The discovery of novel neurohormones is important for the advancement of neuroendocrinology. In early 1970s, gonadotropin-releasing hormone (GnRH), a hypothalamic neuropeptide that promotes gonadotropin release, was identified to be an endogenous neurohormone in mammals. In 2000, thirty years later, another hypothalamic neuropeptide, gonadotropin-inhibitory hormone (GnIH), that inhibits gonadotropin release, was found in quail. GnIH acts via GPR147 and inhibits gonadotropin release and synthesis and reproductive function in birds through actions on GnRH neurons in the hypothalamus and pituitary gonadotrophs. Later, GnIH was found in other vertebrates including humans. GnIH studies have advanced the progress of reproductive neuroendocrinology. Furthermore, recent GnIH studies have indicated that abnormal changes in GnIH expression may cause pubertal disorder and reproductive dysfunction. Here, we describe GnIH discovery and its impact on the progress of reproductive neuroendocrinology. This review also highlights advancement and perspective of GnIH studies on drug development for pubertal disorder and reproductive dysfunction. (149/150).