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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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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