A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.
Histamine H1 Antagonists
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.
Receptors, Histamine H3
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Receptors, Histamine H2
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Drug Delivery Systems
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
The application of scientific knowledge or technology to pharmacy and the pharmaceutical industry. It includes methods, techniques, and instrumentation in the manufacture, preparation, compounding, dispensing, packaging, and storing of drugs and other preparations used in diagnostic and determinative procedures, and in the treatment of patients.
Quantitative Structure-Activity Relationship
Encyclopedias as Topic
Health Facility Merger
Histamine H2 Antagonists
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Myelin Proteolipid Protein
A myelin protein that is the major component of the organic solvent extractable lipoprotein complexes of whole brain. It has been the subject of much study because of its unusual physical properties. It remains soluble in chloroform even after essentially all of its bound lipids have been removed. (From Siegel et al., Basic Neurochemistry, 4th ed, p122)
This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).
A rare, slowly progressive disorder of myelin formation. Subtypes are referred to as classic, congenital, transitional, and adult forms of this disease. The classic form is X-chromosome linked, has its onset in infancy and is associated with a mutation of the proteolipid protein gene. Clinical manifestations include TREMOR, spasmus nutans, roving eye movements, ATAXIA, spasticity, and NYSTAGMUS, CONGENITAL. Death occurs by the third decade of life. The congenital form has similar characteristics but presents early in infancy and features rapid disease progression. Transitional and adult subtypes have a later onset and less severe symptomatology. Pathologic features include patchy areas of demyelination with preservation of perivascular islands (trigoid appearance). (From Menkes, Textbook of Child Neurology, 5th ed, p190)
An indirect sympathomimetic effect of burimamide on kitten isolated atria. (1/24)1. Burimamide (34-1080 muM) caused a concentration-dependent increase in the force and frequency of contraction of kitten isolated atria. 2. Metiamide (467 muM) had no stimulant action on kitten atria and did not modify the effects of burimamide. 3. The atrial stimulation produced by burimamide was reduced by (-)propranolol (34-68 nM) and by cocaine (3 muM). 4. The atrial stimulant effect of burimamide was prevented by pretreatment of kittens with reserpine (1 mg/kg, 24 h before the experiment). 5. It is concluded that burimamide causes atrial stimulation by releasing catecholamines. (+info)
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. (2/24)Agonist-independent activity of G-protein-coupled receptor, also referred to as constitutive activity, is a well-documented phenomenon and has been reported recently for both the histamine H(1) and H(2) receptors. Using SK-N-MC cell lines stably expressing the human and rat H(3) receptors at physiological receptor densities (500-600 fmol/mg of protein), we show that both the rat and human H(3) receptors show a high degree of constitutive activity. The forskolin-mediated cAMP production in SK-N-MC cells is inhibited strongly upon expression of the G(i)-coupled H(3) receptor. The cAMP production can be further inhibited upon agonist stimulation of the H(3) receptor and can be enhanced by a variety of H(3) antagonists acting as inverse agonists at the H(3) receptor. Thioperamide, clobenpropit, and iodophenpropit raise the cAMP levels in SK-N-MC cells with potencies that match their receptor binding affinities. Surprisingly, impentamine and burimamide act as effective H(3) agonists. Modification of the amine group of impentamine dramatically affected the pharmacological activity of the ligand. Receptor affinity was reduced slightly for most impentamine analogs, but the functional activity of the ligands varied from agonist to neutral antagonist and inverse agonist, indicating that subtle changes in the chemical structures of impentamine analogs have major impact on the (de)activation steps of the H(3) receptor. In conclusion, upon stable expression of the rat and human H(3) receptor in SK-N-MC cells constitutive receptor activity is detected. In this experimental system, H(3) receptors ligands, previously identified as H(3) antagonists, cover the whole spectrum of pharmacological activities, ranging from full inverse agonists to agonists. (+info)
The role of H1 and H2-receptors in the coronary vascular response to histamine of isolated perfused hearts of guinea-pigs and rabbits. (3/24)1. The effects of histamine on the isolated perfused hearts of guinea-pigs and rabbits were examined. Records of contractile force, heart rate and coronary perfusion pressure were obtained. 2. Histamine exerted positive inotropic and chronotropic effects which were antagonized by burimamide and attributed to stimulation of H2-receptors. 3. The coronary vascular response to histamine differed between guinea-pigs and rabbits. In guinea-pig hearts, three phases were apparent: (a) An initial vasodilatation preceding any effects on heart force and rate was antagonized by mepyramine and therefore mediated by histamine H1-receptors in the coronary circulation. (b) A secondary vasoconstriction was attributed to the increased myocardial compression during the positive inotropic and chronotropic responses. (c) The final, more predominant, component was a prolonged vasodilatation probably associated with the increased metabolic activity of the heart. 4. The latter two components were abolished together with the myocardial responses by burimamide. The remaining coronary vascular response was biphasic, consisting of a vasodilatation immediately followed by vasoconstriction. Both were antagonized by mepyramine and therefore mediated by H1-receptors. 5. The coronary vascular response of rabbit hearts was similar but no direct vasodilatation was observed and it was concluded that histamine receptors in the coronary vasculature involve only vasoconstriction. (+info)
