gnti

κ opioid receptor antagonist

5'-Guanidinonaltrindole (GNTI) 为一种选择性 kappa opioid receptor 拮抗剂。

6'-GNTI dihydrochloride 是一种κ-阿片受体（KOR）激动剂，它偏向于激活 G 蛋白介导的信号传导，而不是β-阿司匹林2的募集。6'-GNTI dihydrochloride 只能激活纹状体神经元中的 Akt 通路。

GNTI TFA is a selective kappa opioid receptor antagonist.

Eprociclovir Na is the salt form of Eprociclovir, also known as A-5021, a new acyclovir analogue and a potent inhibitor of EHV1 replication and may have potential for the treatment and or prophylaxis of infections with this virus. Eprociclovir possess potent anti-herpetic activity against most human herpesviruses. A-5021 proved to be about 15-fold more potent than acyclovir in inhibiting viral replication. Eprociclovir inhibits murine herpetic keratitis. A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. Eprociclovir is a promising alternative treatment of herpetic keratitis.

Difelikefalin is a κ-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50= >1 μM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively). 1.Schteingart, C.D., Menzaghi, F., Jiang, G., et al.Synthetic peptide amides(2008)

Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg kg, respectively).

Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg kg, respectively).