Target type: molecularfunction
Enables the transmembrane transfer of a cation by a channel that opens when intracellular cAMP has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport]
Intracellularly cAMP-activated cation channel activity represents a crucial molecular function in cellular signaling pathways. This activity is mediated by specific ion channels located within the cell membrane, which are activated by the intracellular messenger molecule cyclic adenosine monophosphate (cAMP). cAMP is produced in response to various extracellular stimuli, such as hormones and neurotransmitters, triggering a cascade of intracellular events that ultimately lead to the opening of these cation channels.
Upon activation, these channels allow the influx of positively charged ions, such as sodium (Na+), potassium (K+), and calcium (Ca2+), across the cell membrane. This influx alters the membrane potential and initiates downstream signaling pathways, ultimately influencing a wide range of cellular processes.
The molecular mechanism underlying this activity involves a complex interplay of protein interactions and conformational changes. cAMP binds to specific regulatory domains within the channel protein, triggering a conformational shift that opens the channel pore. This opening allows for the passage of cations, ultimately leading to the observed physiological effects.
The specific types of cations that can pass through these channels vary depending on the channel's structure and function. Some channels are selective for specific cations, while others allow the passage of multiple ions. The selectivity of the channel is determined by the size and charge of the ion, as well as the amino acid residues lining the channel pore.
Intracellularly cAMP-activated cation channel activity plays a vital role in a diverse array of physiological processes, including:
* **Neuromuscular transmission:** In the nervous system, these channels are crucial for synaptic transmission, where they mediate the release of neurotransmitters.
* **Cardiac function:** In the heart, these channels contribute to the regulation of heart rate and contractility.
* **Smooth muscle contraction:** In smooth muscle tissue, these channels regulate muscle contraction and relaxation.
* **Sensory transduction:** In sensory neurons, these channels participate in the detection of various stimuli, such as taste and smell.
Furthermore, dysregulation of intracellularly cAMP-activated cation channel activity has been implicated in various diseases, including cardiovascular disease, neurological disorders, and cancer. Understanding the molecular mechanisms underlying this activity is therefore critical for developing novel therapeutic strategies for these diseases.
In summary, intracellularly cAMP-activated cation channel activity is a fundamental cellular process that plays a crucial role in mediating the diverse physiological effects of cAMP signaling. Its molecular mechanisms involve specific ion channels that are activated by cAMP binding, leading to the influx of cations and subsequent downstream signaling pathways. This activity is involved in a wide range of cellular processes and has significant implications for human health.'
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Protein | Definition | Taxonomy |
---|---|---|
cGMP-gated cation channel alpha-1 | A cGMP-gated cation channel alpha-1 that is encoded in the genome of cow. [OMA:Q00194, PRO:DNx] | Bos taurus (cattle) |
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 | A potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q9Y3Q4] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
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 |
zatebradine | benzazepine | ||
ivabradine | ivabradine : A member of the class of benzazepines that is 7,8-dimethoxy-1,3,4,5-tetrahydro-3-benzazepin-2-one in which the amide hydrogen is replaced by a [{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl} group. Used (as its hydrochloride salt) to treat patients with angina who have intolerance to beta blockers and/or heart failure. Ivabradine: A benzazepine derivative and selective HYPERPOLARIZATION-ACTIVATED CYCLIC NUCLEOTIDE-GATED CHANNELS inhibitor that lowers the heart rate. It is used in the treatment of CHRONIC STABLE ANGINA in patients unable to take BETA-ADRENERGIC BLOCKERS, and in the treatment of HEART FAILURE. | aromatic ether; benzazepine; carbobicyclic compound; tertiary amino compound | cardiotonic drug |