Tertiapin-Q

Product Name: Tertiapin-Q

CAS No: 910044-56-3

Molar Mass: 2452.0

Chemical Formula: C106H175N35O24S4

Storage: Store at -20 degrees Celsius

Sequence: ALCNCNRIIIPHQCWKKCGKK

Application:

Tertiapin-Q is a synthetic peptide derived from the venom of the honey bee Apis mellifera, specifically designed to inhibit certain potassium channels, including the inward-rectifier potassium channels (Kir1.1 and Kir3.x) and calcium-activated potassium channels (SK channels). By blocking these channels, Tertiapin-Q modulates cellular excitability and neurotransmitter release. This makes it a valuable tool for research in neurophysiology, cardiac function, and renal physiology. Its ability to precisely target specific ion channels offers potential therapeutic applications in treating conditions such as atrial fibrillation, epilepsy, and renal disorders, where potassium channel dysfunction is implicated.

Current Research:

Tertiapin-Q, a modified 21-amino-acid peptide derived from honeybee venom, is a highly selective blocker of specific potassium (K⁺) channels, including the inward-rectifier K⁺ channels (Kir1.1 and Kir3.1/3.4) and the calcium-activated K⁺ channel (SK2). The substitution of glutamine for methionine at position 13 enhances its stability and reduces oxidation, making it more suitable for experimental and therapeutic applications.

Mechanism of Action
Tertiapin-Q binds to the extracellular region of target potassium channels, blocking ion flow and altering cellular excitability. Its high specificity for Kir and SK channels has provided insights into the physiological and pathological roles of these channels in various tissues.

Applications in Research
Cardiovascular Studies
Tertiapin-Q is widely used to investigate the role of K⁺ channels in cardiac electrophysiology, particularly in regulating atrial repolarization and action potential duration. Its ability to block IK,ACh channels makes it a valuable tool for studying atrial fibrillation mechanisms and potential anti-arrhythmic therapies.

Neurological Research
Kir3 channels, modulated by tertiapin-Q, play critical roles in neuronal excitability and synaptic transmission. This peptide is instrumental in studying G protein-coupled signaling pathways and their impact on neural networks, with implications for conditions like epilepsy and Parkinson’s disease.

Renal Function Studies
By inhibiting Kir1.1 channels in the kidney, tertiapin-Q aids in elucidating the regulation of renal K⁺ handling and electrolyte balance, providing insights into disorders such as Bartter syndrome.

Pain and Sensory Signal Modulation
Tertiapin-Q's modulation of K⁺ channels in sensory neurons makes it a potential research tool for exploring pain pathways and sensory processing.

Future Directions
Tertiapin-Q’s specificity and stability have spurred interest in its potential therapeutic applications. Ongoing research aims to optimize its pharmacological properties for the development of targeted therapies for cardiac arrhythmias, neurological disorders, and renal dysfunctions.

For researchers, tertiapin-Q remains an essential tool in ion channel studies, offering precision in understanding the complex roles of potassium channels in health and disease.

Reference:

Okada, M., Kozaki, I., & Honda, H. (2020). Antidepressive effect of an inward rectifier K+ channel blocker peptide, tertiapin-RQ. Plos one, 15(11), e0233815.