MDL 29913 acts as selective antagonist of NK2 tachykinin receptor. It is used for the treatment of IBS.
CAT No: R1071
CAS No:135721-56-1
Synonyms/Alias:1,4,7,10,13,16-Hexaazacyclooctadecane, Cyclic Peptide Deriv.; N-(2-Amino-4-methylpentyl)-N-methyl-L-leucyl-L-glutaminyl-L-tryptophyl-L-phenylalanylglycine (5→1)-Lactam
MDL 29,913 is a small-molecule compound recognized for its role as a potent and selective antagonist of adenosine A2A receptors. As a synthetic purine derivative, it has been widely utilized in neuropharmacology and receptor biology to probe the functional significance of adenosine signaling pathways. Its high affinity and selectivity for the A2A receptor subtype have made it a valuable tool for dissecting the physiological and biochemical processes modulated by adenosine in the central nervous system and peripheral tissues. Researchers rely on MDL 29,913 to elucidate receptor-mediated mechanisms, investigate signal transduction cascades, and explore the modulation of neurotransmitter systems.
Receptor Characterization: In molecular pharmacology and cell signaling research, MDL 29,913 is extensively used for the functional characterization of adenosine A2A receptors. By selectively blocking this receptor subtype, investigators can distinguish A2A-mediated responses from those of other adenosine receptor families, such as A1, A2B, and A3. This specificity enables detailed mapping of receptor distribution, ligand-binding dynamics, and downstream signaling events, facilitating a more precise understanding of adenosine's role in cellular physiology.
Neurotransmission Studies: The compound's ability to antagonize A2A receptors has proven instrumental in neurobiological studies examining the regulation of dopaminergic and glutamatergic neurotransmission. In experimental models, MDL 29,913 aids in delineating the interplay between adenosine and dopamine signaling, particularly within the basal ganglia and striatal pathways. Such investigations provide insights into the modulation of motor activity, synaptic plasticity, and the biochemical basis of neurodegenerative conditions, supporting the development of new hypotheses regarding neural circuitry.
Signal Transduction Analysis: MDL 29,913 serves as a robust pharmacological probe in the study of intracellular signaling mechanisms initiated by adenosine receptor activation. By inhibiting A2A receptor-mediated cyclic AMP (cAMP) accumulation and related second messenger cascades, researchers can interrogate the specificity and magnitude of cellular responses to adenosine agonists. This approach enables the dissection of complex signaling networks and assists in identifying critical regulatory nodes within various cell types, including neurons, glial cells, and immune cells.
Behavioral Pharmacology: In preclinical behavioral research, the compound is utilized to assess the functional consequences of A2A receptor blockade on animal models of learning, memory, and motor function. Its application allows scientists to separate the behavioral effects attributable to A2A receptor activity from those mediated by other neurotransmitter systems. Such studies contribute to a deeper understanding of adenosine's neuromodulatory influence on cognitive and motor processes, informing the design of future experimental paradigms.
Drug Discovery and Screening: MDL 29,913 is frequently employed as a reference antagonist in high-throughput screening assays and pharmacological profiling of novel adenosine receptor modulators. Its well-characterized binding properties and selectivity profile make it an essential standard for validating assay performance, benchmarking new chemical entities, and establishing structure-activity relationships. This utility supports the advancement of receptor-targeted drug discovery efforts and the optimization of screening methodologies in both academic and industrial research settings.
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