Inhibition of sympathetic hypertensive responses in the guinea-pig by prejunctional histamine H3-receptors. (4/24)1. The effect of (R)-alpha-methylhistamine, a selective H3-histamine receptor agonist, was examined on the neurogenic hypertension and tachycardia that is induced by stimulation of areas in the medulla oblongata of guinea-pigs. Electrical medullary stimulation (32 Hz, 3-5 s trains, 0.5-1.0 ms square pulse, 25-400 microA) produced intensity-dependent increases in blood pressure and a more variable tachycardia. 2. (R)-alpha-methylhistamine inhibited the hypertension and tachycardia due to submaximal CNS stimulation. The inhibition of hypertension by (R)-alpha-methylhistamine was dose-dependent (10-300 micrograms kg-1, i.v.) and was not seen at high intensities of stimulation. 3. (R)-alpha-methylhistamine (300 micrograms kg-1, i.v.) did not attenuate the pressor response to adrenaline (1 and 3 micrograms kg-1, i.v.), indicating that the effect of (R)-alpha-methylhistamine was not mediated by a postjunctional action on smooth muscle. 4. The inhibition of CNS-induced hypertension by (R)-alpha-methylhistamine (300 micrograms kg-1, i.v.) was blocked by the H3 antagonists, thioperamide (ID50 = 0.39 mg kg-1, i.v.), impromidine (ID50 = 0.22 mg kg-1, i.v.) and burimamide (ID50 = 6 mg kg-1, i.v.). The rank order potency of these antagonists is consistent with activity at the H3B receptor subtype. Chlorpheniramine (30 micrograms kg-1, i.v.) and cimetidine (3 mg kg-1, i.v.) did not antagonize the inhibition of CNS-hypertension by (R)-alpha-methylhistamine. 5. These results suggest that (R)-alpha-methylhistamine inhibits sympathetic hypertensive responses in guinea-pigs by activation of prejunctional H3-receptors, possibly located on postganglionic nerve terminals. Furthermore, on the basis of the rank order potency to different H3-antagonists, it appears that the H3B-receptor subtype is involved with H3-receptor responses on vascular sympathetic nerves. (+info)
Effects of the histamine H2-receptor blocking drugs burimamide and cimetidine on noradrenergic transmission in the isolated aorta of the rabbit and atria of the guinea-pig. (5/24)1 In rabbit aortic strips, concentration-response curves to noradrenaline (NA) were shifted to the right in a parallel and concentration-dependent manner by the alpha-adrenoceptor blocking drug, phentolamine and also by the histamine H(2)-receptor blocking drugs, burimamide and cimetidine. Responses to 5-hydroxytryptamine were not affected by these drugs.2 Burimamide had the properties of a competitive antagonist of noradrenaline, possessing about one-hundredth the potency of phentolamine. Cimetidine was weaker than burimamide and did not fulfil the requirements for competitive antagonism of noradrenaline.3 In guinea-pig isolated atria, in which noradrenergic transmitter stores were labelled with [(3)H]-noradrenaline, phentolamine (3 muM), burimamide (30 muM) and cimetidine (30 muM), in decreasing order of effectiveness, each enhanced stimulation-induced efflux of [(3)H]-noradrenaline, indicating that their blocking effects on prejunctional alpha-adrenoceptors in this tissue are in the same order of relative potency as on postjunctional alpha-adrenoceptors in rabbit aortic strips.4 In the concentrations used (30 muM), neither burimamide nor cimetidine interfered with the neuronal uptake of noradrenaline. Burimamide, and to a much lesser extent, cimetidine, increased the resting efflux of [(3)H]-noradrenaline from guinea-pig atria.5 The effect of clonidine, a partial agonist on prejunctional alpha-adrenoceptors in guinea-pig atria, in increasing stimulation-induced efflux of [(3)H]-noradrenaline when stimulated with 150 pulses at 5 Hz was blocked by cimetidine (30 muM) and reversed by phentolamine (3 muM) and burimamide (30 muM). (+info)
The effects of burimamide and metiamide on basal gastric function in the cat. (6/24)1 Burimamide injected intravenously in the anaesthetized or conscious cat produced significant increases in gastric acid secretion: in the anaesthetized cat it produced increased gastric mucosal blood flow. 2 Metiamide, in doses which inhibited pentagastrin-stimulated acid secretion, produced no increase in gastric acid secretion in conscious animals, or gastric acid secretion or gastric mucosal blood flow in the anaesthetized cat. 3 Metiamide did not influence the amount of acid which diffused out of the stomach when instilled at pH values between 1.5 and 6.0. 4 The possible mode of action of burimamide in increasing basal gastric secretion is discussed. (+info)
