202463-68-1
202463-68-1 structure
- Name: AM281
- Chemical Name: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide
- CAS Number: 202463-68-1
- Molecular Formula: C21H19Cl2IN4O2
- Molecular Weight: 557.212
- Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
- Create Date: 2018-12-28 17:22:00
- Modify Date: 2024-01-11 19:37:18
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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].
| Name | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide |
|---|---|
| Synonyms |
AM 281
1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl- Tocris-1115 S1595_Selleck 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(morpholin-4-yl)-1H-pyrazole-3-carboxamide MFCD01861180 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(4-morpholinyl)-1H-pyrazole-3-carboxamide |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
CB1:9.91 nM (IC50) CB2:13000 nM (IC50) |
| 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]. |
| 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. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Molecular Formula | C21H19Cl2IN4O2 |
| Molecular Weight | 557.212 |
| Exact Mass | 555.992981 |
| PSA | 59.39000 |
| LogP | 4.90 |
| Index of Refraction | 1.706 |
| Storage condition | 2-8C |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H300-H315-H319-H335 |
| Precautionary Statements | P261-P264-P301 + P310-P305 + P351 + P338 |
| Personal Protective Equipment | Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges |
| Hazard Codes | T: Toxic; |
| Risk Phrases | R25 |
| Safety Phrases | 26-36/37/39-45 |
| RIDADR | UN 2811 6 |