|
Receptor Modulator
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric modulators, and allosteric modulators, Examples of receptor modulators in modern medicine include CFTR modulators, selective androgen receptor modulators (SARMs), and muscarinic ACh receptor modulators. = General Description = Currently, receptor modulators are categorized in the Agonist, Partial Agonist, Selective Tissue Modulators, Antagonist, and Inverse Agonist categories in terms of the affect they cause. They are further divided into Orthosteric or Allosteric Modulators according to how they effect said ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and cause some form of cellular/tissue response, e.g. a change in the electrical activity of a cell. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Transmembrane receptors include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Blood Glucose
Glycaemia, also known as blood sugar level, blood sugar concentration, or blood glucose level is the measure of glucose concentrated in the blood of humans or other animals. Approximately 4 grams of glucose, a simple sugar, is present in the blood of a 70 kg (154 lb) human at all times. The body tightly regulates blood glucose levels as a part of metabolic homeostasis. Glucose is stored in skeletal muscle and liver cells in the form of glycogen; in fasting individuals, blood glucose is maintained at a constant level at the expense of glycogen stores in the liver and skeletal muscle. In humans, a blood glucose level of 4 grams, or about a teaspoon, is critical for normal function in a number of tissues, and the human brain consumes approximately 60% of blood glucose in fasting, sedentary individuals. A persistent elevation in blood glucose leads to glucose toxicity, which contributes to cell dysfunction and the pathology grouped together as complications of diabetes. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (for example, infection). Pharmacodynamics and pharmacokinetics are the main branches of pharmacology, being itself a topic of biology interested in the study of the interactions between both endogenous and exogenous chemical substances with living organisms. In particular, pharmacodynamics is the study of how a drug affects an organism, whereas pharmacokinetics is the study of how the organism affects the drug. Both together influence dosing, benefit, and adverse effects. Pharmacodynamics is sometimes abbreviated as PD and pharmacokinetics as PK, especially in combined reference (for example, when speaking of PK/PD models). Pharmacodynamics places particular emphasis on dose–response relationships, that is, the relationships betwe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Transporter Modulator
A reuptake modulator, or transporter modulator, is a type of drug which modulates the reuptake of one or more neurotransmitters via their respective neurotransmitter transporters. Examples of reuptake modulators include reuptake inhibitors (transporter blockers) and reuptake enhancers. See also * Releasing agent * Release modulator * Transporter substrate * Channel modulator * Enzyme modulator An enzyme modulator is a type of drug which modulates enzymes. They include enzyme inhibitors and enzyme inducers. In an homogeneous assay, "an enzyme modulator ... is covalently linked to the ligand which competes with free ligand from the test sam ... * Receptor modulator References Drugs by mechanism of action Psychopharmacology {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Modulator
An enzyme modulator is a type of drug which modulates enzymes. They include enzyme inhibitors and enzyme inducers. In an homogeneous assay, "an enzyme modulator ... is covalently linked to the ligand which competes with free ligand from the test sample for the available antibodies." See also * Channel modulator * Receptor modulator * Transporter modulator A reuptake modulator, or transporter modulator, is a type of drug which modulates the reuptake of one or more neurotransmitters via their respective neurotransmitter transporters. Examples of reuptake modulators include reuptake inhibitors (transp ... References Metabolism Enzyme inhibitors {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Channel Modulator
A channel modulator, or ion channel modulator, is a type of drug which modulates ion channels. They include channel blockers and channel openers. Direct modulators Ion channels are typically categorised by gating mechanism and by the ion they conduct. Note that an ion channel may overlap between different categories. Some channels conduct multiple ion currents and some are gated by multiple mechanisms. Examples of targets for modulators include: Voltage gated ion channels * Calcium channel: see also Calcium channel blocker, Calcium channel opener * Potassium channel: see also Potassium channel blocker, Potassium channel opener * Sodium channel: see also Sodium channel blocker, Sodium channel opener * Chloride channel: see also Chloride channel blocker, Chloride channel opener * Transient receptor potential channel) Ligand gated ion channels * 5-HT3: see also 5-HT3 antagonist, * GABAA receptor: see also GABA receptor agonist, GABA receptor antagonist * Glutamate rec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Obesity
