For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I016918 |
| CAS Number | 1394371-75-5 |
| Synonyms | 4-[5-(4-chlorophenyl)-4-methyl-2-propanoylthiophen-3-yl]benzenesulfonamide |
| Molecular Formula | C20H18ClNO3S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H18ClNO3S2/c1-3-17(23)20-18(13-6-10-16(11-7-13)27(22,24)25)12(2)19(26-20)14-4-8-15(21)9-5-14/h4-11H,3H2,1-2H3,(H2,22,24,25) |
| InChIKey | DYIIYIJHDMIABW-UHFFFAOYSA-N |
| SMILES | CCC(=O)C1=C(C(=C(S1)C2=CC=C(C=C2)Cl)C)C3=CC=C(C=C3)S(=O)(=O)N |
| Reference | [1]. Sinha N, et al.Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relati |
