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About This Item
Empirical Formula (Hill Notation):
C106H176N34O23S5
CAS Number:
Molecular Weight:
2455.07
UNSPSC Code:
12352200
NACRES:
NA.32
MDL number:
assay
>95%
form
powder
technique(s)
HPLC: suitable
storage temp.
−20°C
Application
Tertiapin was used for developing a novel CZE-DAD method for analyzing the honeybee venom.
Biochem/physiol Actions
A potent inhibitor of the inward-rectifier K+ channels, blocked a G-protein-gated channel (GIRK1/4) and the ROMK1 channel with nanomolar affinities, however a closely related channel, IRK1, was insensitive to tertiapin. Thus, tertiapin is a tool for purifying functional channels as well as for screening pharmaceutical agents against these channels.
Potent inhibitor of the inward-rectifier K+ channels.
Tertiapin is a peptide isolated from honey bee venom, which is a selective IKACh blocker that prolongs the atrial effective refractory period and terminates the atrial fibrillation. It is a selective and potent inhibitor of muscarinic K+ channels in rabbit cardiac myocytes.
Preparation Note
Tertiapin dissolves in water at 1 mg/ml to yield a clear solution.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Regulatory Information
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H Kitamura et al.
The Journal of pharmacology and experimental therapeutics, 293(1), 196-205 (2000-03-29)
Tertiapin is a 21-residue peptide isolated from honey bee venoms. A recent study indicated that tertiapin is a potent blocker of certain types of inwardly rectifying K(+) (Kir) channels (). We examined the effect of tertiapin on ion channel currents
Norio Hashimoto et al.
Pharmacological research, 54(2), 136-141 (2006-05-27)
It is well known that vagal nerve tone plays a crucial role in atrial fibrillation (AF). Acetylcholine-activated potassium current (IKACh) mediates much of the cardiac response to vagal nerve stimulation (VNS), but the contribution of IKACh to AF remains unknown.
Zenon J Kokot et al.
Analytical and bioanalytical chemistry, 399(7), 2487-2494 (2011-01-12)
The aim of this study was to develop a new precise and accurate CZE-DAD method for honeybee venom analysis using cytochrome c as an internal standard. The 64.5 cm total length, 56 cm effective length, 75 μm ID, and 360
W Jin et al.
Biochemistry, 37(38), 13291-13299 (1998-09-28)
Inward-rectifier K+ channels are a group of highly specialized K+ channels that accomplish a variety of important biological tasks. Inward-rectifier K+ channels differ from voltage-activated K+ channels not only functionally but also structurally. Each of the four subunits of the
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