1394371-75-5
1394371-75-5 structure
- Name: nAChR agonist 1
- Chemical Name: nAChR agonist 1
- CAS Number: 1394371-75-5
- Molecular Formula: C20H18ClNO3S2
- Molecular Weight: 419.94
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
- Create Date: 2020-04-10 15:04:26
- Modify Date: 2024-01-08 12:58:48
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nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease[1].
| Name | nAChR agonist 1 |
|---|
| Description | nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease[1]. |
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| Related Catalog | |
| In Vivo | Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial[1]. nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively[1]. nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively[1]. Animal Model: Male BALB/c mice[1] Dosage: 10 mg/kg Administration: p.o.(Pharmacokinetic Analysis) Result: The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively. |
| References |
| Molecular Formula | C20H18ClNO3S2 |
|---|---|
| Molecular Weight | 419.94 |