741738-57-8
Chemical Structure
Phrixotoxin 2
- CAS No.: 741738-57-8
- Formula:C169H259N49O43S8
- Molecular Weight:3921.69
SMILES: O=C([C@@H](N)CC1=CC=C(O)C=C1)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]2CSSC[C@H](NC3=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CCSC)=O)CC(N)=O)=O)[C@H](CC)C)=O)[C@H](CC)C)=O)CCCNC(N)=N)=O)CCCCN)=O)=O)CCCCN)=O)CCCNC(N)=N)=O)CCC(O)=O)=O)CCC(O)=O)=O)CC(O)=O)=O)CSSC[C@H](NC4=O)C(N[C@H](C(N[C@H](C(N[C@H]3CC5=CNC6=CC=CC=C56)=O)CC(C)C)=O)CCCNC(N)=N)=O)=O)[C@@H](C)O)=O)CC7=CNC8=CC=CC=C78)=O)CCSC)=O)CC9=CNC%10=CC=CC=C9%10)=O)CCCCN)=O)CCC(N)=O)=O)CSSC[C@H](NC2=O)C(N[C@H](C(NCC(N[C@H](C(N[C@H]4C(C)C)=O)CC(C)C)=O)=O)CCC(O)=O)=O
Biological Activity: Phrixotoxin 2 is a Kv4 family potassium channel inhibitor, with Ki values in rats of 120 nM for Kv4.2, 110 nM for Kv4.3, and 230 nM for Kv4.1. Phrixotoxin 2 mediates voltage-dependent inhibition of Kv4.2 and Kv4.3 currents, and voltage-independent inhibition of Kv4.1 currents. Phrixotoxin 2 fails to inhibit A-type K+ currents in visceral dorsal root ganglion neurons. Phrixotoxin 2 induces contraction of non-pregnant uterine smooth muscle and triggers orofacial cold hyperalgesia in rats. Phrixotoxin 2 can distinguish the contribution of Kv4 subunits to A-type K+ currents in different subsets of sensory neurons. Phrixotoxin 2 can be used in research related to chronic pain and trigeminal neuropathic pain[1][2][3].
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Phrixotoxin 2 | Phrixotoxin 2 is a Kv4 family potassium channel inhibitor, with Ki values in rats of 120 nM for Kv4.2, 110 nM for Kv4.3, and 230 nM for Kv4.1. Phrixotoxin 2 mediates voltage-dependent inhibition of Kv4.2 and Kv4.3 currents, and voltage-independent inhibition of Kv4.1 currents. Phrixotoxin 2 fails to inhibit A-type K+ currents in visceral dorsal root ganglion neurons. Phrixotoxin 2 induces contraction of non-pregnant uterine smooth muscle and triggers orofacial cold hyperalgesia in rats. Phrixotoxin 2 can distinguish the contribution of Kv4 subunits to A-type K+ currents in different subsets of sensory neurons. Phrixotoxin 2 can be used in research related to chronic pain and trigeminal neuropathic pain. | |||||||||||||||||||||
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References
- [1]. Yunoki T, et al. Differential contribution of Kv4-containing channels to A-type, voltage-gated potassium currents in somatic and visceral dorsal root ganglion neurons. J Neurophysiol. 2014 Nov 15;112(10):2492-504. [Content Brief]
- [2]. Smith RC, et al. The role of voltage-gated potassium channels in the regulation of mouse uterine contractility. Reproductive biology and endocrinology : RB&E. 2007 Nov 02;5:41. [Content Brief]
- [3]. Kanda H, et al. Kv4.3 Channel Dysfunction Contributes to Trigeminal Neuropathic Pain Manifested with Orofacial Cold Hypersensitivity in Rats. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2021 Mar 10;41(10):2091-2105. [Content Brief]