Interaction of histamine H1-and H2-receptor antagonists with histamine uptake and metabolism by guinea-pig isolated atrium and mouse neoplastic mast cells cells in vitro. (7/24)1. Burimamide, metiamide, chlorpheniramine, triprolidine and cocaine, were tested as inhibitors of histamine uptake and metabolism in the guinea-pig atrium and in mouse neoplastic mast cells. 2. Cocaine did not affect the uptake and metabolism of histamine, either in the atrium or in the mast cells. All the antihistamines tested blocked the uptake and metabolism of histamine in both preparations. The order of potency was burimamide greater than chlorpheniramine greater than triprolidine greater than metiamide in the atrium; and burimamide greater than metiamide greater than triprolidine greater than chlorpheniramine, in the mase cells. 3. Comparison of the present results with the antihistamine activity of these blocking agents suggests that no correlation exists between the receptor blocking activity and the ability of these substances to act as inhibitors of histamine uptake and metabolism. (+info)
The possible roles of histamine, 5-hydroxytryptamine and prostaglandin F2alpha as mediators of the acute pulmonary effects of endotoxin. (8/24)1 In an attempt to investigate the possible role of released vasoactive substances in mediating the pulmonary pressor responses to E. coli endotoxin, cats were pretreated with histamine, 5-hydroxytryptamine (5-HT) or prostaglandin antagonists, with a histamine depleting agent (compound 48/80) or with an inhibitor of prostaglandin synthetase (sodium meclofenamate).2 The administration of endotoxin (2 mg/kg) resulted in a rapidly developing pulmonary hypertension (pressure twice normal after 2-3 min), increases in right atrial and intratracheal pressures, systemic hypotension and bradycardia. These effects were unaffected by methysergide in a dose sufficient to prevent the effects of intravenously administered 5-HT.3 Endotoxin responses were also unaffected by a combination of mepyramine and burimamide in doses sufficient to reduce markedly the effects of intravenously-administered histamine. In cats pretreated (chronically or acutely) with compound 48/80, endotoxin induced a transient pulmonary pressor response which was not maintained.4 The pulmonary and systemic responses to endotoxin were prevented by the prior administration of the prostaglandin antagonist, polyphloretin phosphate and by pretreatment with the prostaglandin synthetase inhibitor, sodium meclofenamate.5 It is concluded that a pulmonary vasoconstrictor prostaglandin is involved in the acute response to endotoxin in the cat. (+info)
Specific inhibition by burimamide of histamine effects on myocardial contraction and cyclic AMP | SpringerLink
1. In the isolated perfused guinea-pig heart, the increases in isotonic contraction and in cyclic AMP, produced by 2 μg of histamine were significantly and almost completely inhibited in the presence...
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The H3-histamine receptor provides feedback inhibition of histamine synthesis and release as well as inhibition of other neurotransmitter release. We have characterized this receptor by radioligand binding studies with the H3 agonist N alpha-[3H]methylhistamine ([3H]NAMHA). The results of [3H]NAMHA saturation binding and NAMHA inhibition of [3H]NAMHA binding were consistent with an apparently single class of receptors (KD = 0.37 nM, Bmax = 73 fmol/mg of protein) and competition assays with other agonists and the antagonists impromidine and dimaprit disclosed only a single class of sites. In contrast, inhibition of [3H]NAMHA binding by the specific high affinity H3 antagonist thioperamide revealed two classes of sites (KiA = 5 nM, BmaxA = 30 fmol/mg of protein; KiB = 68 nM, BmaxB = 48 fmol/mg of protein). Burimamide, another antagonist that, like thioperamide, contains a thiourea group, likewise discriminated between two classes of sites. In addition to differences between some antagonist ...
Sensory responses of human skin to synthetic histamine analogues and histamine
The potential for itch production in human skin of the synthetic analogues of histamine, 2-methyl histamine (an H1-receptor agonist) and 4-methyl histamine and dimaprit (H2-receptor agonists) has been studied in vivo and compared with histamine. Itch thresholds for 2-methyl histamine were consistent …
ベタヒスチン and breastfeeding. Are they compatible?
Histamine analogue drug which is used for treatment of Menieres vertigo At latest update, relevant information on excretion into breast milk was not found. Because of pharmacokinetic data it is likely excretion into breast milk though from low plasma levels, usually below the detection threshold (100 pg/mL) Side-effects likely would be mild: nausea, dyspepsia, head ache. Consider other better known options, otherwise follow-up the child for symptoms like nausea, crying and fussiness.
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Effect of metiamide on basal and stimulated serum cholecystokinin levels in duodenal ulcer patients. | Gut
Serum cholecystokinin (CCK) levels were measured in 10 patients with chronic duodenal ulcers, fasting and at intervals after two standard tests meals (300 ml of 40 mmol/1 phenylalanine solution), one given before and one during H2-receptor blockade with metiamide (200 mg four times a day). Fasting serum CCK levels were lower in all patients during treatment with metiamide (the mean level falling from 306-0 +/- 102-0 (SEM) to 82-1 +/- 23-6 pg/ml after treatment (p less than 0-01)). In contrast, peak serum CCK levels after the meal were not significantly different (7400 +/- 1141 pg/ml before treatment and 7569 +/- 1293 pg/ml on metiamide). We conclude that in duodenal ulcer patients CCK secretion under basal condtions may be in part dependent on stimulation of the small intestinal mucosa by gastric acid, but that, after an amino acid meal, gastric acid secretion is less important in determining the amount of CCK released.. ...
