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nAChR agonist 1

SKU: orb1218861

Description

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

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1394371-75-5
MW419.95
Purity>98% (HPLC)
FormulaC20H18ClNO3S2
SMILESCCC(c(sc(-c(cc1)ccc1Cl)c1C)c1-c(cc1)ccc1S(N)(=O)=O)=O
TargetAChR
SolubilityDMSO:120mg/ml(285.76mM; Need ultrasonic)

Bioactivity

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. 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 mice. 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

DUN71755

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Protocol Information

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