Abstract: Three gaseous molecules are widely accepted as important gasotransmitters in mammalian cells, namely NO, CO and H2S. Due to the pharmacological effects observed in preclinical studies, these three gasotransmitters represent promising drug candidates for clinical translation. Fluorescent probes of the gasotransmitters are also in high demand; however, the mechanisms of actions or the roles played by gasotransmitters under both physiological and pathological conditions remain to be answered. In order to bring these challenges to the attention of both chemists and biologists working in this field, we herein summarize the chemical strategies used for the design of both probes and prodrugs of these three gasotransmitters.