G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries. Belongs to the G-protein coupled receptor 1 family. Detected in cerebral artery smooth muscle cells (at protein level). Detected in brain cortex, striatum, amygdala, medulla, hippocampus, caudate nucleus and putamen. Note: This description may include information from UniProtKB.
Protein type: GPCR, family 1; Membrane protein, integral; Membrane protein, multi-pass; Receptor, GPCR
Cellular Component: calyx of Held; cytoplasm; integral component of plasma membrane; integral component of presynaptic membrane; plasma membrane; serotonergic synapse
Molecular Function: drug binding; G protein-coupled serotonin receptor activity; protein binding; serotonin binding; voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels
Biological Process: adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway; adenylate cyclase-inhibiting serotonin receptor signaling pathway; bone remodeling; cellular response to alkaloid; cellular response to drug; cellular response to temperature stimulus; drinking behavior; G protein-coupled receptor internalization; G protein-coupled receptor signaling pathway; negative regulation of serotonin secretion; negative regulation of synaptic transmission, GABAergic; negative regulation of synaptic transmission, glutamatergic; positive regulation of vascular smooth muscle cell proliferation; presynaptic modulation of chemical synaptic transmission; protein kinase C-activating G protein-coupled receptor signaling pathway; regulation of behavior; regulation of dopamine secretion; regulation of presynaptic cytosolic calcium ion concentration; regulation of synaptic vesicle exocytosis; response to cocaine; response to ethanol; response to mineralocorticoid; vasoconstriction