ZSET1446

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子认知增强剂，可增强乙酰胆碱介导的海马神经元抑制性突触传递的促进作用。

A small molecule cognitive enhancer that potentiates acetylcholine-mediated facilitation of inhibitory synaptic transmission in the hippocampal neurons; increases the extracellular ACh in the cortex and hippocampus and enhances nicotine-stimulated ACh release in the hippocampus in normal rats, without affecting nAChRs.Alzheimer's Disease Phase 2 Discontinued(In Vitro):ZSET1446 (100 pM-10 nM) exerts limited effects on the basal neuronal excitability and synaptic transmission. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency. ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5 μM; 2 minutes) without affecting the basal sIPSC frequency at the range of 10 pM to 1 nM.(In Vivo):ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats. Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats. Moreover, oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone. ZSET1446 (0.002, 0.01, and 0.1 mg/kg, p.o.) ameliorates cognitive deficits of SAMP8 after 4, 8, 12, and 16 weeks of treatment in a novel object recognition test. ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment. Further, 8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus.

ZSET1446 (100 pM-10 nM) exerts limited effects on the basal neuronal excitability and synaptic transmission. ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency. ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5 μM; 2 minutes) without affecting the basal sIPSC frequency at the range of 10 pM to 1 nM.

ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats. Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats. Moreover, oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control. Further, concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone. ZSET1446 (0.002, 0.01, and 0.1 mg/kg, p.o.) ameliorates cognitive deficits of SAMP8 after 4, 8, 12, and 16 weeks of treatment in a novel object recognition test. ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment. Further, 8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus.

ST101 | ZSET-1446 | ZSET 1446 | ST-101 | ST 101

Membrane Transporter/Ion Channel

nAChR

nAChR

Neurological Disease

Alzheimer Disease

887603-94-3

236.2686

C15H12N2O

>98% (HPLC)

DMSO: ≥ 34 mg/mL

O=C1N=C2C=CC=CN2C13CC4=C(C=CC=C4)C3

Spiro[imidazo[1,2-a]pyridine-3(2H),2'-[2H]inden]-2-one, 1',3'-dihydro-

(-20℃)

With Ice Pack

≥ 2 years