GR94800 is extremely potent and selective NK-2 receptor antagonist.
CAT No: R1021
CAS No:141636-65-9
Synonyms/Alias:N-Benzoyl-L-alanyl-L-alanyl-D-tryptophyl-L-phenylalanyl-D-prolyl-L-prolyl-L-norleucinamide
GR 94800 is a synthetic peptide compound recognized as a highly selective antagonist of the 5-hydroxytryptamine 3 (5-HT3) receptor, a subtype of serotonin receptor. As a structurally defined peptide, it has become an important molecular tool for neuropharmacological research, particularly in studies elucidating serotonergic signaling pathways. Its specificity for the 5-HT3 receptor allows researchers to dissect the physiological and pharmacological roles of this receptor in both central and peripheral nervous system contexts. The compound's ability to modulate ligand-gated ion channel activity makes it especially valuable for investigating neurotransmission, receptor pharmacology, and synaptic modulation.
Neuropharmacology research: GR 94800 is widely employed in neuropharmacological studies to probe the function of 5-HT3 receptors in neuronal signaling. By selectively inhibiting these ionotropic receptors, investigators can isolate the effects of serotonergic transmission from those mediated by other serotonin receptor subtypes. This selectivity enables detailed analysis of synaptic currents, receptor kinetics, and downstream signaling events, advancing understanding of how 5-HT3 receptors contribute to neural circuit modulation and neurotransmitter release.
Electrophysiological studies: The compound serves as an effective pharmacological tool in electrophysiological experiments, such as patch-clamp recordings and voltage-clamp assays. Its high affinity for the 5-HT3 receptor allows precise manipulation of receptor activity, facilitating the characterization of receptor-mediated ion flux and synaptic responses. Researchers utilize GR 94800 to delineate the ionic mechanisms underlying fast excitatory neurotransmission in both central and peripheral neurons, providing insights into receptor gating, desensitization, and pharmacological modulation.
Behavioral neuroscience: In preclinical behavioral assays, GR 94800 is used to investigate the role of 5-HT3 receptors in modulating anxiety, emesis, nociception, and cognitive processes. By selectively blocking these receptors, scientists can evaluate their contribution to behavioral phenotypes and neuropsychiatric models. Such studies are instrumental in clarifying the neurobiological basis of serotonergic influence on mood, sensory processing, and higher-order brain functions, supporting the development of targeted neuropharmacological hypotheses.
Drug discovery and screening: The compound is valuable in high-throughput screening platforms designed to identify novel ligands or modulators of the 5-HT3 receptor. Its well-characterized antagonist profile provides a benchmark for evaluating the potency, specificity, and efficacy of new chemical entities. Additionally, GR 94800 is used to validate assay systems, optimize screening conditions, and establish structure-activity relationships for drug candidates targeting serotonergic signaling pathways.
Peptide structure-activity relationship studies: As a synthetic peptide with defined receptor selectivity, GR 94800 is also employed in structure-activity relationship (SAR) investigations. Researchers utilize it to explore the molecular determinants of 5-HT3 receptor binding and antagonism, informing the design of next-generation peptide-based modulators. Insights gained from such studies contribute to the rational development of research tools and potential lead compounds for neuropharmacological applications.
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