SML3009
Indiplon
≥98% (HPLC)
别名:
CL 285,489, CL 285489, CL-285,489, CL-285489, CL285,489, CL285489, N-Methyl-N-(3-(3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)acetamide, N-Methyl-N-[3-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide, NBI 34060, NBI-34060, NBI34060
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About This Item
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![2-Methyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-carboxylic acid AldrichCPR](/deepweb/assets/sigmaaldrich/product/structures/204/259/e1c44511-5ba6-4d2f-81e8-5d29de590d54/640/e1c44511-5ba6-4d2f-81e8-5d29de590d54.png)
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
[s]1c(ccc1)C(=O)c2c3[n](nc2)C(=CC=N3)c4cc(ccc4)N(C)C(=O)C
InChI
1S/C20H16N4O2S/c1-13(25)23(2)15-6-3-5-14(11-15)17-8-9-21-20-16(12-22-24(17)20)19(26)18-7-4-10-27-18/h3-12H,1-2H3
InChI 密鑰
CBIAWPMZSFFRGN-UHFFFAOYSA-N
生化／生理作用
Indiplon (NBI 34060) is an orally active, high-affinity GABAA receptor positive allosteric modulator (PAM) with preferential labeling of alpha1 subunits-containing receptors (rat cerebellar/cerebral cortex membranes binding KD = 1.01/0.45 nM). Indiplon potentiates GABA-induced chloride conductance of cultured rat cortical neurons (EC50 = 11.6 nM vs 152 nM/630 nM) and exhibits sedative efficacy in mice (ED50 = 1 mg/kg/passive avoidance & 2.7 mg/kg/locomotor activity inhibition po.) and rats (ED50 = 2.5 mg/kg/locomotor activity inhibition & 3 mg/kg/vigilance impairment po.) in vivo. Indiplon shows greater affinity, in vitor and in vivo potency than zaleplon and zolpidem.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
D K Cass et al.
Molecular psychiatry, 19(5), 536-543 (2014-03-05)
Converging epidemiological studies indicate that cannabis abuse during adolescence increases the risk of developing psychosis and prefrontal cortex (PFC)-dependent cognitive impairments later in life. However, the mechanisms underlying the adolescent susceptibility to chronic cannabis exposure are poorly understood. Given that
Alan C Foster et al.
The Journal of pharmacology and experimental therapeutics, 311(2), 547-559 (2004-07-17)
Indiplon (NBI 34060; N-methyl-N-[3-[3-(2-thienylcarbonyl)-pyrazolo[1,5-alpha]pyrimidin-7-yl]phenyl]acetamide), a novel pyrazolopyrimidine and high-affinity allosteric potentiator of GABA(A) receptor function, was profiled for its effects in rodents after oral administration. In mice, indiplon inhibited locomotor activity (ED(50) = 2.7 mg/kg p.o.) at doses lower than
Robert E Petroski et al.
The Journal of pharmacology and experimental therapeutics, 317(1), 369-377 (2006-01-10)
Indiplon (NBI 34060) is a novel pyrazolopyrimidine currently in development for the treatment of insomnia. We have previously shown that indiplon exhibits high-affinity binding to native GABA(A) receptors from rat brain and acts as a positive allosteric modulator of GABA(A)
Yanbo Jiang et al.
Neuropharmacology, 138, 97-105 (2018-06-09)
Ionotropic GABAA receptors expressing at the axon initial segment (AIS) of glutamatergic pyramidal cell (PC) in the cortex plays critical roles in regulating action potential generation. However, it remains unclear whether these receptors also express at the AIS of cortical
Ignacio Vega-Quiroga et al.
Neuropharmacology, 128, 76-85 (2017-10-01)
The mechanisms commanding the activity of dopaminergic neurons of the ventral tegmental area (VTA) and the location of these neurons are relevant for the coding and expression of motivated behavior associated to reward-related signals. Anatomical evidence shows that several brain
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