추천 제품
분석
≥98% (HPLC)
양식
powder
저장 조건
desiccated
색상
white to beige
solubility
H2O: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC
InChI
1S/C23H32N2O2.2ClH/c1-26-22-11-10-21(19-23(22)27-2)12-14-25-17-15-24(16-18-25)13-6-9-20-7-4-3-5-8-20;;/h3-5,7-8,10-11,19H,6,9,12-18H2,1-2H3;2*1H
InChI key
XWOXAKBQEMQMFH-UHFFFAOYSA-N
생화학적/생리학적 작용
High affinity, orally active non-opioid intracellular receptor sigma-1 (σ1R) selective agonist with in vivo efficacy in experimental mice and rats.
SA4503 is a high affinity, orally active non-opioid intracellular receptor sigma-1 (σ1R) selective agonist (IC50 = 17.4 nM against 200 nM (+)-pentazocine for binding σ1R), exhibiting ~100-fold less affinity for the sigma 2 receptor subtype (σ2R) and little or no affinity toward 36 other receptors, ion channels and second messenger systems. Oral administration is reported to elicit cerebral acetylcholine (ACh) release in rat frontal cortex and hippocampus (5-20 mg/kg p.o.) and reduce immobility time in a mouse forced swimming test (Immobility time = 214.8 s without vs. 111.6 s with 1.0 mg/kg oral dosage).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
시험 성적서(COA)
Lot/Batch Number
Yasuharu Shinoda et al.
Journal of pharmacological sciences, 131(3), 172-183 (2016-07-21)
Haloperidol is an antipsychotic drug that inhibits the dopamine D2 receptor among others. Haloperidol also binds the sigma-1 receptor (σ1R) and inhibits it irreversibly. A serious outcome of haloperidol treatment of schizophrenia patients is death due to sudden cardiac failure.
Yasuharu Shinoda et al.
PloS one, 11(10), e0163992-e0163992 (2016-10-16)
Cardiovascular diseases are risk factors for depression in humans. We recently proposed that σ1 receptor (σ1R) stimulation rescued cardiac hypertrophy and heart failure induced by transverse aortic constriction (TAC) in mice. Importantly, σ1R stimulation reportedly ameliorates depression-like behaviors in rodents.
Dennis K Miller et al.
Pharmacology, biochemistry, and behavior, 150-151, 198-206 (2016-11-17)
This study examined the effect of the N-phenylpropyl-N'-substituted piperazine ligands SA4503 (3.4-dimethoxyphenethyl), YZ-067 (4-methoxyphenethyl), YZ-185 (3-methoxyphenethyl) and Nahas-3h (4-methoxybenzyl) on methamphetamine-induced hyperactivity in mice. In a previous study in rats, SA4503 increased methamphetamine-induced hyperactivity at a lower ligand dose and
K Matsuno et al.
European journal of pharmacology, 306(1-3), 271-279 (1996-06-13)
The binding profiles of SA4503 (1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride), a novel sigma receptor ligand, to sigma 1 and sigma 2 receptor subtypes in guinea pig and rat brain membranes were evaluated. SA4503 showed a high affinity for the sigma 1 receptor subtype
K Matsuno et al.
European journal of pharmacology, 312(3), 267-271 (1996-10-03)
The immobility time in the mouse forced swimming test was dose-dependently reduced by sigma 1 receptor agonists, such as 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503) and (+)-pentazocine, and non-specific sigma receptor agonists, such as 1,3-di(2-tolyl)guanidine (DTG) and (+)-N-cyclopropyl-methyl-N-methyl-1,4-diphenyl-1-yl-but-3-en-1-ylamin e hydrochloride (JO-1784). On the
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
고객지원팀으로 연락바랍니다.