Burimamide: An antagonist of histamine that appears to block both H2 and H3 histamine receptors. It has been used in the treatment of ulcers.Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.Isotonic Contraction: Muscle contraction with negligible change in the force of contraction but shortening of the distance between the origin and insertion.Histamine Antagonists: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.Myocardial Contraction: Contractile activity of the MYOCARDIUM.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Muscle Contraction: A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.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.Metiamide: A histamine H2 receptor antagonist that is used as an anti-ulcer agent.Receptors, Histamine: 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.Impromidine: A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.Dimaprit: A histamine H2 receptor agonist that is often used to study the activity of histamine and its receptors.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)Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Thiourea: 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.Methylhistamines: Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.Osmotic Pressure: The pressure required to prevent the passage of solvent through a semipermeable membrane that separates a pure solvent from a solution of the solvent and solute or that separates different concentrations of a solution. It is proportional to the osmolality of the solution.Chemistry, Pharmaceutical: Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.Hydrogel: A network of cross-linked hydrophilic macromolecules used in biomedical applications.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Drug Delivery Systems: Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.Drug Carriers: 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.Technology, Pharmaceutical: 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.Delayed-Action Preparations: Dosage forms of a drug that act over a period of time by controlled-release processes or technology.Capsules: Hard or soft soluble containers used for the oral administration of medicine.Drug Compounding: The preparation, mixing, and assembling of a drug. (From Remington, The Science and Practice of Pharmacy, 19th ed, p1814)Stomach Ulcer: Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).Stomach: An organ of digestion situated in the left upper quadrant of the abdomen between the termination of the ESOPHAGUS and the beginning of the DUODENUM.Duodenal Ulcer: A PEPTIC ULCER located in the DUODENUM.Peptic Ulcer: Ulcer that occurs in the regions of the GASTROINTESTINAL TRACT which come into contact with GASTRIC JUICE containing PEPSIN and GASTRIC ACID. It occurs when there are defects in the MUCOSA barrier. The common forms of peptic ulcers are associated with HELICOBACTER PYLORI and the consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).Leg Ulcer: Ulceration of the skin and underlying structures of the lower extremity. About 90% of the cases are due to venous insufficiency (VARICOSE ULCER), 5% to arterial disease, and the remaining 5% to other causes.Pressure Ulcer: An ulceration caused by prolonged pressure on the SKIN and TISSUES when one stays in one position for a long period of time, such as lying in bed. The bony areas of the body are the most frequently affected sites which become ischemic (ISCHEMIA) under sustained and constant pressure.Skin UlcerSignal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Stomach Neoplasms: Tumors or cancer of the STOMACH.Models, Biological: Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.Peptic Ulcer Hemorrhage: Bleeding from a PEPTIC ULCER that can be located in any segment of the GASTROINTESTINAL TRACT.Peptic Ulcer Perforation: Penetration of a PEPTIC ULCER through the wall of DUODENUM or STOMACH allowing the leakage of luminal contents into the PERITONEAL CAVITY.Helicobacter pylori: A spiral bacterium active as a human gastric pathogen. It is a gram-negative, urease-positive, curved or slightly spiral organism initially isolated in 1982 from patients with lesions of gastritis or peptic ulcers in Western Australia. Helicobacter pylori was originally classified in the genus CAMPYLOBACTER, but RNA sequencing, cellular fatty acid profiles, growth patterns, and other taxonomic characteristics indicate that the micro-organism should be included in the genus HELICOBACTER. It has been officially transferred to Helicobacter gen. nov. (see Int J Syst Bacteriol 1989 Oct;39(4):297-405).Helicobacter Infections: Infections with organisms of the genus HELICOBACTER, particularly, in humans, HELICOBACTER PYLORI. The clinical manifestations are focused in the stomach, usually the gastric mucosa and antrum, and the upper duodenum. This infection plays a major role in the pathogenesis of type B gastritis and peptic ulcer disease.Chagas Disease: Infection with the protozoan parasite TRYPANOSOMA CRUZI, a form of TRYPANOSOMIASIS endemic in Central and South America. It is named after the Brazilian physician Carlos Chagas, who discovered the parasite. Infection by the parasite (positive serologic result only) is distinguished from the clinical manifestations that develop years later, such as destruction of PARASYMPATHETIC GANGLIA; CHAGAS CARDIOMYOPATHY; and dysfunction of the ESOPHAGUS or COLON.Dyspepsia: Impaired digestion, especially after eating.Gastritis: Inflammation of the GASTRIC MUCOSA, a lesion observed in a number of unrelated disorders.Arrhythmias, Cardiac: Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.Defibrillators, Implantable: Implantable devices which continuously monitor the electrical activity of the heart and automatically detect and terminate ventricular tachycardia (TACHYCARDIA, VENTRICULAR) and VENTRICULAR FIBRILLATION. They consist of an impulse generator, batteries, and electrodes.Defibrillators: Cardiac electrical stimulators that apply brief high-voltage electroshocks to the HEART. These stimulators are used to restore normal rhythm and contractile function in hearts of patients who are experiencing VENTRICULAR FIBRILLATION or ventricular tachycardia (TACHYCARDIA, VENTRICULAR) that is not accompanied by a palpable PULSE. Some defibrillators may also be used to correct certain noncritical dysrhythmias (called synchronized defibrillation or CARDIOVERSION), using relatively low-level discharges synchronized to the patient's ECG waveform. (UMDNS, 2003)Fovea Centralis: An area approximately 1.5 millimeters in diameter within the macula lutea where the retina thins out greatly because of the oblique shifting of all layers except the pigment epithelium layer. It includes the sloping walls of the fovea (clivus) and contains a few rods in its periphery. In its center (foveola) are the cones most adapted to yield high visual acuity, each cone being connected to only one ganglion cell. (Cline et al., Dictionary of Visual Science, 4th ed)Correspondence as Topic: Communication between persons or between institutions or organizations by an exchange of letters. Its use in indexing and cataloging will generally figure in historical and biographical material.Death, Sudden, Cardiac: Unexpected rapid natural death due to cardiovascular collapse within one hour of initial symptoms. It is usually caused by the worsening of existing heart diseases. The sudden onset of symptoms, such as CHEST PAIN and CARDIAC ARRHYTHMIAS, particularly VENTRICULAR TACHYCARDIA, can lead to the loss of consciousness and cardiac arrest followed by biological death. (from Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine, 7th ed., 2005)Electric Countershock: An electrical current applied to the HEART to terminate a disturbance of its rhythm, ARRHYTHMIAS, CARDIAC. (Stedman, 25th ed)Medicine, Chinese Traditional: A system of traditional medicine which is based on the beliefs and practices of the Chinese culture.Operator Regions, Genetic: The regulatory elements of an OPERON to which activators or repressors bind thereby effecting the transcription of GENES in the operon.Tachycardia, Ventricular: An abnormally rapid ventricular rhythm usually in excess of 150 beats per minute. It is generated within the ventricle below the BUNDLE OF HIS, either as autonomic impulse formation or reentrant impulse conduction. Depending on the etiology, onset of ventricular tachycardia can be paroxysmal (sudden) or nonparoxysmal, its wide QRS complexes can be uniform or polymorphic, and the ventricular beating may be independent of the atrial beating (AV dissociation).

