Advances in bioimaging technologies capable of visualizing physiological and pathological processes are of great significance for revealing diseases development and promoting clinical diagnosis and treatment. Photoacoustic (PA) imaging, utilizing small‐molecule probes, offers a promising approach for achieving high‐spatiotemporal‐imaging of dynamic biological process. The development of near‐infrared absorbing dyes has significantly contributed to the research of small‐molecule PA probes, particularly boron‐dipyrromethene derivatives (BODIPYs) known for their simple synthesis, tunable NIR photophysical properties and superior PA imaging abilities. This review highlights recent advances in biomedical applications of BODIPY‐based PA probes, including the design strategies, spectral characteristics, response mechanisms and applications for imaging biomarkers such as reactive oxygen/nitrogen species, gaseous signaling molecules and metal ions. The insights provided in this review are expected to guide future studies on small‐molecule PA probes for bioimaging and biosensing.
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