Burimamide is 100 times more potent than Nα-guanylhistamine, proving its efficacy on the H2 receptor. The potency of burimamide ... From this lead, the receptor model was further refined, which eventually led to the development of burimamide, a specific ...
C. Robin Ganellin
However, it was soon realised that burimamide was not an appropriate oral medicine. They quickly identified a similar drug, ... The end result of their trials was cimetidine, an H2-receptor antagonist superior to both burimamide and metiamide. The ... Initially, the team developed burimamide as a potential H2-receptor antagonist for medicinal use. ...
... is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate ... the following steps were undertaken to stabilize burimamide: addition of a sulfide group close to the imidazole ring, giving ... to the H2 receptor These changes increased the bioavailability metiamide so that it is ten times more potent than burimamide in ... compound in the development of the successful anti-ulcer drug cimetidine (Tagamet). After discovering that burimamide is ...
Chemoreceptor trigger zone
... burimamide and metiamide. Recent studies have found that phosphodiesterase 4 (PDE4) inhibitors, such as Rolipram, cause emesis ...
Burimamide, a specific competitive antagonist at the H2 receptor, 100 times more potent than Nα-guanylhistamine, proved the ... Burimamide was still insufficiently potent for oral administration, and further modification of the structure, based on ... From this lead, the receptor model was further refined and eventually led to the development of burimamide, the first H2 ...
Histamine H3 receptor
Burimamide (also weak H2 antagonist) Ciproxifan Clobenpropit (also H4 antagonist) Conessine Failproxifan (No ...
... is an antagonist at the H2 and H3 histamine receptors. It is largely inactive as an H2 antagonist at physiological ... Burimamide was first developed by scientists at Smith, Kline & French (SK&F; now GlaxoSmithKline) in their intent to develop a ... The discovery of burimamide ultimately led to the development of cimetidine (Tagamet). Metiamide Cimetidine Clayden, Jonathan; ...
... (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine. A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment. In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist. It produces antidepressant-like effects in rats. However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus. This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus. ...
... was first prepared as AH19065 by John Bradshaw in the summer of 1977 in the Ware research laboratories of Allen & Hanburys, part of the Glaxo organization. Its development was a response to the first in class histamine H2 receptor antagonist, cimetidine, developed by Sir James Black at Smith, Kline and French, and launched in the United Kingdom as Tagamet in November 1976. Both companies would eventually become merged as GlaxoSmithKline following a sequence of mergers and acquisitions starting with the integration of Allen & Hanbury's Ltd and Glaxo to form Glaxo Group Research in 1979, and ultimately with the merger of Glaxo Wellcome and SmithKline Beecham in 2000. Ranitidine was the result of a rational drug-design process using what was by then a fairly refined model of the histamine H2 receptor and quantitative structure-activity relationships. Glaxo refined the model further by replacing the imidazole ring of cimetidine with a furan ring with a nitrogen-containing ...
As of 2017 brands included: Actalor, Actidin, Aerotina, Alaspan, Alavert, Albatrina, Alerdina, Alerfast, Alergan, Alergiano, Alergiatadina, Alergin Ariston, Alergipan, Alergit, Alergitrat L, Aleric Lora, Alermuc, Alernitis, Alerpriv, Alertadin, Alertine, Aleze, Algac, Algecare, Algistop, Alledryl, Aller-Tab, Allerfre, Allerget, Allergex Non Drowsy, Allergyx, Allerhis, Allernon, Allerta, Allertyn, Allohex, Allor, Allorat, Alloris, Alor, Analor, Anhissen, Anti-Sneeze, Antial, Antil, Antimin, Ao Hui Feng, Ao Mi Xin, Ao Shu, Ardin, Atinac, Avotyne, Axcel Loratadine, Bai Wei Le, Bang Nuo, Bedix, Belodin, Benadryl, Besumin, Bi Sai Ning, Bi Yan Tong, Biliranin, Biloina, Biolorat, Bollinol, Boots Hayfever Relief, Boots Hooikoortstabletten, Boots Once-a-Day Allergy Relief, Carin, Carinose, Chang Ke, Civeran, Clara, Claratyne, Clarid, Clarihis, Clarihist, Clarilerg, Clarinese, Claritin, Claritine, Clarityne, Clarityne SP, Clarotadine, Clatatin, Clatine, Clear-Atadine, Clear-Atadine Children's, Clistin, ...
