Introduction
The control of smooth muscle tension, which is essential for physiological regulation of vascular resistance, involves a variety of ion channels. These channels include Ca2+-permeable channels such as Cav1.2, P2X4, nAChRα7, and most TRP channels. Additionally, there are channels that regulate the release of vasoactive substances and those that control arterial tone by managing membrane potential. The latter group includes K+-selective channels like BK, SK3, IK, Kir2.1, Kir6.1, Kir6.2, Kv1.5, and Kv7.1, as well as the non-selective channel TRPM4.
Under pathological conditions such as vascular inflammation, chronic hypertension, heart failure, or hypoxia, the vascular integrity may decrease, endothelial permeability may increase, and hyperplasia may occur, all of which can compromise vascular function. Certain ion channels play a role in these pathological mechanisms, including Kv7.1, nAChRα7, and several TRP channels.
Cardiovascular Ion Channel Portfolio
Our cardiac portfolio offers a comprehensive off-target profile of the principal ion channels that have an impact on physiological function of Cardiovascular system.
Recognizing the significance of these channels, our Cardiovascular Ion Channel Portfolio has been designed to include a selection of channels that are potential therapeutic targets for conditions like hypertension, atherosclerosis, and heart failure. It is important to note that dysfunction of these channels, potentially induced by drugs, may lead to adverse effects. This highlights the importance of understanding and profiling ion channels in the context of cardiovascular health and disease
Ion Channel Family | Target | Method | Species | Mode |
---|---|---|---|---|
Voltage-gated sodium channel | Nav1.5 | Manual patch clamp | human | Agonist or Antagonist |
Voltage-gated potassium channel | Kv1.3 | Manual patch clamp | human | Agonist or Antagonist |
Kv1.5 | Manual patch clamp | human | Agonist or Antagonist | |
hERG (Kv11.1) | Manual patch clamp | human | Agonist or Antagonist | |
Kv4.3 | Manual patch clamp | human | Agonist or Antagonist | |
Iks (Kv7.1) | Manual patch clamp | human | Agonist or Antagonist | |
Potassium channel, calcium activated | BK | Manual patch clamp | human | Agonist or Antagonist |
IK | Manual patch clamp | human | Agonist or Antagonist | |
Potassium channel, inward rectifier | Kir2.1 | Manual patch clamp | human | Agonist or Antagonist |
Kir3.1/3.4 (KAch, GIRK) | Manual patch clamp | human | Agonist or Antagonist | |
Kir6.2/Sur2A | Manual patch clamp | human | Agonist or Antagonist | |
Voltage-gated calcium channel | Cav1.2 | Manual patch clamp | human | Agonist or Antagonist |
Cav3.2 | Manual patch clamp | human | Agonist or Antagonist | |
Hyperpolarization-activated channel | HCN2 | Manual patch clamp | human | Agonist or Antagonist |
HCN4 | Manual patch clamp | human | Agonist or Antagonist | |
Transient receptor potential channel | TRPA1 | Manual patch clamp | human | Agonist or Antagonist |
TRPV1 | Manual patch clamp | human | Agonist or Antagonist | |
TRPV3 | Manual patch clamp | human | Agonist or Antagonist | |
TRPV4 | Manual patch clamp | human | Agonist or Antagonist | |
TRPM4 | Manual patch clamp | human | Agonist or Antagonist | |
TRPM8 | Manual patch clamp | human | Agonist or Antagonist | |
TRPC5 | Manual patch clamp | human | Agonist or Antagonist | |
TRPC6 | Manual patch clamp | human | Agonist or Antagonist | |
Ligand-gated ion channel | P2X1 | Manual patch clamp | human | Agonist or Antagonist |
P2X4 | Manual patch clamp | human | Agonist or Antagonist | |
P2X7 | Manual patch clamp | human | Agonist or Antagonist | |
nAChR α7/RIC3 | Manual patch clamp | human | Agonist or Antagonist |
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