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BRL-32872
BRL-32872 is an experimental drug candidate that provides a novel approach to the treatment of cardiac arrhythmia. Being a derivative of verapamil, it possesses the ability to inhibit Ca+2 membrane channels. Specific modifications in hydrogen bonding activity, nitrogen lone pair availability, and molecular flexibility allow BRL-32872 to inhibit K+ channels as well. As such, BRL-32872 is classified as both a class III (K+ blocking) and class IV (Ca+2 blocking) antiarrhythmic agent. Arrhythmia Cardiac arrhythmia arises from abnormalities in action potential formation and propagation through the heart. Changes in electrolyte balance, or development of ectopic pacemaker activity, disrupt normal heart rhythmicity and conduction. Antiarrhythmic agents are used to manipulate ion flux through membrane channels to restore normal pacemaker activity. Cellular conduction and refractory periods are also modified to eliminate re-entry depolarization causing arrhythmia. Factors contributing to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrochloride
In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (e.g. an amine). An alternative name is chlorhydrate, which comes from French. An archaic alternative name is muriate, derived from hydrochloric acid's ancient name: muriatic acid. Uses Converting amine In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent su ...s into their hydrochlorides is a common way to improve their water solubility, which can be desirable for substances used in medications. The European Pharmacopoeia lists more than 200 hydrochlorides as active ingredients in medications. These hydrochlorides, compared to free bases, may more readily dissolve in the gastrointestinal tract and be absorbed into the bloodstream more quickly. A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Membrane Channel
Membrane channels are a family of biological membrane proteins which allow the passive movement of ions (ion channels), water ( aquaporins) or other solutes to passively pass through the membrane down their electrochemical gradient. They are studied using a range of channelomics experimental and mathematical techniques. Insights have suggested endocannabinoids (eCBs) as molecules that can regulate the opening of these channels during diverse conditions. Properties Hemichannels A hemichannel is a membrane channel made up of six subunits. A hemichannel is defined as one-half of a gap junction channel. Hemichannels consist of connexins. Pannexin Pannexins are involved in the process of purinergic signalling. They release adenosine triphosphate (ATP), which activate purinergic receptors. On the other hand, purinergic receptor activation can also lead to the opening of the channel, via a positive feedback loop. In addition, P2Y receptor P2Y receptors are a family ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fibrillation
Fibrillation is the rapid, irregular, and unsynchronized contraction of muscle fibers. An important occurrence is with regard to the heart. Cardiology There are two major classes of cardiac fibrillation: atrial fibrillation and ventricular fibrillation. * Atrial fibrillation is an irregular and uncoordinated contraction of the cardiac muscle of atria. It can be a chronic condition, usually treated with anticoagulation and sometimes with conversion to normal sinus rhythm. In this condition the normal electrical pulses coming from the sinoatrial node are overwhelmed by disorganized electrical impulses usually originating in the roots of the pulmonary veins, leading to irregular conduction of impulses to the ventricles which generate the heartbeat. * Ventricular fibrillation is an irregular and uncoordinated contraction of the cardiac muscle of ventricles. It is a common cause of cardiac arrest and is usually fatal if not reversed by defibrillation. Fibrillation may sometime ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachycardia
Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal (such as with exercise) or abnormal (such as with electrical problems within the heart). Complications Tachycardia can lead to fainting. When the rate of blood flow becomes too rapid, or fast blood flow passes on damaged endothelium, it increases the friction within vessels resulting in turbulence and other disturbances. According to the Virchow's triad, this is one of the three conditions that can lead to thrombosis (i.e., blood clots within vessels). Causes Some causes of tachycardia include: * Adrenergic storm * Anaemia * Anxiety * Atrial fibrillation * Atrial flutter * Atrial tachycardia * Atrioventricular reentrant tachycardia * AV nodal reentrant tachycardia * Brugada syndrome * Circulatory shock and its various ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradycardia
Bradycardia (also sinus bradycardia) is a slow resting heart rate, commonly under 60 beats per minute (BPM) as determined by an electrocardiogram. It is considered to be a normal heart rate during sleep, in young and healthy or elderly adults, and in athletes. In some people, bradycardia below 60 BPM may be associated with fatigue, weakness, dizziness, sweating, and fainting. The term "relative bradycardia" is used to refer to a heart rate slower than an individual's typical resting heart rate. Athletes may have athletic heart syndrome, which includes bradycardia as part of the cardiovascular adaptations to training and participation. The word "bradycardia" is from the Greek βραδύς ''bradys'' "slow", and καρδία ''kardia'' "heart". Classification Sinus Atrial bradycardias are divided into three types. The first, respiratory sinus arrhythmia, is usually found in young and healthy adults. Heart rate increases during inhalation and decreases during exhalation. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acidosis
Acidosis is a process causing increased acidity in the blood and other body tissues (i.e., an increase in hydrogen ion concentration). If not further qualified, it usually refers to acidity of the blood plasma. The term ''acidemia'' describes the state of low blood pH, while ''acidosis'' is used to describe the processes leading to these states. Nevertheless, the terms are sometimes used interchangeably. The distinction may be relevant where a patient has factors causing both acidosis and alkalosis, wherein the relative severity of both determines whether the result is a high, low, or normal pH. Acidemia is said to occur when arterial pH falls below 7.35 (except in the fetus – see below), while its counterpart (alkalemia) occurs at a pH over 7.45. Arterial blood gas analysis and other tests are required to separate the main causes. The rate of cellular metabolic activity affects and, at the same time, is affected by the pH of the body fluids. In mammals, the normal pH of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypoxia (medical)
