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Home > Inhibitors & Agonists > GPCR > Cannabinoid Receptor

AM 281

  Cat. No.:  DC7251   Featured
Chemical Structure
202463-68-1
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More than 5000 active chemicals with high quality for research!
Field of application
Potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 202463-68-1
Chemical Name: 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
Synonyms: AM281,AM-281
SMILES: O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCOCC4
Formula: C21H19Cl2In4O2
M.Wt: 557.21
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
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]. 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.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1076 Otenabant(CP945598.HCl) CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.
DC2050 WIN-55212-2 mesylate WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
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DC7251 AM 281 Potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).
DC7109 Otenabant (CP-945598 free base) Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.
DC12081 LY2828360 LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
DC10095 JD5037 JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).
DC7840 BML-190 BML-190 is an indomethacin morpholinylamide which functions as a selective inverse agonist of the human cannabinoid CB2 receptor.
DC9783 Bay 59-3074 Bay 59-3074 is a novel CB1/CB2 receptor partial agonist (Ki values are 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively).
DC8886 Iodopravadoline(AM-630) AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.
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