Balance between excitatory glutamate and inhibitory GABA neurotransmitter is essential and critical for proper development and functioning of brain. GABAergic (gamma aminobutyric acid) and glutamatergic interneurons maintain excitability, integrity and synaptic plasticity. Several evidences implicated relative loss of inhibitory GABA with corresponding glutamate mediated hyperexcitation in the development of autism spectrum disorder (ASD) and attention deficit hyperactivity disorder (ADHD). ASD is the common neurological disorder with an estimated relative occurrence of 0.5-1% of universal population. Several studies have demonstrated the imbalance of excitatory/inhibitory neurotransmitters resulting from neurodevelopmental impairments in glutamatergic and GABAergic system, which might resemble common pathological mechanism for developmental disorders. This review focuses on the necessity for developing GABA enhancing and glutamate suppressing drug candidates, and illustrates the role of GABAergic and glutamatergic system in cognition and memory impairment involved in neurodevelopmental disorders, with emphasis on ASD and ADHD. The review also highlights the emerging drugs for neurodevelopmental disorders.