-30)
Schizophrenia is a chronic, severe and highly complex mental illness. Current treatments manage the positive symptoms, yet have minimal effects on the negative and cognitive symptoms, two prominent features of the disease with critical impact on the long-term morbidity. In
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