1101854-58-3
1101854-58-3 structure
- Name: JZL184
- Chemical Name: (4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate
- CAS Number: 1101854-58-3
- Molecular Formula: C27H24N2O9
- Molecular Weight: 520.487
- Catalog: Signaling Pathways Metabolic Enzyme/Protease MAGL
- Create Date: 2017-03-24 19:28:49
- Modify Date: 2024-01-01 22:30:59
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JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.IC50 value: 8 nM [1]Target: MAGL inhibitorin vitro: JZL184 prolongs DSE in Purkinje neurons in cerebellar slices and DSI in CA1 pyramidal neurons in hippocampal slices. JZL184 is more potent in inhibiting mouse MAGL than rat MAGL [2]. in vivo: When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety of pain assays that qualitatively mimics direct central cannabinoid (CB1) agonists [1]. Acute administration of JZL184 to FAAH(-/-) mice enhanced the magnitude of a subset of cannabimimetic responses, repeated JZL184 treatment led to tolerance to its antinociceptive effects, cross-tolerance to the pharmacological effects of Δ(9)-tetrahydrocannabinol, decreases in CB1 receptor agonist-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding, and dependence as indicated by rimonabant-precipitated withdrawal behaviors, regardless of genotype [3].
| Name | (4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate |
|---|---|
| Synonyms |
4-Nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]-1-piperidinecarboxylate
unii-7mz1i2j68a 1-Piperidinecarboxylic acid, 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]-, 4-nitrophenyl ester jzl184 JZL 184 |
| Description | JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.IC50 value: 8 nM [1]Target: MAGL inhibitorin vitro: JZL184 prolongs DSE in Purkinje neurons in cerebellar slices and DSI in CA1 pyramidal neurons in hippocampal slices. JZL184 is more potent in inhibiting mouse MAGL than rat MAGL [2]. in vivo: When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety of pain assays that qualitatively mimics direct central cannabinoid (CB1) agonists [1]. Acute administration of JZL184 to FAAH(-/-) mice enhanced the magnitude of a subset of cannabimimetic responses, repeated JZL184 treatment led to tolerance to its antinociceptive effects, cross-tolerance to the pharmacological effects of Δ(9)-tetrahydrocannabinol, decreases in CB1 receptor agonist-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding, and dependence as indicated by rimonabant-precipitated withdrawal behaviors, regardless of genotype [3]. |
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| Related Catalog | |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 706.4±60.0 °C at 760 mmHg |
| Molecular Formula | C27H24N2O9 |
| Molecular Weight | 520.487 |
| Flash Point | 381.0±32.9 °C |
| Exact Mass | 520.148193 |
| PSA | 132.51000 |
| LogP | 5.25 |
| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
| Index of Refraction | 1.661 |
| Storage condition | -20℃ |