BIBP 3226

BIBP 3226 is a synthetic non-peptide compound recognized as a highly selective antagonist of the neuropeptide Y (NPY) Y1 receptor. Structurally designed to interact with G protein-coupled receptors, it plays a pivotal role in neuropharmacological research due to its specificity and potency. BIBP 3226 is widely utilized in studies exploring the physiological and pathophysiological functions of the NPY system, particularly in the central nervous system. By enabling precise inhibition of the Y1 receptor without significant off-target effects on other NPY receptor subtypes, it offers a powerful tool for dissecting the complex signaling pathways mediated by neuropeptide Y in both basic and applied research contexts.

Receptor Pharmacology: BIBP 3226 is extensively used in receptor binding and functional assays to elucidate the pharmacological profile of the NPY Y1 receptor. Its high selectivity allows researchers to distinguish Y1-mediated signaling from other NPY receptor subtypes, facilitating the characterization of receptor-ligand interactions, downstream signaling cascades, and receptor dynamics. Such studies are crucial for understanding the molecular basis of NPY-mediated effects in neuronal and peripheral tissues.

Neuroscience Research: As a selective Y1 receptor antagonist, BIBP 3226 is instrumental in investigating the role of NPY in neurobiology, including studies on anxiety, stress response, feeding behavior, and energy homeostasis. By selectively blocking Y1 receptor activity, it enables the delineation of receptor-specific contributions to complex behavioral and physiological outcomes. This specificity is particularly valuable for mechanistic studies aiming to parse the distinct roles of NPY receptor subtypes in the central nervous system.

Signal Transduction Studies: The compound is frequently applied in experiments designed to map intracellular signaling pathways activated by NPY Y1 receptor stimulation. By antagonizing Y1-mediated signaling, researchers can identify downstream effectors, second messenger systems, and gene expression changes attributable to this receptor subtype. Such insights are essential for unraveling the molecular mechanisms underlying NPY's diverse biological actions and for identifying potential points of pharmacological intervention.

Pharmacological Screening: BIBP 3226 serves as a benchmark antagonist in high-throughput screening assays and comparative pharmacology studies. Its well-characterized profile makes it an ideal reference compound for evaluating the selectivity and efficacy of novel Y1 receptor ligands or antagonists. This application supports drug discovery efforts targeting the NPY system, as well as the validation of new chemical entities with potential relevance to neuropharmacology.

In vivo Functional Analysis: The compound is also employed in animal models to assess the physiological and behavioral consequences of selective Y1 receptor blockade. Through targeted administration, it enables the investigation of NPY Y1 receptor involvement in processes such as cardiovascular regulation, nociception, and stress adaptation. These studies provide valuable data on the functional significance of NPY signaling in whole-organism contexts, advancing the understanding of neuropeptide-mediated regulation in health and disease models.

1. Oleic acid and glucose regulate glucagon-like peptide 1 receptor expression in a rat pancreatic ductal cell line

2. Investigating Potential Interactions Between Neurohypophyseal Peptides, their Drug Analogs, and Coagulation Factor VIII

3. Myotropic activity and immunolocalization of selected neuropeptides of the burying beetle Nicrophorus vespilloides (Coleoptera: Silphidae)

4. An Isolated TCR αβ Restricted by HLA-A* 02: 01/CT37 Peptide Redirecting CD8+ T Cells to Kill and Secrete IFN-γ in Response to Lung Adenocarcinoma Cell Lines

5. Implications of ligand-receptor binding kinetics on GLP-1R signalling