Acefylline
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Acefylline
Acefylline (INN), also known as acetyloxytheophylline, is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation etanautine to help offset diphenhydramine induced drowsiness. A silanol–mannuronic acid conjugate of acefylline, ''acefylline methylsilanol mannuronate'' (INCI; trade name Xantalgosil C) is marketed as a lipolytic phosphodiesterase inhibitor. It is used as an ingredient in cosmeceuticals for the treatment of cellulite and as a skin conditioner. See also * 8-Chlorotheophylline * Theophylline * Caffeine Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class. It is mainly used recreationally as a cognitive enhancer, increasing alertness and attentional performance. Caffeine acts by blocking binding of adenosine to ... References Adenosine receptor antagonists Xanthines {{respiratory-system-drug-stub ...
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Mannuronic Acid
Mannuronic acid is a uronic acid monosaccharide that can be derived from mannose. Along with -guluronic acid, -mannuronic acid is a component of alginic acid, a polysaccharide found predominantly in brown algae Brown algae (singular: alga), comprising the class Phaeophyceae, are a large group of multicellular algae, including many seaweeds located in colder waters within the Northern Hemisphere. Brown algae are the major seaweeds of the temperate and p .... Mannuronic acid is also incorporated into some bacterial capsular polysaccharides. References Uronic acids {{organic-compound-stub ...
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Caffeine
Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class. It is mainly used recreationally as a cognitive enhancer, increasing alertness and attentional performance. Caffeine acts by blocking binding of adenosine to the adenosine A1 receptor, which enhances release of the neurotransmitter acetylcholine. Caffeine has a three-dimensional structure similar to that of adenosine, which allows it to bind and block its receptors. Caffeine also increases cyclic AMP levels through nonselective inhibition of phosphodiesterase. Caffeine is a bitter, white crystalline purine, a methylxanthine alkaloid, and is chemically related to the adenine and guanine bases of deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). It is found in the seeds, fruits, nuts, or leaves of a number of plants native to Africa, East Asia and South America, and helps to protect them against herbivores and from competition by preventing the germination of nearby seeds, as well as en ...
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Theophylline
Theophylline, also known as 1,3-dimethylxanthine, is a phosphodiesterase inhibiting drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the xanthine family, it bears structural and pharmacological similarity to theobromine and caffeine, and is readily found in nature, being present in tea (''Camellia sinensis'') and cocoa (''Theobroma cacao''). A small amount of theophylline is one of the products of caffeine metabolic processing in the liver. Medical uses The main actions of theophylline involve: * relaxing bronchial smooth muscle * increasing heart muscle contractility and efficiency (positive inotrope) * increasing heart rate (positive chronotropic) * increasing blood pressure * increasing renal blood flow * anti-inflammatory effects * central nervous system stimulatory effect mainly on the medullary respiratory center. The main therapeutic uses of theophylline are ...
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8-Chlorotheophylline
8-Chlorotheophylline, also known as 1,3-dimethyl-8-chloroxanthine, is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. Its main use is in combination (salt) with diphenhydramine in the antiemetic dimenhydrinate (Dramamine). Diphenhydramine reduces nausea but causes drowsiness, and the stimulant properties of 8-Chlorotheophylline help reduce that side effect. Despite being classified as a xanthine stimulant, 8-chlorotheophylline can generally not produce any locomotor activity above control in mice and does not appear to cross the blood-brain barrier well. The 8-chloro modification is not selected for pharmacological properties; instead, it was to raise the acidity of the xanthine amine group enough to form a co-salt with diphenhydramine.10.1126/science.109.2840.574.a The drug is also sold in combination with promethazine Promethazine is a first-generation antihistamine, antipsychotic, sedative, and antiemetic used to treat al ...
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Cellulite
Cellulite is the herniation of subcutaneous fat within fibrous connective tissue that manifests as skin dimpling and nodularity, often on the pelvic region (specifically the buttocks), lower limbs, and abdomen. Cellulite occurs in most postpubescent females. A review gives a prevalence of 85–98% of women, indicating that it is physiological rather than pathological. It can result from a complex combination of factors ranging from hormones to heredity. Causes The causes of cellulite include changes in metabolism, physiology, diet and exercise habits, obesity, sex-specific dimorphic skin architecture, alteration of connective tissue structure, hormonal factors, genetic factors, the microcirculatory system, the extracellular matrix, and subtle inflammatory alterations. Hormonal factors Hormones play a dominant role in the formation of cellulite. Estrogen may be the important hormone in the development of cellulite. However, there has been no reliable clinical evidence to sup ...
