Title: Tertiapin
CAS Registry Number: 58694-52-3
Additional Names: TPN
Literature References: Neurotoxic 21 residue peptide isolated from the venom of the European honey bee, Apis mellifera. Characterized by 2 disulfide linkages and the complete absence of negatively charged residues, it selectively inhibits G-protein inwardly rectifying potassium channels (GIRK) by binding to the external vestibule of the channel. Isoln: J. Gauldie et al., Eur. J. Biochem. 61, 369 (1976); B. E. C. Banks et al., Bull. Instit. Pasteur 74, 137 (1976). Primary structure: Y. A. Ovchinnikov et al., Soviet J. Bioorg. Chem. 6, 187 (1980); 3D-structure: X. Xu, J. W. Nelson, Proteins Struct. Funct. Genet. 17, 124 (1993). Inhibition of GIRK-channels: W. Jin, Z. Lu, Biochemistry 37, 13291 (1998); of muscarinic inwardly rectifying potassium channels (IK(ACh)): M.-D. Drici et al., Br. J. Pharmacol. 131, 569 (2000); D. E. Benavides-Haro et al., Arch. Pharm. 368, 309 (2003).
Derivative Type: Tertiapin Q
CAS Registry Number: 252198-49-5
Additional Names: TPNQ
Literature References: Non-air-oxidizable derivative of TPN in which Met-13 is replaced with Gln. Synthesis: W. Jin, Z. Lu, Biochemistry 38, 14286 (1999). Mechanism of inhibition: W. Jin et al., ibid. 14294. Proton titration of TPNQ binding: Y. Ramu et al., ibid. 40, 3601 (2001).
Use: Biochemical probe for potassium channels. |