产品
编 号：F504379
分子式：C29H30N2O5
分子量：486.56
分子式：C29H30N2O5
分子量：486.56
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 892039-23-5
产品详情
生物活性：
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47?nM and a Kb of 0.21?nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56?nM and Kb=9.43?nM) and κ-opioid receptor (KOR; Ki=5.31?nM and Kb=7.18?nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
体内研究：
TAN-452 (1, 3, 10?mg/kg for p.o. or 0.3, 1, 3?mg/kg?for s.c.) suppresses morphine-induced emesis in ferrets. TAN-452 (30?mg/kg/2?mL for PO or 3?mg/kg/mL for IV) has a T1/2 of 2.1 hours. TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30?mg/kg alone does not affect SIT. TAN-452 (10, 30?mg/kg; s.c.)?significantly suppresses morphine-induced antinociception 30?min after administration. TAN-452 (po) produces no effect up to 300?mg/kg. Animal Model:Male ferrets (1.3-1.9?kg)
Dosage:1, 3, 10?mg/kg (p.o.) or 0.3, 1, 3?mg/kg?(s.c.)
Administration:PO or SC; before morphine
Result:Prevented morphine-induced emesis in half of the animals with orally administered of 1?mg/kg and completely abolished emesis at 3 and 10?mg/kg. Completely abolished emesis by subcutaneous injection at 0.3, 1, and 3?mg/kg.
Animal Model:Crj:CD(SD) IGS male rats (7?weeks old)
Dosage:30?mg/kg/2?mL for PO or 3?mg/kg/mL for IV (Pharmacokinetic Analysis)
Administration:Orally or intravenously
Result:Had a T1/2 of 2.1 hours, a CL of 78.1 mL/min?kg, a Vss of 12.1 L/kg, and a Cmax of 526 ng/mL.
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47?nM and a Kb of 0.21?nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56?nM and Kb=9.43?nM) and κ-opioid receptor (KOR; Ki=5.31?nM and Kb=7.18?nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
体内研究：
TAN-452 (1, 3, 10?mg/kg for p.o. or 0.3, 1, 3?mg/kg?for s.c.) suppresses morphine-induced emesis in ferrets. TAN-452 (30?mg/kg/2?mL for PO or 3?mg/kg/mL for IV) has a T1/2 of 2.1 hours. TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30?mg/kg alone does not affect SIT. TAN-452 (10, 30?mg/kg; s.c.)?significantly suppresses morphine-induced antinociception 30?min after administration. TAN-452 (po) produces no effect up to 300?mg/kg. Animal Model:Male ferrets (1.3-1.9?kg)
Dosage:1, 3, 10?mg/kg (p.o.) or 0.3, 1, 3?mg/kg?(s.c.)
Administration:PO or SC; before morphine
Result:Prevented morphine-induced emesis in half of the animals with orally administered of 1?mg/kg and completely abolished emesis at 3 and 10?mg/kg. Completely abolished emesis by subcutaneous injection at 0.3, 1, and 3?mg/kg.
Animal Model:Crj:CD(SD) IGS male rats (7?weeks old)
Dosage:30?mg/kg/2?mL for PO or 3?mg/kg/mL for IV (Pharmacokinetic Analysis)
Administration:Orally or intravenously
Result:Had a T1/2 of 2.1 hours, a CL of 78.1 mL/min?kg, a Vss of 12.1 L/kg, and a Cmax of 526 ng/mL.
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