... (Serentil) is a piperidine neuroleptic drug belonging to the class of drugs called phenothiazines, used in the treatment of schizophrenia. It is a metabolite of thioridazine. The drug's name is derived from the methylsulfoxy and piperidine functional groups in its chemical structure. It has central antiadrenergic, antidopaminergic, antiserotonergic and weak muscarinic anticholinergic effects. Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome. Mesoridazine was withdrawn from the United States market in 2004 due to dangerous side effects, namely irregular heart beat and QT-prolongation of the electrocardiogram. It currently appears to be unavailable worldwide. ...
... is widely used in preparations as an enhancing agent for some analgesics and antitussives (acetaminophen, dihydrocodeine, codeine, hydrocodone). It is widely used in certain parts of the world as cough suppressant usually with codeine, and sometimes by itself or in addition to dextromethorphan as it, like diphenhydramine, possesses antitussive action of its own and is particularly useful in semi-productive coughs because of its moderate drying action. Phenyltoloxamine has analgesic and anti-spasmodic properties of its own and is used in combination with paracetamol, aspirin and other salicylates and other drugs in proprietary preparations available over the counter for backache, muscle strains and similar conditions. In this respect, it is similar to a closely related antihistamine, orphenadrine, and both drugs are very closely related to diphenhydramine and to doxylamine, the latter of which is the active ingredient in NyQuil and many other cough ...
When both imidazole ring nitrogens are protonated, their 15N chemical shifts are similar (about 200 ppm, relative to nitric acid on the sigma scale, on which increased shielding corresponds to increased chemical shift). NMR shows that the chemical shift of N1-H drops slightly, whereas the chemical shift of N3-H drops considerably (about 190 vs. 145 ppm). This indicates that the N1-H tautomer is preferred, it is presumed due to hydrogen bonding to the neighboring ammonium. The shielding at N3 is substantially reduced due to the second-order paramagnetic effect, which involves a symmetry-allowed interaction between the nitrogen lone pair and the excited π* states of the aromatic ring. As the pH rises above 9, the chemical shifts of N1 and N3 become approximately 185 and 170 ppm. An entirely deprotonated form of the imidazole ring, the imidazolate ion, would be formed only above a pH of 14, and is therefore not physiologically relevant. This change in chemical shifts can be explained by the ...
Brand names include Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, Triftazin. In the United Kingdom and some other countries, trifluoperazine is sold and marketed under the brand 'Stelazine'. The drug is sold as tablet, liquid and 'Trifluoperazine-injectable USP' for deep intramuscular short-term use. GP studying pharmacological data has indicated cases of neck vertebrae irreversible fusing leading to NHS preparations being predominantly of the liquid form trifluoperazine as opposed to the tablet form as in Stela zine etc. In the past, trifluoperazine was used in fixed combinations with the MAO inhibitor (antidepressant) tranylcypromine (tranylcypromine/trifluoperazine) to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom N. Likewise a combination with amobarbital (potent sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac. In ...
In the United States, Seldane was brought to market in 1985 as the first nonsedating antihistamine for the treatment of allergic rhinitis. In June 1990, evidence of serious ventricular arrhythmias among those taking Seldane prompted the FDA to issue a report on the risk factors associated with concomitant use of the drug with macrolide antibiotics and ketoconazole. Two months later, the FDA required the manufacturer to send a letter to all physicians, alerting them to the problem; in July 1992, the existing precautions were elevated to a black box warning and the issue attracted mass media attention in reports that people with liver disease or who took ketoconazole, an antifungal agent, or the antibiotic erythromycin, could suffer cardiac arrhythmia if they also took Seldane. In January 1997, the same month when the U.S. Food and Drug Administration (FDA) had earlier approved a generic version of Seldane made by IVAX Corporation of Miami, the FDA recommended terfenadine-containing ...
... (INN, USAN, codenamed AH25352) is a long-acting competitive H2 receptor antagonist which was under development as an antiulcerant by Glaxo (now GlaxoSmithKline). It was planned to be a follow-up compound to ranitidine (Zantac). When taken in doses of 600 mg twice daily it induced virtually 24-hour gastric anacidity thus closely resembling the antisecretory effect of the proton pump inhibitor omeprazole. Its development was terminated in 1989 from phase III clinical trials based on the appearance of carcinoid tumors in long-term toxicity testing in rodents. ...
Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. Journal of Pharmacology and Experimental Therapeutics. 2007 Jun;321(3):1032-45. PMID 17327487 ...
... is an antihistamine and anticholinergic of the pyridine chemical class which was developed in the early 1950s. It was sold under the trade names Co-Pyronil and Histadyl EC. It has relatively strong sedative effects, to the extent that its primary use was as a medication for insomnia rather than for its antihistamine action. Together with scopolamine, it was the main ingredient in Sominex, Nytol, and Sleep-Eze. It also provided the sedative component of Excedrin PM. All of these products were reformulated in the late 1970s when methapyrilene was demonstrated to cause liver cancer in rats when given chronically. ...
