Effective TREK-1 channel blocker (IC50 = 71 nM) that enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis in adult mice. Exhibits antidepressant effects.
CAT No: R1093
CAS No:1270083-24-3
Synonyms/Alias:Spadin;1270083-24-3;Spadin (trifluoroacetate salt);HB5438;AKOS025293510;C96H142N26O22;DA-77962;S-1270083-24-3;
Spadin is a synthetic peptide derived from the propeptide sequence of sortilin, recognized for its unique ability to modulate the activity of the TREK-1 (TWIK-related potassium channel 1) potassium channel. As a bioactive peptide, it has gained significant attention in neurobiological and biochemical research due to its specificity for TREK-1 and its role in influencing neuronal excitability. The compound's structural properties and selective mechanism of action make it a valuable tool for dissecting potassium channel functions, as well as for exploring the physiological and pathophysiological processes associated with neuronal signaling and membrane potential regulation.
Ion Channel Research: Spadin serves as a crucial molecular probe for investigating the functional dynamics of the TREK-1 potassium channel. By acting as a selective inhibitor, it enables researchers to delineate the physiological roles of TREK-1 in neuronal cells, including its involvement in maintaining resting membrane potential, mediating neuroprotection, and modulating responses to mechanical and chemical stimuli. This specificity supports detailed studies into the channel's contribution to central nervous system function and its impact on neuronal excitability.
Neuroscience Mechanistic Studies: In the context of neurophysiology, the peptide provides a valuable means to analyze the downstream effects of potassium channel inhibition on synaptic transmission, plasticity, and overall neural circuitry. Its application in electrophysiological experiments allows for precise manipulation of neuronal activity, facilitating the elucidation of TREK-1's involvement in sensory processing, stress responses, and brain homeostasis. Utilizing Spadin in such studies helps clarify the molecular mechanisms underlying neural adaptation and signaling.
Drug Discovery and Screening: The selective interaction of this peptide with TREK-1 makes it an important reference compound in high-throughput screening assays aimed at identifying novel modulators of potassium channels. Its well-characterized binding properties and functional effects provide a benchmark for evaluating the efficacy and specificity of new chemical entities. This supports the advancement of pharmacological research focused on ion channel-targeted therapeutics, particularly in the realm of central nervous system disorders.
Cellular Signaling Pathway Elucidation: By modulating potassium channel activity, Spadin enables researchers to probe the broader signaling cascades and cellular responses influenced by membrane potential changes. Its use in cellular models assists in mapping the interplay between ion channel regulation and downstream intracellular pathways, such as those governing gene expression, neurotransmitter release, and cellular survival mechanisms. These insights are essential for understanding the integrative roles of potassium channels in cell physiology.
Peptide Functional Analysis: Beyond its role as a channel modulator, Spadin is also utilized in studies focused on peptide-receptor interactions, peptide stability, and bioavailability within biological systems. Its synthetic nature allows for the exploration of structure-activity relationships, peptide optimization, and the development of analogs with refined functional properties. Such investigations contribute to the broader field of peptide science, supporting the rational design of novel bioactive molecules for research applications.
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