SML3009
Indiplon
≥98% (HPLC)
동의어(들):
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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모든 사진(1)
About This Item
추천 제품
Quality Level
분석
≥98% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°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 key
CBIAWPMZSFFRGN-UHFFFAOYSA-N
생화학적/생리학적 작용
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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
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)
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
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
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