sFTX-3.3 is a calcium ion channel antagonist, exhibiting IC50 values of approximately 0.24 mM and 0.70 mM against P-type and N-typechannels respectively.
Huwentoxin XVI TFA,一种来自鸟蛛 Ornithoctonus huwena 的止痛剂,一种高度可逆和选择性的哺乳动物 N 型钙通道 (N-typecalcium channel) (IC50约为 60 nM) 拮抗剂。Huwentoxin XVI TFA 对电压门控的 T 型钙通道,钾通道或钠通道没有影响。
N-Acyl taurines, such as N-lignoceroyl taurine, alongside various arachidonoyl amino acid conjugates like N-arachidonoyl dopamine and N-arachidonoyl-L-serine, have been identified in bovine brain and through mass spectrometry lipidomic studies in the brain and spinal cord of both wild-type and FAAH knockout mice. Notably, N-lignoceroyl taurine levels were found to be 23-26 times higher in FAAH knockout mice than in wild types, suggesting its degradation by FAAH, despite in vitro evidence showing FAAH hydrolyzes N-lignoceroyl taurine significantly slower than oleoyl ethanolamide. Additionally, N-acyl taurines with polyunsaturated acyl chains are known to activate TRPV1 and TRPV4 channels within the transient receptor potential (TRP) family of calciumchannels.
ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various transporters, L- and N-typecalciumchannels, K_ATP, and hERG potassium channels. However, it does inhibit the melatonin MT1 receptor by 61% at a 10 µM concentration.
Ziconotide TEA acts by binding to N-typecalciumchannels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.
Peptide neurotoxin; selectively and reversibly blocks N-typecalciumchannels (IC50 = 0.15 nM). Reduces (RS)-3,5-DHPG -induced long term depression in vivo.