Biological ActivityTertiapin-Q is a high affinity blocker for inward-rectifier K+ channels. Tertiapin-Q is a stable derivative of the bee venom toxin tertiapin. Tertiapin-Q binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and is selective over Kir2.1 channels. Tertiapin-Q improves heart rate and atrioventricular conduction in a mouse model of bradycardia. Derivative Tertiapin LQ (Cat. No. 4339) also available.
(Modifications: Disulfide bridges: 3-14, 5-18, Lys-21 = C-terminal amide)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q.
Jin et al.
Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels.
Jin and Lu
Citations for Tertiapin-Q
The citations listed below are publications that use Tocris products. Selected citations for Tertiapin-Q include:
10 Citations: Showing 1 - 10
Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels.
Authors: Patel Et al.
Transmural Autonomic Regulation of Cardiac Contractility at the Intact Heart Level.
Authors: Aguilar-Sanchez Et al.
Front Physiol 2019;10:773
Inactivation of GIRK channels weakens the pre- and postsynaptic inhibitory activity in dorsal raphe neurons.
Authors: Llamosas Et al.
Physiol Rep 2017;5
Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats.
Authors: Stott Et al.
Rapid antidepressants stimulate the decoupling of GABAB receptors from GIRK/Kir3 channels through increased protein stability of 14-3-3η.
Authors: Workman Et al.
Mol Psychiatry 2015;20:298
Phasic DA release drives rapid activation of striatal D2-receptors.
Authors: Marcott Et al.
Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro.
Authors: Chu Et al.
PLoS One 2013;8:e53863
Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart.
Authors: Choisy Et al.
PLoS One 2012;7:e33448
Acute desensitization of acetylcholine and endothelin-1 activated inward rectifier K+ current in myocytes from the cardiac atrioventricular node.
Authors: Choisy Et al.
Biochem Biophys Res Commun 2012;423:496
Sperm GIRK2-containing K+ inward rectifying channels participate in sperm capacitation and fertilization.
Authors: Yi Et al.
Syst Biol Reprod Med 2011;57:296
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Reviews for Tertiapin-Q
Average Rating: 5 (Based on 2 Reviews)
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We performed ex-vivo slice physiology and pre-incubated the slices in tertiapin-Q (200 nM). Pre-incubation blocked inward rectifying channels.
The product shows great Kir channel blocking properties even at very small cocentrations, the data was reproducible every time.