Harsh Kumar Tamrakar Tamrakar

D₂ antagonism toward multimodal receptor targeting, glutamatergic modulation, and neuroinflammatory regulation. Despite the success of atypical antipsychotics, limitations such as metabolic side effects, cognitive deficits, and treatment resistance persist. Novel compounds—including third-generation antipsychotics, trace amine-associated receptor 1 (TAAR1) agonists, serotonin–dopamine activity modulators (SDAMs), and glutamatergic agents—are redefining psychopharmacology through receptor-biased signaling, synaptic plasticity enhancement, and neuroimmune modulation. This review consolidates current insights into the neuropharmacological mechanisms of emerging antipsychotics, compares their efficacy and safety profiles, and explores future directions in precision psychiatry, AI-based drug design, and neurocircuit-level therapeutics.

Brain-targeted drug delivery represents one of the most challenging frontiers in pharmacology due to the presence of the blood–brain barrier (BBB), enzymatic degradation, and efflux transporters. Integration of biopharmaceutics with neuropharmacology has enabled the design of advanced delivery systems that enhance drug bioavailability, specificity, and therapeutic efficacy in central nervous system (CNS) disorders. This review explores current strategies for brain-targeted delivery, including nanoparticles, liposomes, polymeric carriers, and ligand-mediated systems. Mechanistic insights into BBB penetration, pharmacokinetic considerations, and clinical translation challenges are discussed. Future directions involve stimuli-responsive carriers, nanotheranostics, and precision neuropharmacology for personalized CNS therapy.