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Cosmeceutical
Cosmeceuticals are cosmetic products with bioactive ingredients purported to have medical benefits. In America, there are no legal requirements to prove that these products live up to their claims. The name is a portmanteau of "cosmetics" and "pharmaceuticals". Nutricosmetics are related dietary supplement or food or beverage products with additives that are marketed as having medical benefits that affect appearance. Quasi-drug (labelled 医薬部外品 or 薬用) is a Japanese term that refer to many of the same products with functional claims, albeit regulation is stronger as pre-market approval from the Ministry of Health, Labour and Welfare is required. Criticism Consumers are willing to pay a premium for skin and hair care products that they perceive as high-performance. The term "cosmeceutical" is often used in cosmetic advertising and may be misleading to the consumer. If the consumer interprets a "cosmeceutical" or "nutricosmetic" to be similar to a pharmaceutical p ...
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Phosphodiesterase Inhibitor
A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). The ubiquitous presence of this enzyme means that non-specific inhibitors have a wide range of actions, the actions in the heart, and lungs being some of the first to find a therapeutic use. History The different forms or subtypes of phosphodiesterase were initially isolated from rat brains in the early 1970s and were soon afterward shown to be selectively inhibited in the brain and in other tissues by a variety of drugs. The potential for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait. This prediction meanwhile has proved to be true in a variety of fields. Classification Nonselective PDE inhibitors Methy ...
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Lipolysis
Lipolysis is the metabolic pathway through which lipid triglycerides are hydrolyzed into a glycerol and free fatty acids. It is used to mobilize stored energy during fasting or exercise, and usually occurs in fat adipocytes. The most important regulatory hormone in lipolysis is insulin; lipolysis can only occur when insulin action falls to low levels, as occurs during fasting. Other hormones that affect lipolysis include glucagon, epinephrine, norepinephrine, growth hormone, atrial natriuretic peptide, brain natriuretic peptide, and cortisol. Mechanisms In the body, stores of fat are referred to as adipose tissue. In these areas, intracellular triglycerides are stored in cytoplasmic lipid droplets. When lipase enzymes are phosphorylated, they can access lipid droplets and through multiple steps of hydrolysis, breakdown triglycerides into fatty acids and glycerol. Each step of hydrolysis leads to the removal of one fatty acid. The first step and the rate-limiting step of l ...
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International Nomenclature Of Cosmetic Ingredients
The International Nomenclature of Cosmetic Ingredients, abbreviated INCI, are the unique identifiers for cosmetic ingredients such as waxes, oils, pigments, and other chemicals that are assigned in accordance with rules established by the Personal Care Products Council (PCPC), previously the Cosmetic, Toiletry, and Fragrance Association (CTFA). INCI names often differ greatly from systematic chemical nomenclature or from more common trivial names and is a mixture of conventional scientific names, Latin and English words. INCI nomenclature conventions "are continually reviewed and modified when necessary to reflect changes in the industry, technology, and new ingredient developments". INCI and CAS The relationship between a CAS Registry Number and an INCI name is not always one-to-one. In some cases, more than one INCI name may have the same CAS number, or more than one CAS number may apply to an INCI name. For example, the CAS number 1245638-61-2 has the CA Index Name of 2-Pr ...
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Silanol
A silanol is a functional group in silicon chemistry with the connectivity Si–O–H. It is related to the hydroxy functional group (C–O–H) found in all alcohols. Silanols are often invoked as intermediates in organosilicon chemistry and silicate mineralogy. If a silanol contains one or more organic residue, it is an organosilanol. Preparation From alkoxysilanes The first isolated example of a silanol was , reported in 1871 by Albert Ladenburg. He prepared the “silicol” by hydrolysis of (Et = ). From silyl halides and related compounds Silanols are generally synthesized by hydrolysis of halosilanes, alkoxysilanes, or aminosilanes. Chlorosilanes are the most common reactants: :R3Si–Cl + H2O → R3Si–OH + HCl The hydrolysis of fluorosilanes requires more forcing reagents, i.e. alkali. The alkoxysilanes (silyl ethers) of the type are slow to hydrolyze. Compared to the silyl ethers, silyl acetates are faster to hydrolyze, with the adv ...
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Stimulant
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or illicitly) as performance-enhancing or recreational drugs. Among narcotics, stimulants produce a noticeable crash or '' comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and prescription stimulants" (with "amphetamines" including amphetamine and methamphetamine) the value was 0.7%, an ...
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