Tryptamine the important psychotropic drug having indole ring has wider biological and pharmaceutical significance. The focus is to see the relevant and recent achievements as neurotransmitter and neuromodulator, vasoconstrictor and vasodilator, antimicrobial and antibacterial, antioxidant and antifungal agents. Tryptamine and its natural and synthetic derivative have been reported for the variety of biological significance in the above mentioned area. This review covers all these aspects in a comprehensive way.