Calcitonin gene-related peptide (CGRP), a predominant neurotransmitter in sensory nerves, is widely distributed in central and peripheral tissues. In the cardiovascular system, besides relaxing vascular smooth muscle, CGRP protects against ischemic myocardium while inhibiting cardiac remodeling. The pharmacological effects of nitroglycerin and rutaecarpine have proved to be associated with the increase in the synthesis and release of CGRP. In gastrointestinal tissues, CGRP participates in the regulation of gastrointestinal function and has protective effects on the gastric mucosa. Rutaecar?pine, capsaicin and its derivatives can reduce gastric mucosa damage induced by a variety of factors by increasing synthesis and release of CGRP.