1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. TAN-452

TAN-452 

目录号: HY-136208
产品使用指南

TAN-452 是一种具有口服活性,选择性的外周作用的 δ 阿片受体 (DOR) 拮抗剂,Ki 值为 0.47 nM,Kb 值为 0.21 nM。TAN-452 是 μ 阿片受体 (MORKi=36.56 nM;Kb=9.43 nM) 和 κ 阿片受体 (KORKi=5.31 nM;Kb=7.18 nM) 的拮抗剂。TAN-452 是 Naltrindole 的衍生物,具有较低的大脑渗透性,可减轻吗啡引起的副作用,而不会影响疼痛控制。

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TAN-452 Chemical Structure

TAN-452 Chemical Structure

CAS No. : 892039-23-5

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Description

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[1].

IC50 & Target

Ki: 0.47 nM (DOR), 36.56 nM (MOR) and 5.31 nM (KOR)[1]
Kb: 0.21 nM (DOR), 9.43 nM (MOR) and 7.18 nM (KOR)[1]

In Vivo

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[1].
TAN-452 (30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV) has a T1/2 of 2.1 hours[1].
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[1].
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[1].

Animal Model: Male ferrets (1.3-1.9 kg)[1]
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)[1]
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.
Molecular Weight

486.56

Formula

C₂₉H₃₀N₂O₅

CAS No.

892039-23-5

SMILES

O=C(C1=CC2=C(C=C1)C3=C([C@@](OC4=C(O)C=CC(C5)=C46)([H])[C@]76[C@@]([C@]5([H])N(CC8CC8)CC7)(O)C3)N2)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

TAN-452TAN452TAN 452Opioid Receptororallyδ-opioidreceptorDORμ-opioidMORκ-opioidKORNaltrindolemorphineantinociceptionInhibitorinhibitorinhibit

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TAN-452
目录号:
HY-136208
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