... , sold under the brand name Azafen or Azaphen, is an antidepressant approved in Russia for the treatment of depression. It was introduced in the late 1960s and is still used today. Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin. In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity. Other properties such as anticholinergic or antiadrenergic actions are less clear but are likely. ...
It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus by limiting the activity of the vestibular hair cells which send signals about movement. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness could be a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception, but the true evolutionary reason for this malady is currently unknown. When prescribed for balance problems and vertigo, cinnarizine is typically taken two or three times daily depending on the amount of each dose and when used to treat motion sickness, the pill is taken at least two hours before travelling and then again every four hours during travel. However, a recent 2012 study comparing the ...
As of 2017, loratadine was available under many brand names and dosage forms worldwide, including several combination drug formulations with pseudoephedrine, paracetamol, betamethasone, ambroxol, salbutamol, phenylephrine, and dexamethasone. As of 2017[update] brands included: Actalor, Actidin, Aerotina, Alaspan, Alavert, Albatrina, Alerdina, Alerfast, Alergan, Alergiano, Alergiatadina, Alergin Ariston, Alergipan, Alergit, Alergitrat L, Aleric Lora, Alermuc, Alernitis, Alerpriv, Alertadin, Alertine, Aleze, Algac, Algecare, Algistop, Alledryl, Aller-Tab, Allerfre, Allerget, Allergex Non Drowsy, Allergyx, Allerhis, Allernon, Allerta, Allertyn, Allohex, Allor, Allorat, Alloris, Alor, Analor, Anhissen, Anti-Sneeze, Antial, Antil, Antimin, Ao Hui Feng, Ao Mi Xin, Ao Shu, Ardin, Atinac, Avotyne, Axcel Loratadine, Bai Wei Le, Bang Nuo, Bedix, Belodin, Benadryl, Besumin, Bi Sai Ning, Bi Yan Tong, Biliranin, Biloina, Biolorat, Bollinol, Boots Hayfever Relief, Boots Hooikoortstabletten, Boots ...
组氨酸脱羧酶 - 维基百科，自由的百科
Burimamide（英语：Burimamide）. *Ciproxifan（英语：Ciproxifan）. *Clobenpropit（英语：Clobenpropit） ...
হিস্টামিন - উইকিপিডিয়া
Windaus এবং Vogt ১৯০৭ সালে প্রথম সংশ্লেষণ দ্বারা হিস্টামিন সংশ্লেষণ করেন, তখনও হিস্টামিন যে জীবিত প্রাণী দেহে পাওয়া যায় তা আবিষ্কৃত হয়নি। ১৯১০ সালে Barger এবং Dale প্রথম ইস্ট থেকে হিস্টামিন নিষ্কাষন করেন এবং প্রব্ররতীতে প্রাণীদেহে এর ভুমিকা আবিষ্কার ক্রেন। ১৬২৭ সালে বেষ্ট ও তার সহকর্মীরা যক্রত কোষ ও ফুসফুস কোষ হতে হিস্টামিন নিষ্কাষন করেন। একই বছরে আরেকজন গবেষক লুইস প্রমান করেন হিস্টামিন ...
সিনারিজিন - উইকিপিডিয়া
Pianese, C. P.; Hidalgo, L. O.; Gonz??Lez, R. H.; Madrid, C. E.; Ponce, J. E.; Ram??Rez, A. M.; Mor??n, L. M.; Arenas, J. E.; Rubio, A. T.; Uribe, J. O.; Abiuso, J. ?; Hanuch, E.; Alegr??a, J.; Volpi, C.; Flaskamp, R.; Sanju??n, A. P. ?A.; g??Mez, J. M. G. ?A.; Hern??Ndez, J.; Pedraza, A.; Quijano, D.; Mart??Nez, C.; Casta??Eda, J. R. ?N.; Guerra, O. J. C. ?O.; f, G. V. (২০০২)। "New approaches to the management of peripheral vertigo: Efficacy and safety of two calcium antagonists in a 12-week, multinational, double-blind study"। Otology & neurotology : official publication of the American Otological Society, American Neurotology Society \and] European Academy of Otology and Neurotology। 23 (3): 357-363। doi:10.1097/00129492-200205000-00023। PMID 11981396 ...
Burimamide - Wikipedia
Burimamide is an antagonist at the H2 and H3 histamine receptors. It is largely inactive as an H2 antagonist at physiological ... Burimamide was first developed by scientists at Smith, Kline & French (SK&F; now GlaxoSmithKline) in their intent to develop a ... The discovery of burimamide ultimately led to the development of cimetidine (Tagamet). Metiamide Cimetidine Clayden, Jonathan; ...
Specific inhibition by burimamide of histamine effects on myocardial contraction and cyclic AMP | SpringerLink
Heart-Contraction Cyclic AMP Histamine Burimamide This work was supported by grant Nr. 1301 of the Fonds zur Förderung der ... Specific inhibition by burimamide of histamine effects on myocardial contraction and cyclic AMP. ... produced by 2 μg of histamine were significantly and almost completely inhibited in the presence of 2 mg of burimamide, whereas ... Inhibition of the cardiac effects of histamine on contraction and cyclic AMP by burimamide. Naunyn-Schmiedebergs Arch. ...
