Recombinant Human HTR1B protein

The 5-hydroxytryptamine receptor 1B (HTR1B), also known as 5-HT1B, is a G protein-coupled receptor (GPCR) that primarily binds serotonin (5-HT), a key neurotransmitter regulating mood, cognition, and sensory processing. Encoded by the HTR1B gene in humans, it is widely expressed in the central nervous system (CNS), particularly in the basal ganglia, cortex, and hippocampus, as well as in peripheral tissues like blood vessels. HTR1B modulates synaptic serotonin levels by inhibiting neurotransmitter release via presynaptic autoreceptors, influencing neural circuits associated with aggression, anxiety, and depression.

Recombinant HTR1B protein is artificially produced using expression systems (e.g., mammalian, insect, or bacterial cells) to study its structure, ligand interactions, and signaling pathways. Its recombinant form typically retains the seven transmembrane domains characteristic of GPCRs, along with extracellular loops involved in ligand binding and intracellular regions critical for G-protein coupling (primarily Gi/o-mediated inhibition of cAMP). Researchers utilize this protein to screen psychoactive drugs, antidepressants, and migraine therapeutics (e.g., triptans, which target 5-HT1B/1D receptors). Structural studies of recombinant HTR1B, often stabilized in specific conformations, have advanced the design of biased agonists that selectively activate therapeutic signaling pathways while minimizing side effects. Challenges in its recombinant production include maintaining proper post-translational modifications (e.g., glycosylation) and membrane integration for functional assays. Despite these hurdles, HTR1B remains a pivotal target in neuropharmacology due to its role in serotonin-related disorders and its therapeutic potential.