1. GPCR/G Protein
    Neuronal Signaling
  2. Cannabinoid Receptor
  3. AM281

AM281 

Cat. No.: HY-13505
Handling Instructions

AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.

For research use only. We do not sell to patients.

AM281 Chemical Structure

AM281 Chemical Structure

CAS No. : 202463-68-1

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Description

AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].

IC50 & Target[1]

CB1

9.91 nM (IC50)

CB2

13000 nM (IC50)

In Vitro

AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281[3].
Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NMRI mice with the weight of 25-30 g[3]
Dosage: 0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration)
Administration: Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration)
Result: The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle.
Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.
Molecular Weight

557.21

Formula

C₂₁H₁₉Cl₂IN₄O₂

CAS No.

202463-68-1

SMILES

O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCOCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

AM281AM 281AM-281Cannabinoid ReceptorCB1neurotoxicitySH-SY5YmemoryInhibitorinhibitorinhibit

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AM281
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HY-13505
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