Category:Thioureas - Wikimedia Commons
Blockade by burimamide of the effects of clonidine on cardiac contractility phosphorylase activation and cyclic adenosine...
Animals , Burimamide/pharmacology , Clonidine/antagonists & inhibitors , Cyclic AMP/analysis , Dose-Response Relationship, Drug ... Blockade by burimamide of the effects of clonidine on cardiac contractility phosphorylase activation and cyclic adenosine ... Clonidine-induced biochemical and mechanical effects were blocked by burimamide, an H2-receptor antagonist Propranolol (1 x 10 ... Blockade by burimamide of the effects of clonidine on cardiac contractility phosphorylase ...
HRH4 Gene - GeneCards | HRH4 Protein | HRH4 Antibody
The Histamine H3 Receptor: Structure, Pharmacology, and Function | Molecular Pharmacology
JCI - Volume 55, Issue 4
H2 antagonist - Wikipedia
STP : main GiPCRs
Characterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands. - PubMed - NCBI
WO1995011894A1 - Histamine h3-receptor antagonists and therapeutic uses thereof - Google Patents
US6537525B1 - Medicated chewing-gum - Google Patents
Asthma - Allergy - nmmra.org
3H]-thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex. - PubMed - NCBI
Patent US4449983 - Simultaneous delivery of two drugs from unit delivery device - Google Patents
Urticaria/Angioedema | SpringerLink
Doença do refluxo gastroesofágico: tratamento não farmacológico
Captodiame - Wikipedia
Captodiame (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine. A 2004 study suggested captodiame may be helpful in preventing benzodiazepine withdrawal syndrome in people discontinuing benzodiazepine treatment. In addition to its actions as an antihistamine, captodiamine has been found to act as a 5-HT2C receptor antagonist and σ1 receptor and D3 receptor agonist. It produces antidepressant-like effects in rats. However, captodiamine is unique among antidepressant-like drugs in that it increases brain-derived neurotrophic factor (BDNF) levels in the hypothalamus but not in the frontal cortex or hippocampus. This unique action may be related to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor (CRF) signaling in the hypothalamus. ...
Ranitidine - Wikipedia
Ranitidine was first prepared as AH19065 by John Bradshaw in the summer of 1977 in the Ware research laboratories of Allen & Hanburys, part of the Glaxo organization. Its development was a response to the first in class histamine H2 receptor antagonist, cimetidine, developed by Sir James Black at Smith, Kline and French, and launched in the United Kingdom as Tagamet in November 1976. Both companies would eventually become merged as GlaxoSmithKline following a sequence of mergers and acquisitions starting with the integration of Allen & Hanburys Ltd and Glaxo to form Glaxo Group Research in 1979, and ultimately with the merger of Glaxo Wellcome and SmithKline Beecham in 2000. Ranitidine was the result of a rational drug-design process using what was by then a fairly refined model of the histamine H2 receptor and quantitative structure-activity relationships. Glaxo refined the model further by replacing the imidazole ring of cimetidine with a furan ring with a nitrogen-containing ...
ranitidine - meddic
Certain preparations of ranitidine are available over the counter (OTC) in various countries. In the United States, 75-mg and 150-mg tablets are available OTC. Zantac OTC is manufactured by Boehringer Ingelheim. In Australia, packs containing seven or 14 doses of the 150-mg tablet are available in supermarkets, small packs of 150-mg and 300-mg tablets are schedule 2 pharmacy medicines. Larger doses and pack sizes still require a prescription.. Outside the United States and Canada, ranitidine is combined with bismuth (which acts as a mild antibiotic) as a citrate salt (ranitidine bismuth citrate, Tritec), to treat Helicobacter pylori infections. This combination is usually given with clarithromycin, an antibiotic.. Ranitidine can also be coadministered with NSAIDs to reduce the risk of ulceration. Proton-pump inhibitors (PPIs) are more effective for the prevention of NSAID-induced ulcers.. Ranitidine can be administered preoperatively to reduce the risk of aspiration pneumonia. The drug not ...
ketotifen - meddic
Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three. The mean elimination half life is 12 hours. Besides its anti-histaminic activity, it is also a functional leukotriene antagonist and a phosphodiesterase inhibitor.. The drug may also help relieve the symptoms of irritable bowel syndrome.. ...
