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SML0940

Sigma-Aldrich

Nepicastat hydrochloride

≥95% (HPLC)

同義詞:

5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride, SYN-117

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About This Item

經驗公式(希爾表示法):
C14H15F2N3S · HCl
CAS號碼:
分子量::
331.81
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

化驗

≥95% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: 10 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

FC1=CC2=C(CC[C@H](N3C(CN)=CNC3=S)C2)C(F)=C1.Cl

InChI

1S/C14H15F2N3S.ClH/c15-9-3-8-4-10(1-2-12(8)13(16)5-9)19-11(6-17)7-18-14(19)20;/h3,5,7,10H,1-2,4,6,17H2,(H,18,20);1H/t10-;/m0./s1

InChI 密鑰

DIPDUAJWNBEVOY-PPHPATTJSA-N

應用

Nepicastat hydrochloride has been used as an inhibitor of dopamine β-hydroxylase (DBH) in zinc finger protein 521 (ZFP521) deficient mice.

生化/生理作用

By inhibiting dopamine β-hydroxylase (DβH), nepicastat enhances dopamine levels and norepinephrine levels in brain.
Nepicastat is a potent and selective dopamine β-hydroxylase inhibitor with an IC50 of 9 nM and negligible affinity (>10 μM) for twelve other enzymes and thirteen neurotransmitter receptors tested. Nepicastat has been shown to attenuate multiple aspects of cocaine-seeking behavior and suppress cocaine-primed reinstatement of cocaine seeking in rats, and has been in clinical trials for cocaine dependence. Nepicastat also suppressed chocolate self-administration and reinstatement of chocolate seeking in rats.

特點和優勢

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

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


分析證明 (COA)

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Richard De La Garza et al.
Progress in neuro-psychopharmacology & biological psychiatry, 59, 40-48 (2015-01-21)
In the present study, we tested the hypothesis that the potent and selective dopamine-β-hydroxylase (DβH) inhibitor nepicastat would have minimal effects on cardiovascular and pharmacokinetic parameters associated with cocaine administration and would reduce the positive subjective effects produced by cocaine.
Nobutaka Ohkubo et al.
Life sciences, 231, 116559-116559 (2019-06-15)
Previously, we reported that mice deficient in most of the Zfp521 coding region (Zfp521Δ/Δ mice) displayed abnormal behaviors, including hyperlocomotion and lower anxiety. In this study, we aimed to elucidate the involvement and mechanisms of monoamine variation. First, we compared

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