1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
[1] Mair ID, et al. Br J Pharmacol. 1998 Aug;124(8):1667-74. [2] Higgins GA, et al. J Pharmacol Exp Ther. 1993 Mar;264(3):1440-9.
Cell experiment: | HT29 cells are washed with Phosphate buffer saline (PBS) and harvested with a 0.5% trypsin solution at 50-60% confluency. Cells are then added to wells at a density of 104 cells/well in a 96-well plate to a final volume of 100 μL/well. After 24 hours of incubation at 37°C in a 5% CO2 atmosphere, the culture medium is replaced with 200 μL fresh culture medium containing 5HT hydrochloride, Phenylbiguanide hydrochloride at concentrations of: 3.125, 6.25, 12.5, 25, 50, and 100 μM . Cells cultured solely in media served as negative controls. After 48 hours of incubation at 37°C in a 5% CO2 atmosphere, the culture medium is removed and 8 μL MTT reagent (diluted in PBS at a concentration of 4 mg/mL) is added to 50 μL of fresh culture medium at a final concentration of 0.55 mg/mL. The optimum incubation period time is determined in a pilot study[2]. |
Animal experiment: | Mice[3] Adult male specified pathogen free (SPF) BALB/c mice (28-33 g; n=10) are used throughout this study. All mice have free access to water and food in a light (12: 12 h light/ dark cycle, lights on at 0700 h) and temperature-controlled (21-23°C) environment. Mice are randomly assigned to two treatment groups, 1) intra-atrial injection of 0.9% saline (controls, n=5) or 2) intra-atrial injection of vehicle containing Phenylbiguanide (n=5). For the PBGinjected group, mice are injected with an effective dose of Phenylbiguanide (1-1.5 μg in 10-15 μL saline) . This is repeated five times in total with each injection separated by 8-10 min. For control mice, each mouse receives five saline injections (10-15 μL each), also at 8-10 min intervals[3]. |
参考文献: [1]. Mair ID, et al. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b)) expressed in Xenopus laevis oocytes. Br J Pharmacol. 1998 Aug;124(8):1667-74. | |
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