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Benzazepines
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 Benzodiazepines (BZD, BDZ, BZs), colloquially known as "benzos", are a class of central nervous system (CNS) depressant, depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed t ... * Dibenzazepine References {{Heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azepine
Azepine is unsaturated heterocycle of seven atoms, with a nitrogen replacing a carbon at one position. The atoms are numbered starting with the nitrogen. The 1H form shown to the right is unstable and converts to the 3H form. See also * * * Diazepine *Oxepin
Oxepine is an oxygen-containing heterocycle consisting of a seven-membered ...
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Varenicline
Varenicline, sold under the brand names Chantix and Champix among others, is a medication used for smoking cessation and for the treatment of dry eye syndrome. It is a nicotinic acetylcholine receptor partial agonist. When activated, this receptor leads to the release of dopamine in the nucleus accumbens, the brain's reward center, thereby reducing cravings and withdrawal symptoms with smoking cessation, although less pronounced than a full agonist (e.g. nicotine). Common side effects include nausea, insomnia, abnormal dreams, headache, and nasopharyngitis ( inflammation of the nose and throat). Despite these potential adverse effects, varenicline has proven efficacy in helping individuals quit smoking. It is estimated that approximately one in eleven smokers who use varenicline successfully remain abstinent from tobacco at six months. It is on the World Health Organization's List of Essential Medicines. The medication is available as a generic medication. In the United Stat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocyclic Compound
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of py ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzene
Benzene is an Organic compound, organic chemical compound with the Chemical formula#Molecular formula, molecular formula C6H6. The benzene molecule is composed of six carbon atoms joined in a planar hexagonal Ring (chemistry), ring with one hydrogen atom attached to each. Because it contains only carbon and hydrogen atoms, benzene is classed as a hydrocarbon. Benzene is a natural constituent of petroleum and is one of the elementary petrochemicals. Due to the cyclic continuous pi bonds between the carbon atoms, benzene is classed as an aromatic hydrocarbon. Benzene is a colorless and highly Combustibility and flammability, flammable liquid with a sweet smell, and is partially responsible for the aroma of gasoline. It is used primarily as a Precursor (chemistry), precursor to the manufacture of chemicals with more complex structures, such as ethylbenzene and cumene, of which billions of kilograms are produced annually. Although benzene is a major Chemical industry, industrial che ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benazepril
Benazepril, sold under the brand name Lotensin among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure. It is taken by mouth. Versions are available as the combinations benazepril/hydrochlorothiazide and benazepril/amlodipine. Common side effects include feeling tired, dizziness, cough, and light-headedness with standing. Serious side effects may include kidney problems, low blood pressure, high blood potassium, and angioedema. Use in pregnancy may harm the baby, while use when breastfeeding may be safe. It is an ACE inhibitor and works by decreasing renin-angiotensin-aldosterone system activity. Benazepril was patented in 1981 and came into medical use in 1990. It is available as a generic medication. In 2022, it was the 159th most commonly prescribed medication in the United States, with more than 3million prescriptions. Medical uses Lotensin is indicate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK-189,254
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor ( Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuo ... which do not respond well to conventional analgesic drugs. References ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ivabradine
Ivabradine, sold under the brand name Procoralan among others, is a medication, which is a pacemaker current (I''f'') inhibitor, used for the symptomatic management of heart-related chest pain and heart failure. Patients who qualify for use of ivabradine for congestive heart failure are patients who have symptomatic heart failure, with reduced ejection fraction, and heart rate at least 70 bpm, and the condition not able to be fully managed by beta blockers. Ivabradine acts by allowing negative chronotropy in the sinoatrial structure, thus reducing the heart rate via specific inhibition of the pacemaker current. It operates by a mechanism different from that of beta blockers and calcium channel blockers, which are two commonly prescribed antianginal classes of cardiac drugs. Ivabradine has no apparent inotropic properties and may be a cardiotonic agent. Medical uses It is used for the symptomatic treatment of chronic stable angina pectoris in patients with normal sinus rhythm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semagacestat
Semagacestat (LY-450139) was a candidate drug for a causal therapy against Alzheimer's disease. It was originally developed by Eli Lilly and Elan, and clinical trials were conducted by Eli Lilly. Phase III trials included over 3000 patients, but in August 2010, a disappointing interim analysis, in which semagacestat performed worse than the placebo, led to the trials being stopped. Mechanism of action β-Amyloid is a peptide of 39 to 43 amino acids. The isoforms with 40 and 42 amino acids (Aβ40/42) are the main constituents of amyloid plaques in the brains of Alzheimer's disease patients. β-Amyloid is formed by proteolysis of amyloid precursor protein (APP). Research on laboratory rats suggest that the soluble form of this peptide is a causative agent in the development of Alzheimer's. Semagacestat blocks the enzyme γ-secretase, which (along with β-secretase) is responsible for APP proteolysis. Clinical trials Phase III double-blind clinical trials started in March 2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
