Molecular structure of NESS 0327, CAS Number: 494844-07-4
NESS 0327 (CAS 494844-07-4)
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Alternate Names:
8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide
Application:
NESS 0327 is a potent, selective CB1 receptor antagonist
CAS Number:
494844-07-4
Purity:
≥98%
Molecular Weight:
489.82
Molecular Formula:
C24H23Cl3N4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
NESS 0327 is an extremely potent cannabinoid receptor antagonist with high selectivity for the CB1 receptor compared to the CB2 receptor with Ki values of 0.35 pM and 21 nM, respectively.1 It is a much more potent antagonist and more selective for the CB1 receptor compared to SR 141716A. At nM concentrations NESS 0327 competitively inhibits the binding of the synthetic CB agonist WIN 55,212-2 in isolated rat cerebella membranes and murine vas deferens.1,2 Unlike SR 141716A, NESS 0327 at higher doses does not act as a CB1 receptor inverse agonist and does not produce any physiological effects of its own.1,2
NESS 0327 (CAS 494844-07-4) References
- Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. | Ruiu, S., et al. 2003. J Pharmacol Exp Ther. 306: 363-70. PMID: 12663689
- Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors. | Tambaro, S., et al. 2005. Eur J Pharmacol. 525: 150-3. PMID: 16271359
- Bisphenol A Induces Fatty Liver by an Endocannabinoid-Mediated Positive Feedback Loop. | Martella, A., et al. 2016. Endocrinology. 157: 1751-63. PMID: 27014939
- mGluR-LTD at Excitatory and Inhibitory Synapses in the Lateral Habenula Tunes Neuronal Output. | Valentinova, K. and Mameli, M. 2016. Cell Rep. 16: 2298-307. PMID: 27545888
- Cell-Autonomous Excitation of Midbrain Dopamine Neurons by Endocannabinoid-Dependent Lipid Signaling. | Gantz, SC. and Bean, BP. 2017. Neuron. 93: 1375-1387.e2. PMID: 28262417
- Corticosterone Attenuates Reward-Seeking Behavior and Increases Anxiety via D2 Receptor Signaling in Ventral Tegmental Area Dopamine Neurons. | Peng, B., et al. 2021. J Neurosci. 41: 1566-1581. PMID: 33372063
- Tonic Endocannabinoid Signaling Gates Synaptic Plasticity in Dorsal Raphe Nucleus Serotonin Neurons Through Peroxisome Proliferator-Activated Receptors. | Oubraim, S., et al. 2021. Front Pharmacol. 12: 691219. PMID: 34262460
- Cannabinoid receptor 1 antagonist genistein attenuates marijuana-induced vascular inflammation. | Wei, TT., et al. 2022. Cell. 185: 1676-1693.e23. PMID: 35489334
- 2-AG and anandamide enhance hippocampal long-term potentiation via suppression of inhibition. | Lemtiri-Chlieh, F. and Levine, ES. 2022. Front Cell Neurosci. 16: 1023541. PMID: 36212685
- A Complete Endocannabinoid Signaling System Modulates Synaptic Transmission between Human Induced Pluripotent Stem Cell-Derived Neurons. | Asher, MJ., et al. 2023. Mol Pharmacol. 103: 100-112. PMID: 36379717
Inhibitor of:
CB1, CBS, and Clb1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
NESS 0327, 1 mg | sc-222054 | 1 mg | $316.00 | |||
NESS 0327, 5 mg | sc-222054A | 5 mg | $1270.00 |