SKF-38,393
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SKF-38,393
SKF-38393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/ D5 receptor partial agonist. It has stimulant and anorectic effects. The trimethylation of SKF-38,393 leads to a named agent called Trepipam. As with fenoldopam the inclusion of a chlorine halogen gave an agent that is called SKF-81,297 SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/ D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self-administration in animals .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Drugs developed by GSK plc D1 receptor agonists D5 receptor agonists Catechols {{gastrointestinal-drug-stub ...
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Benzazepine
Benzazepines are heterocyclic chemical compounds consisting of a benzene ring fused to an azepine ring. Examples include: File:Benazepril structure.svg, Benazepril File:Fenoldopam.svg, Fenoldopam File:GSK-189,254.svg, GSK-189,254 File:Ivabradine 2.svg, Ivabradine File:Semagacestat structure.svg, Semagacestat File:Varenicline.svg, Varenicline File:Trepipam.svg, Trepipam File:SKF38393.svg, SKF-38,393 See also * Benzodiazepine * Dibenzazepine Dibenzazepine (iminostilbene) is a chemical compound with two benzene functional group, rings fused to an azepine ring (chemistry), ring. Many pharmaceuticals, such as carbamazepine, oxcarbazepine, and depramine, are based on a dibenzazepine struc ... References {{Heterocyclic-stub ...
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Chemical Synthesis
Chemical synthesis (chemical combination) is the artificial execution of chemical reactions to obtain one or several products. This occurs by physical and chemical manipulations usually involving one or more reactions. In modern laboratory uses, the process is reproducible and reliable. A chemical synthesis involves one or more compounds (known as '' reagents'' or ''reactants'') that will experience a transformation under certain conditions. Various reaction types can be applied to formulate a desired product. This requires mixing the compounds in a reaction vessel, such as a chemical reactor or a simple round-bottom flask. Many reactions require some form of processing (" work-up") or purification procedure to isolate the final product. The amount produced by chemical synthesis is known as the '' reaction yield''. Typically, yields are expressed as a mass in grams (in a laboratory setting) or as a percentage of the total theoretical quantity that could be produced based ...
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Trepipam
Trepipam (; developmental code name SCH-12679) is a dopamine receptor agonist of the benzazepine group that was never marketed. It acts specifically as an agonist of the dopamine D1 receptor. It is closed related structurally to fenoldopam, a peripherally acting selective D1 receptor partial agonist which is used as an antihypertensive agent Antihypertensives are a class of medication, drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke, heart failure, kidney failure and myo .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Abandoned drugs Benzazepines D1 receptor agonists Peripherally selective drugs {{drug-stub ...
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D1 Receptor Agonists
D1, D01, D.I, D.1 or D-1 can refer to: Science and technology Biochemistry and medicine * ATC code D01 ''Antifungals for dermatological use'', a subgroup of the Anatomical Therapeutic Chemical Classification System * Dopamine receptor D1, a protein * Haplogroup D1 (Y-DNA) * Vitamin D1, a form of Vitamin D * DI, Iodothyronine deiodinase type I, an enzyme involved with thyroid hormones Technology * Nikon D1, a digital single-lens reflex camera * D1, former brand of T-Mobile in Germany * D1, an abbreviation for DOCSIS 1.0 1.0, an international telecommunications standard * D-1 (Sony), an early digital video recording format * STS-61-A, also known as D-1, the 22nd mission of NASA's Space Shuttle program * D-1, from the Proton (rocket family), Russian rockets * Mercedes D.I, a 1913 German aircraft engine Military World War I fighter aircraft * AEG D.I * Albatros D.I * Halberstadt D.I, experimental version of Halberstadt D.II (and Aviatik D.I variant) * Aviatik (Berg) D.I * ...
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Drugs Developed By GSK Plc
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 inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or 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 treat, cure, prevent, or 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 regular basis for chronic disorders. Classification Pharmaceutical drugs are often classified into drug classes—groups of related drugs that hav ...
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SKF-81,297
SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/ D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self-administration in animals. This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958, but not with certain other D1 full agonists such as A-77,636, reflecting functional selectivity Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the end ... of D1 activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers. One of the patented uses for SKF-81,297 is as an augmentation agent when combined with an appropriate choice of an antidepressant.Akinori Nishi, et al. WO2012127871 (Kurume University, Nip ...
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Fenoldopam
Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is used as an antihypertensive agent. It was approved by the Food and Drug Administration (FDA) in September 1997. Indications Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis. Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitant chronic kidney disease. It can cause reflex tachycardia, but it is dependent on the infusion of the drug. Pharmacology Fenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D1 receptors. It decreases afterload and also promotes sodium excretion via specific dopamine receptors along the nephron. The renal effect of fenoldopam and dopamine may invo ...
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Stimulant
Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, Mood disorder, mood, and physical activity, physical performance. Some stimulants occur naturally, while others are exclusively synthetic. Common stimulants include caffeine, nicotine, amphetamines, cocaine, methylphenidate, and modafinil. Stimulants may be subject to varying forms of regulation, or outright prohibition, depending on jurisdiction. Stimulants increase activity in the sympathetic nervous system, either directly or indirectly. Prototypical stimulants increase synaptic concentrations of neurotransmitter, excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the Receptor (biochemistry), receptors of excitatory neurotransmitters (e.g., nicotine) or by ...
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Anorectic
An anorectic is a drug that reduces appetite, resulting in lower food consumption, leading to weight loss. These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desire to eat. The understanding of anorexiant effects is crucial in the development of interventions for weight management, eating disorders, and related health concerns. The anorexiant effect can be induced through diverse mechanisms, ranging from hormonal regulation to neural signaling. Ghrelin, leptin, and peptide YY are among the hormones involved in appetite control. Additionally, neurotransmitters such as serotonin and dopamine in the central nervous system contribute significantly to the regulation of food intake. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek and ), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term ...
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Chemical Compound
A chemical compound is a chemical substance composed of many identical molecules (or molecular entities) containing atoms from more than one chemical element held together by chemical bonds. A molecule consisting of atoms of only one element is therefore not a compound. A compound can be transformed into a different substance by a chemical reaction, which may involve interactions with other substances. In this process, bonds between atoms may be broken or new bonds formed or both. There are four major types of compounds, distinguished by how the constituent atoms are bonded together. Molecular compounds are held together by covalent bonds; ionic compounds are held together by ionic bonds; intermetallic compounds are held together by metallic bonds; coordination complexes are held together by coordinate covalent bonds. Non-stoichiometric compounds form a disputed marginal case. A chemical formula specifies the number of atoms of each element in a compound molecule, usin ...
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Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (biochemistry), ligands which display both agonistic and Receptor antagonist, antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspi ...
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