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Adenosine Receptor Agonist
An adenosine receptor agonist is a drug which acts as an agonist of one or more of the adenosine receptors. Examples include the neurotransmitter adenosine, its phosphates, adenosine monophosphate (AMP), adenosine diphosphate (ADP), and adenosine triphosphate (ATP), and the pharmaceutical drug regadenoson. List of adenosine receptor agonists * ATL146e (A2A selective) * PD81,723 ( A1 allosteric enhancer) * CF102 (Adenosine A3 receptor) * Rosmarinic acid (A1 agonist) * 5′-(N-Ethylcarboxamido)adenosine (NECA) See also * Adenosine receptor antagonist * Adenosine reuptake inhibitor An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). Th ... References Drugs acting on the nervous system {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine A2A Receptor
The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. Structure This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as well as an extracellular N-terminus and an intracellular C-terminus. Furthermore, located in the intracellular side close to the membrane is a small alpha helix, often referred to as helix 8 (H8). The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin).; Below this primary ( orthosteric) binding pocket lies a secondary ( allosteric) binding pocket. The crystal-structure of A2A bound to the antagonist ZM241385 (PDB code: 4EIY) showed that a sodium-ion can be found in this location of the protein, thus giving it the name 'sodium-ion binding pocket'. Heteromers The actions of th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Reuptake Inhibitor
An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). This in turn leads to increased extracellular concentrations of adenosine and therefore an increase in adenosinergic neurotransmission. List of AdoRIs * Acadesine * Acetate * Barbiturates * Benzodiazepines * Calcium channel blockers * Carbamazepine * Carisoprodol * Cilostazol * Cyclobenzaprine * Dilazep * Dipyridamole * Estradiol * Ethanol * Flumazenil * Hexobendine * Hydroxyzine * Indomethacin * Inosine * KF24345 * Meprobamate * Nitrobenzylthioguanosine * Nitrobenzylthioinosine * Papaverine * Pentoxifylline * Phenothiazines * Phenytoin * Progesterone * Propentofylline * Propofol * Puromycin * R75231 * RE 102 BS * Soluflazine * Toyocamycin * Tracazolate * Tricyclic antidepressant Tricyclic antidepressants (TCAs) are a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Receptor Antagonist
An adenosine receptor antagonist is a drug which acts as an antagonist of one or more of the adenosine receptors. The best known are xanthines and their derivatives (natural: caffeine, theophylline, and theobromine; and synthetic: PSB-1901), but there are also non-xanthine representatives (e.g. ISAM-140, ISAM-R316, etrumadenant, and AZD-4635) See also * Adenosine receptor agonist * Adenosine reuptake inhibitor An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). Th ... References Drugs acting on the nervous system {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rosmarinic Acid
Rosmarinic acid, named after rosemary (''Salvia rosmarinus'' Spenn.), is a polyphenol constituent of many culinary herbs, including rosemary (''Salvia rosmarinus'' L.), perilla (''Perilla frutescens'' L.), sage (''Salvia officinalis'' L.), mint (''Mentha arvense'' L.), and basil (''Ocimum basilicum'' L.). History Rosmarinic acid was first isolated and characterized in 1958 by the Italian chemists Scarpatti and Oriente from rosemary ('' Salvia rosmarinus''), after which the acid is named. Chemistry Chemically, rosmarinic acid is a caffeic acid ester, with tyrosine providing another phenolic ring via dihydroxyphenyl-lactic acid. It has a molecular mass of 360 daltons. Natural occurrences Rosmarinic acid accumulation is shown in hornworts, in the fern family Blechnaceae, and in species of several orders of mono- and dicotyledonous angiosperms. It is found most notably in many Lamiaceae (dicotyledons in the order Lamiales), especially in the subfamily Nepetoideae. It is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine A3 Receptor
The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it. Function Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death. Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18). Gene Multiple transcript variants encoding different isoforms have been found for this gene. Therapeutic implications An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthriti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CF102
Namodenoson is a small molecule A3 adenosine receptor (A3AR) agonist. It is developed by Can-Fite for non-alcoholic fatty liver disease An alcohol-free or non-alcoholic drink, also known as a temperance drink, is a version of an alcoholic drink made without alcohol, or with the alcohol removed or reduced to almost zero. These may take the form of a non-alcoholic mixed drink or n ..., liver cancer, and pancreatic cancer. References {{reflist Adenosine receptor agonists Nucleosides Purines 3-Iodophenyl compounds Carboxamides Secondary amines Chloroarenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine A1 Receptor
The adenosine A1 receptor (A1AR) is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand. Biochemistry A1 receptors are implicated in sleep promotion by inhibiting wake-promoting cholinergic neurons in the basal forebrain. A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. Signaling Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an inhibition of adenylate cyclase and, therefore, a decrease in the cAMP concentration. An increase of the inositol triphosphate/ diacylglycerol concentration is caused by an activation of phospholipase C, whereas the elevated levels of arachidonic acid are mediated by DAG lipase, which cleaves DAG to form arachidonic acid. Several types of potassium channels are activated but N-, P-, and Q-type calc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