ICD-10 Code T47.1X3 - Poisoning by other antacids and anti-gastric-secretion drugs, assault
View the content page [c]
View the content page [c]
Nordoxepin, also known as N-desmethyldoxepin, is the major active metabolite of the tricyclic antidepressant (TCA) doxepin (Sinequan). It has been found to play a significant role in the antidepressant effects of doxepin. Nordoxepin is a mixture of (E) and (Z) stereoisomers. Whereas pharmaceutical doxepin is supplied in an approximate 85:15 ratio mixture of (E)- and (Z)-stereoisomers and plasma concentrations of doxepin remain roughly the same as this ratio with treatment, plasma levels of the (E)- and (Z)-stereoisomers of nordoxepin, due to stereoselective metabolism of doxepin by cytochrome P450 enzymes, are approximately 1:1. Nordoxepin is pharmacologically active similarly to doxepin, but relative to doxepin, is much more potent and selective as a norepinephrine reuptake inhibitor. In general, the demethylated variants of tertiary amine TCAs like doxepin are much more potent inhibitors of norepinephrine reuptake, less potent inhibitors of serotonin reuptake, and less ...
US Patent for Pharmaceutical agents containing carbohydrate moieties and methods of their preparation and use Patent (Patent # ...
组氨酸脱羧酶 - 维基百科，自由的百科
- The discovery of burimamide ultimately led to the development of cimetidine (Tagamet). (wikipedia.org)
- Recent studies have shown that cimetidine, burimamide and improgan (also known as SKF92374, a cimetidine congener lacking H 2 antagonist activity) induce antinociception after intracerebroventricular administration in rodents. (aspetjournals.org)
- H2 mediate gastric acidification and certain smooth muscle functions and are blocked by cimetidine, burimamide, and related compounds. (healthmatics.info)
Potency of burimamide3
- The potency of burimamide was still too low for oral administration. (wikipedia.org)
- Jetter a, kinzig m, rodamer m, tomalik-scharte d, sorgel f, staib ah (1993) inhibitory potency of burimamide is poswltued to be approved or example. (commquest.org)
- Lasker jm, wester mr, aramsombatdee e, raucy jl (1998) characterization of simple modifications on tihydrocodoino h depress cough the analgesic potency of burimamide is poswltued to be sterilised, the time the whole size distribution is uniform. (wisc.edu)
- Burimamide is an antagonist at the H2 and H3 histamine receptors. (wikipedia.org)
- Clonidine -induced biochemical and mechanical effects were blocked by burimamide , an H2-receptor antagonist Propranolol (1 x 10(-6)M), phentolamine (1 x 10(-6)M) or reserpine pretreatment , did not affect the clonidine responses on the perfused guinea pig heart . (bvsalud.org)
- From this lead, the receptor model was further refined, which eventually led to the development of burimamide, a specific competitive antagonist at the H2 receptor. (wikipedia.org)
- Although highly potent H 3 antagonists such as thioperamide lacked antinociceptive activity, homologs of burimamide and thioperamide containing N-aromatic substituents retained H 3 antagonist activity and also showed potent, effective analgesia. (aspetjournals.org)
- Effect of mepyramine, a histamineH1 and burimamide, a histamine H2 receptor antagonist, on ovum implantation in the rat. (lanefertilitymagazine.com)
- The Traeing of thioperamide 1 comes from synthetic efforts that were initiated with the knowledge that some of the known H2 receptor ligands (impromidine 6 (Ki 63 nM) and burimamide 7 (Ki 63 nM)) displayed significant H3 antagonist activity (Figure 2). (dnbforexpriceaction.com)
- In the isolated perfused guinea-pig heart, the increases in isotonic contraction and in cyclic AMP, produced by 2 μg of histamine were significantly and almost completely inhibited in the presence of 2 mg of burimamide, whereas the adrenergic β-receptor blocking drug Kö 592 (50 μg) was ineffective. (springer.com)
- Under the same conditions similar effects of 0.1 μg of isoprenaline, which was equieffective with 2 μg of histamine, were not changed by 2 mg of burimamide, but prevented by 50 μg of Kö 592. (springer.com)
- The close parallelism between changes in contractile amplitude and in cyclic AMP produced by histamine in the absence and in the presence of burimamide is in accordance with the concept that cyclic AMP mediates the mechanical response of the heart to histamide. (springer.com)
- A specific histamine H2-receptor blockator--burimamide--inhibited competitively the binding of labelled histamine by plasma membranes. (termsreign.gq)
- Burimamide is 100 times more potent than Nα-guanylhistamine, proving its efficacy on the H2 receptor. (wikipedia.org)
- Burimamide was also a potent inhibitor of this response but the Schild slope obtained (1.3) was significantly greater than unity. (nih.gov)
- Burimamide was still insufficiently potent for oral administration, and further modification of the structure, based on modifying the pKa of buy xanax long beach the compound, led to the development of metiamide. (consterior.com)
- Esta modificación en la permeabilidad es mediada por la activación del receptor histaminérgico H1, pero es incierta la participación del receptor H2. (bvsalud.org)
- Blockade by burimamide of the effects of clonidine on cardiac contractility phosphorylase activation and cyclic adenosine monophosphate in isolated guinea pig heart. (bvsalud.org)
- 1. Inflammation: Generated by leukocytes at the neuronal of light reflex innervation are relaxed by adr and had a 25% higher incidence of immediate hypersensitivity if h1 blocker burimamide hypersecretory states. (creativecall.org)