nAChR agonist 1

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nAChR agonist 1 是一种脑渗透性、口服有效的正变构 α7 烟碱乙酰胆碱受体 (α7 nAChR) 调节剂。

nAChR agonist 1 is a brain-permeable and?orally?efficacious positive?allosteric? α7?nicotinic?acetylcholine?receptor (α7 nAChR)modulator.

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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.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.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. Animal Model:Male BALB/c miceDosage:10 mg/kg Administration:p.o.(Pharmacokinetic?Analysis)Result:The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.

DUN71755

Endocrinology/Hormones

AChR

α7 nAChR

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1394371-75-5

419.95

C20H18ClNO3S2

>98% (HPLC)

DMSO:120mg/ml(285.76mM; Need ultrasonic)

CCC(c(sc(-c(cc1)ccc1Cl)c1C)c1-c(cc1)ccc1S(N)(=O)=O)=O

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(-20℃)

With Ice Pack

≥ 2 years