NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).References
NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).
References
Fanapanel hydrate is a highly selective antagonist of AMPA/kainate with little activity against NMDA(Ki of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively).
Napamezole is an α2 adrenergic receptor antagonist. Napamezole antagonizes methoxamine-induced contractions (alpha-1) of the rat vas deferens with a Kb of 135 nM. Napamezole reverses clonidine-induced decreased in twitch height in the electrically stimula
Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. [2] Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg/kg every other day.[1]
9-cis-Vitamin A palmitate (9-cis-Retinyl palmitate) is a 9-cis isomer resulting from the interaction of vitamin A palmitate in corn flakes. It exhibits a biological activity of 26% compared to all-trans-vitamin A palmitate, which is known to be the most biologically active form of vitamin A.
Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.