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Circadian rhythm is a universal phenomenon driven by the day-night cycle among the living beings on the earth. It is considered a basic element of life, which involves oscillations of most physiological activity through the body. The coordination of the different physiologic activities should be attributed to the convergence of a diversity of regulatory mechanisms. Among the multiple links in sleep-wake cycle, the receptors are of primary importance. Since they initiate the downstream signaling leading to cell responses, the receptors are considered a commonly intervention target. Here we summarize the major receptors in sleep-wake regulation, along with a brief introduction of their functional findings, aiming to provide clues to further function understanding and intervention developing. <br />