1445605-23-1
1445605-23-1 structure
- Name: Lu AF21934
- Chemical Name: (1S,2R)-N-(3,4-Dichlorophenyl)-1,2-cyclohexanedicarboxamide
- CAS Number: 1445605-23-1
- Molecular Formula: C14H16Cl2N2O2
- Molecular Weight: 315.195
- Catalog: Research Areas Neurological Disease
- Create Date: 2018-02-01 02:27:04
- Modify Date: 2024-01-02 19:49:42
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Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
| Name | (1S,2R)-N-(3,4-Dichlorophenyl)-1,2-cyclohexanedicarboxamide |
|---|---|
| Synonyms |
(1S,2R)-N-(3,4-Dichlorophenyl)-1,2-cyclohexanedicarboxamide
1,2-Cyclohexanedicarboxamide, N-(3,4-dichlorophenyl)-, (1S,2R)- Lu AF21934 |
| Description | Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. |
|---|---|
| Related Catalog | |
| Target |
IC50: 500 nM (hmGlu4)[1] |
| In Vivo | Lu AF21934 treatment shows a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases the basal locomotor activity of mice that are not habituated to activity cages[1]. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min[2]. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI[3]. |
| Animal Admin | Rats: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Lu AF21934 (2, 5, 10 and 15 mg/kg, s.c.) and diazepam (5 mg/kg, i.p.) are administered acutely 1 h before the Vogel’s conflict test. The effects of each drug in all experiments are measured in groups of 8-10 animals[1]. Mice: Lu AF21934 is dispersed in 20% (2-hydropropyl)-b-cyclodextrin and are administered subcutaneously (s.c.) 60 min before the test. Mice are gently placed into the box and allowed to explore for 15 s. Then, each time a mouse passed from one plate to another, the experimenter electrifies the whole floor thus evoking a visible flight reaction of the animal. If the animal continues running, no new shock is delivered for the following 3 s[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 577.6±50.0 °C at 760 mmHg |
| Molecular Formula | C14H16Cl2N2O2 |
| Molecular Weight | 315.195 |
| Flash Point | 303.1±30.1 °C |
| Exact Mass | 314.058868 |
| LogP | 2.62 |
| Appearance | white solid |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.615 |
| Storage condition | -20℃ |