Hypoxia is a condition in which the body or a region of the body is deprived of adequate oxygen supply at the tissue level. Hypoxia may be classified as either '' generalized'', affecting the whole body, or ''local'', affecting a region of the body. Although hypoxia is often a pathological condition, variations in arterial oxygen concentrations can be part of the normal physiology, for example, during strenuous physical exercise.. Hypoxia differs from hypoxemia and anoxemia, in that hypoxia refers to a state in which oxygen present in a tissue or the whole body is insufficient, whereas hypoxemia and anoxemia refer specifically to states that have low or no oxygen in the blood. Hypoxia in which there is complete absence of oxygen supply is referred to as anoxia. Hypoxia can be due to external causes, when the breathing gas is hypoxic, or internal causes, such as reduced effectiveness of gas transfer in the lungs, reduced capacity of the blood to carry oxygen, compromised gene ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ischemia
Ischemia or ischaemia is a restriction in blood supply to any tissue, muscle group, or organ of the body, causing a shortage of oxygen that is needed for cellular metabolism (to keep tissue alive). Ischemia is generally caused by problems with blood vessels, with resultant damage to or dysfunction of tissue i.e. hypoxia and microvascular dysfunction. It also implies local hypoxia in a part of a body resulting from constriction (such as vasoconstriction, thrombosis, or embolism). Ischemia causes not only insufficiency of oxygen, but also reduced availability of nutrients and inadequate removal of metabolic wastes. Ischemia can be partial (poor perfusion) or total blockage. The inadequate delivery of oxygenated blood to the organs must be resolved either by treating the cause of the inadequate delivery or reducing the oxygen demand of the system that needs it. For example, patients with myocardial ischemia have a decreased blood flow to the heart and are prescribed wit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cardiac Rhythmicity
Cardiac rhythmicity is the spontaneous depolarization and repolarization event that occurs in a repetitive and stable manner within the cardiac muscle. Rhythmicity is often abnormal or lost in cases of cardiac dysfunction or cardiac failure. It is the ability of the heart to maintain a relatively stable relation between its systole and diastole Diastole ( ) is the relaxed phase of the cardiac cycle when the chambers of the heart are re-filling with blood. The contrasting phase is systole when the heart chambers are contracting. Atrial diastole is the relaxing of the atria, and ventri .... Not increasing one on the expense of the other. However, external factors may lead to the disruption of the heart's rhythmicity. References * PhysioEx 6.0 by Peter Zao, Timothy Stabler, Greta Peterson, Lori Smith Cardiac electrophysiology {{circulatory-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Verapamil
Verapamil, sold under various trade names, is a calcium channel blocker medication used for the treatment of high blood pressure, angina (chest pain from not enough blood flow to the heart), and supraventricular tachycardia. It may also be used for the prevention of migraines and cluster headaches. It is given by mouth or by injection into a vein. Common side effects include headache, low blood pressure, nausea, and constipation. Other side effects include allergic reactions and muscle pains. It is not recommended in people with a slow heart rate or heart failure. It is believed to cause problems for the fetus if used during pregnancy. It is in the non–dihydropyridine calcium channel blocker family of medications. Verapamil was approved for medical use in the United States in 1981. It is on the World Health Organization's List of Essential Medicines. Verapamil is available as a generic medication. Long acting formulations exist. In 2020, it was the 151st most ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Electrolyte
An electrolyte is a medium containing ions that is electrically conducting through the movement of those ions, but not conducting electrons. This includes most soluble salts, acids, and bases dissolved in a polar solvent, such as water. Upon dissolving, the substance separates into cations and anions, which disperse uniformly throughout the solvent. Solid-state electrolytes also exist. In medicine and sometimes in chemistry, the term electrolyte refers to the substance that is dissolved. Electrically, such a solution is neutral. If an electric potential is applied to such a solution, the cations of the solution are drawn to the electrode that has an abundance of electrons, while the anions are drawn to the electrode that has a deficit of electrons. The movement of anions and cations in opposite directions within the solution amounts to a current. Some gases, such as hydrogen chloride (HCl), under conditions of high temperature or low pressure can also function as elect ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Action Potential
An action potential occurs when the membrane potential of a specific cell location rapidly rises and falls. This depolarization then causes adjacent locations to similarly depolarize. Action potentials occur in several types of animal cells, called excitable cells, which include neurons, muscle cells, and in some plant cells. Certain endocrine cells such as pancreatic beta cells, and certain cells of the anterior pituitary gland are also excitable cells. In neurons, action potentials play a central role in cell-cell communication by providing for—or with regard to saltatory conduction, assisting—the propagation of signals along the neuron's axon toward synaptic boutons situated at the ends of an axon; these signals can then connect with other neurons at synapses, or to motor cells or glands. In other types of cells, their main function is to activate intracellular processes. In muscle cells, for example, an action potential is the first step in the chain of event ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