Obesity is a medical condition, sometimes considered a disease, in which excess body fat has accumulated to such an extent that it may negatively affect health. People are classified as obese when their body mass index (BMI)—a person's weight divided by the square of the person's height—is over ; the range is defined as overweight. Some East Asian countries use lower values to calculate obesity. Obesity is a major cause of disability and is correlated with various diseases and conditions, particularly cardiovascular diseases, type 2 diabetes, obstructive sleep apnea, certain types of cancer, and osteoarthritis. Obesity has individual, socioeconomic, and environmental causes. Some known causes are diet, physical activity, automation, urbanization, genetic susceptibility, medications, mental disorders, economic policies, endocrine disorders, and exposure to endocrine-disrupting chemicals. While a majority of obese individuals at any given time are attemptin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hemopressin
Hemopressin (Hp) is an alpha hemoglobin fragment with the sequence PVNFKFLSH, originally identified in extracts of rat brain using an enzyme capture technique. It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors. Longer forms of hemopressin containing 2-3 additional amino acids on the N-terminus have been identified in extracts of mouse brain. These longer hemopressin peptides, named RVD-Hpα and VD-Hpα, bind to CB1 receptors and were originally reported to be agonists. In addition to the Hp peptides from alpha hemoglobin, a related peptide from beta hemoglobin has been found in mouse brain extracts; this peptide, named VD-Hpβ, is also an agonist at CB1 cannabinoid receptors. Hemopressin is not an endogenous peptide but rather an extraction artefact [Bauer M, Chicca A, Tamborrini M, Eisen D, Lerner R, Lutz B, Poetz O, Pluschke G, Gertsch J. Identification and quantification of a new family of peptide endocannabinoids (Pepcans) showing negative alloste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parkinson's Disease
Parkinson's disease (PD), or simply Parkinson's, is a long-term degenerative disorder of the central nervous system that mainly affects the motor system. The symptoms usually emerge slowly, and as the disease worsens, non-motor symptoms become more common. The most obvious early symptoms are tremor, rigidity, slowness of movement, and difficulty with walking. Cognitive and behavioral problems may also occur with depression, anxiety, and apathy occurring in many people with PD. Parkinson's disease dementia becomes common in the advanced stages of the disease. Those with Parkinson's can also have problems with their sleep and sensory systems. The motor symptoms of the disease result from the death of cells in the substantia nigra, a region of the midbrain, leading to a dopamine deficit. The cause of this cell death is poorly understood, but involves the build-up of misfolded proteins into Lewy bodies in the neurons. Collectively, the main motor symptoms are also k ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pimavanserin
Pimavanserin (ACP-103; BVF-036), sold under the brand name Nuplazid, is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis and is also being studied for the treatment of Alzheimer’s disease psychosis, schizophrenia, agitation, and major depressive disorder. Unlike other antipsychotics, pimavanserin is not a dopamine receptor antagonist. Pharmacology Pharmacodynamics Pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity ( Ki 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki 0.44 nM). Pimavanserin shows low binding to σ1 receptors (Ki 120 nM) and has no appreciable affinity (Ki >300 nM) to serotonin 5-HT2B, dopamine (including D2), muscarinic acetylcholine, histamine, or adrenergic receptors, or to calcium channels. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selecti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihistamine
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use. Although people typically use the word "antihistamine" to describe drugs for treating allergies, doctors and scientists use the term to describe a class of drug that opposes the activity of histamine receptors in the body. In this sense of the word, antihistamines are subclassified acco ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta Blocker
Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms, and to protect the heart from a second heart attack after a first heart attack ( secondary prevention). They are also widely used to treat high blood pressure, although they are no longer the first choice for initial treatment of most patients. Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response. Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 receptors. β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are located mainly in the lungs, gastrointestinal tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
.svg "Click for more on -> Receptor (biochemistry)")
