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アプリケーション
5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate (GNTI) has been used as a selective κ opioid receptor antagonist:
- to study the influence of opioid receptor types on the anti-hyperalgesic effect of dipeptidyl peptidase 4 (DPP4) inhibitors in inflammation
- to study the role of κ opioid receptor in the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB)
- to validate its inhibitory actions on Akt kinase activities
生物化学的／生理学的作用
5′-Guanidinonaltrindole di(trifluoroacetate) (GNTI) is a 5‘-guanidine derivative and a selective κ opiate receptor antagonist. It is five-fold more potent and 500-fold more selective than norbinaltorphimine (nor-BNI) for the κ opioid receptor in smooth muscle preparations.
特徴および利点
This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
法的情報
Sold under US Patent No. 6,500,824.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
個人用保護具 (PPE)
Eyeshields, Gloves, type N95 (US)
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
G3416-VAR:
G3416-5MG:
G3416-25MG:
G3416-BULK:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Ryan Loh et al.
Behavioural brain research, 323, 1-10 (2017-01-26)
Previous work from our laboratory has shown that nonspecific kappa opioid receptor (KOR) antagonism in primary somatosensory cortex (S1) can inhibit acquisition for the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB). Although studies have demonstrated that KOR activation can alter
W C Stevens et al.
Journal of medicinal chemistry, 43(14), 2759-2769 (2000-07-14)
The indole moiety in the delta-opioid antagonist, naltrindole (2, NTI), was employed as a scaffold to hold an "address" for interaction with the kappa-opioid receptor. The attachment of the address to the 5'-position of the indole moiety was based on
Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific reports (2017)
Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific Reports (2017)
R M Jones et al.
European journal of pharmacology, 396(1), 49-52 (2000-05-24)
5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid
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