AM 281

Name: AM 281
Brand: Tocris Bioscience
SKU: 1115

Tocris Bioscience, part of Bio-Techne | Catalog # 1115

Citations (32)

COA / SDS

Potent and selective CB1 inverse agonist

Discontinued Product

1115 has been discontinued. View all Cannabinoid R1 / CB1 Inverse Agonists products.

Key Product Details

Description:	Potent and selective CB₁ inverse agonist
Chemical Name:	1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
Purity:	≥99% (HPLC)
Molecular Weight:	557.22

View Full Technical Details for AM 281

Technical Data
Citations

Biological Activity for AM 281

AM 281 is a potent, selective CB₁ cannabinoid receptor antagonist/inverse agonist (K_i values are 12 and 4200 nM for CB₁ and CB₂ receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (K_i = 14 nM).

Licensing Information

Sold with the permission of the University of Connecticut

Technical Data for AM 281

M. Wt	557.22
Formula	C₂₁H₁₉Cl₂IN₄O₂
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	202463-68-1
PubChem ID	4302962
InChi Key	AJFFBPZYXRNAIC-UHFFFAOYSA-N
Smiles	CC1=C(N(N=C1C(=O)NN1CCOCC1)C1=C(Cl)C=C(Cl)C=C1)C1=CC=C(I)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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References for AM 281

References are publications that support the biological activity of the product.

Lan Design and synthesis of the CB1 selective cannabinoid antagonist AM281: a potential human SPECT ligand. AAPS Pharmsci. 1999 PMID: 11741201
Gifford Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices. Neurosci.Lett. 1997 PMID: 9464661
Gatley Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo. J.Neurochem. 1998 PMID: 9422389
Cosenza Locomotor activity and occupancy of brain cannabinoid CB1 receptors by the antagonist/inverse agonist AM281. Synapse 2000 PMID: 11044895