| Identification | Back Directory | [Name]
Tertiapin Q | [CAS]
910044-56-3 | [Synonyms]
Teriapin Q
L-Lysinamide, L-alanyl-L-leucyl-L-cysteinyl-L-asparaginyl-L-cysteinyl-L-asparaginyl-L-arginyl-L-isoleucyl-L-isoleucyl-L-isoleucyl-L-prolyl-L-histidyl-L-glutaminyl-L-cysteinyl-L-tryptophyl-L-lysyl-L-lysyl-L-cysteinylglycyl-L-lysyl-, cyclic (3→14),(5→18)-bis(disulfide) | [Molecular Formula]
C106H175N35O24S4 | [MDL Number]
MFCD02684419 | [MOL File]
910044-56-3.mol | [Molecular Weight]
2452 |
| Chemical Properties | Back Directory | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [form ]
Solid | [color ]
White to off-white | [Water Solubility ]
Soluble in water (2mg/ml) | [Sequence]
Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18) |
| Hazard Information | Back Directory | [Uses]
Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1). | [Biochem/physiol Actions]
Blocks the GIRK1/4 and ROMK1 members of the inward-rectifier K+ channel family. | [in vivo]
Tertiapin-Q is a muscarinic acetylcholine receptor-operated K+ current (IK,Ach) blocker. After the cessation of rapid atrial pacing, the atrial effective refractory period (AERP) is unchanged during the experimental period in the rapid atrial pacing (RAP) rabbits (n=6). Bepridil (1 mg/kg, n=5 for each group), Amiodarone (10 mg/kg, n=5 for each group), Vernakalant (3 mg/kg, n=5 for each group), Ranolazine (10 mg/kg, n=6 for each group) or Tertiapin-Q (0.03 mg/kg, n=5 for each group) on the AERP in the control and RAP rabbits. Tertiapin-Q significantly prolongs the AERP at each pacing cycle length both in the control and RAP rabbits. The extents of prolonging effect of Tertiapin-Q on the AERP in the RAP rabbits are greater than those in the control animals[3]. | [storage]
-20°C (desiccate) | [References]
[1] Picton LD, et al. Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Sci Rep. 2016 Oct 20;6:35749. DOI:10.1038/srep35749
[2] Günther T, et al. Research Resource: Real-Time Analysis of Somatostatin and Dopamine Receptor Signaling in Pituitary Cells Using a Fluorescence-Based Membrane Potential Assay. Mol Endocrinol. 2016 Apr;30(4):479-90. DOI:10.1210/me.2015-1241
[3] Chiba T, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6. DOI:10.1016/j.jphs.2016.02.007 |
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