Target type: molecularfunction
Enables the transmembrane transfer of a potassium ion by an open rectifier voltage-gated channel. An open rectifier current-voltage relationship is one in which the direction of rectification depends on the external potassium ion concentration. [GOC:mah, PMID:8917578]
Open rectifier potassium channels are a family of voltage-gated potassium channels that exhibit a unique characteristic: they open more readily when the membrane potential is depolarized, allowing potassium ions to flow out of the cell. This outward current contributes to the repolarization of the membrane potential, playing a crucial role in the regulation of neuronal excitability and other physiological processes. The molecular mechanism underlying this "open rectifier" property is attributed to a specific structural feature of the channel pore. The pore is lined by positively charged amino acid residues, which attract potassium ions from the intracellular side of the membrane. As the membrane potential becomes more positive, the electrostatic attraction between the pore and potassium ions increases, facilitating the opening of the channel. This mechanism effectively allows for more efficient potassium efflux during depolarization, thus contributing to the repolarizing current. Open rectifier potassium channels are found in a variety of tissues, including the nervous system, heart, and skeletal muscle. They are involved in numerous physiological processes, such as action potential propagation, neurotransmitter release, and muscle contraction. In neurons, open rectifier potassium channels are crucial for shaping the action potential waveform, contributing to its repolarization and the establishment of the refractory period. This helps to ensure that action potentials propagate in a unidirectional manner, preventing backpropagation. In the heart, open rectifier potassium channels play a role in the regulation of heart rate and contractility. They contribute to the repolarization of the action potential in cardiac muscle cells, affecting the duration of the refractory period and the timing of subsequent contractions. In skeletal muscle, open rectifier potassium channels contribute to the regulation of muscle relaxation. They help to repolarize the membrane potential of muscle cells, allowing for the relaxation of the muscle fibers after contraction.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Potassium channel subfamily K member 3 | A potassium channel subfamily K member 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O14649] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| bupivacaine | 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline. bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic. Bupivacaine: A widely used local anesthetic agent. | aromatic amide; piperidinecarboxamide; tertiary amino compound | |
| lidocaine | lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE. | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| mepivacaine | mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic. Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168) | piperidinecarboxamide | drug allergen; local anaesthetic |
| mexiletine | mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties. | aromatic ether; primary amino compound | anti-arrhythmia drug |
| propafenone | propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| tetracaine | tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia. Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia. | benzoate ester; tertiary amino compound | local anaesthetic |
| etidocaine | etidocaine : An amino acid amide in which 2-[ethyl(propyl)amino]butanoic acid and 2,6-dimethylaniline have combined to form the amide bond. Used as a local anaesthetic (amide caine), it has rapid onset and long action properties, similar to bupivacaine, and is given by injection during surgical procedures and during labour and delivery. Etidocaine: A local anesthetic with rapid onset and long action, similar to BUPIVACAINE. | amino acid amide | local anaesthetic |
| ropivacaine | (S)-ropivacaine : A piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond. ropivacaine : The piperidinecarboxamide obtained by the formal condensation of N-propylpipecolic acid and 2,6-dimethylaniline. Ropivacaine: An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons. | piperidinecarboxamide; ropivacaine | local anaesthetic |
| (2'-(benzyloxycarbonylaminomethyl)biphenyl-2-carboxylic acid 2-(2-pyridyl)ethylamide) | biphenyls | ||
| anandamide | anandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine. | endocannabinoid; N-acylethanolamine 20:4 | human blood serum metabolite; neurotransmitter; vasodilator agent |
| am-356 | methanandamide: structure given in first source; RN given refers to (all-Z)-(+-)-isomer | fatty amide | |
| ave 0118 | |||
| a 1899 | A 1899: a TASK-1 potassium channel blocker; structure in first source |