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)


... 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; ...

*H2 antagonist

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 tolerance ...

*List of MeSH codes (D02)

... burimamide MeSH D02.886.904.282 --- dimaprit MeSH D02.886.904.365 --- guanylthiourea MeSH D02.886.904.390 --- isothiuronium ... burimamide MeSH D02.948.898.282 --- dimaprit MeSH D02.948.898.323 --- ethylenethiourea MeSH D02.948.898.365 --- guanylthiourea ...
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...
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 ...
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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Burimamide - WikipediaBurimamide - 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; ...
more infohttps://en.wikipedia.org/wiki/Burimamide

Specific inhibition by burimamide of histamine effects on myocardial contraction and cyclic AMP | SpringerLinkSpecific 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. ...
more infohttps://link.springer.com/article/10.1007/BF00499184

Category:Thioureas - Wikimedia CommonsCategory:Thioureas - Wikimedia Commons

thiourea (en); tiomocznik (pl) any chemical compound having a general formula RR′NC(=S)NR″R‴ (en); każdy związek chemiczny zawierający ugrupowanie RR′NC(=S)NR″R‴ (pl) thioureas, thiocarbamide, thiocarbamides (en); tiomoczniki, tiokarbamid, tiokarbamidy (pl ...
more infohttps://commons.wikimedia.org/wiki/Category:Thioureas

HRH4 Gene - GeneCards | HRH4 Protein | HRH4 AntibodyHRH4 Gene - GeneCards | HRH4 Protein | HRH4 Antibody

The order of inhibitory activity was imetit , clobenpropit , burimamide , thioperamide. Clobenpropit behaves as a partial ... Shows modest affinity for dimaprit, impromidine, clobenpropit, thioperamide, burimamide clozapine, immepip and imetit. ...
more infohttps://www.genecards.org/cgi-bin/carddisp.pl?id_type=entrezgene&id=59340

STP : main GiPCRsSTP : main GiPCRs

burimamide thioperamide clobenpropit impentamine methylthioperamide N-ethoxycarbonyl-2-ethoxy- 1,2-dihydroquinoline (EEDQ) ...
more infohttp://www.ufrgs.br/imunovet/molecular_immunology/stpgipcrs.html

Volume 55, Issue 4JCI - Volume 55, Issue 4

The estimated dissociation constant (KB) for the burimamide-receptor complex (9 times 10-minus 6 tm) and for the metiamide- ... Both of these histamine activities were reversed by burimamide and metiamide; neither activity was affected by diphenhydramine ...
more infohttps://www.jci.org/55/4

WO1995011894A1 - Histamine h3-receptor antagonists and therapeutic uses thereof 
        - Google PatentsWO1995011894A1 - Histamine h3-receptor antagonists and therapeutic uses thereof - Google Patents

The compounds thioperamide (Arrang et al., Nature 327:117-123 (1987)) and burimamide (Black et al.. Nature 236:385- 390 (1972 ...
more infohttps://patents.google.com/patent/WO1995011894A1/en

US6537525B1 - Medicated chewing-gum 
        - Google PatentsUS6537525B1 - Medicated chewing-gum - Google Patents

Related useful H-2 receptor antagonists include burimamide and metiamide.. Other desirable H-2 receptor antagonists are ...
more infohttps://patents.google.com/patent/US6537525?oq=5920316

H2 antagonist - WikipediaH2 antagonist - Wikipedia

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 ...
more infohttps://en.wikipedia.org/wiki/H2_antagonist

Characterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands.  - PubMed - NCBICharacterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands. - PubMed - NCBI

Burimamide was also a potent inhibitor of this response but the Schild slope obtained (1.3) was significantly greater than ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/1963802?dopt=Abstract

Plus itPlus it

Burimamide, another antagonist that, like thioperamide, contains a thiourea group, likewise discriminated between two classes ...
more infohttp://molpharm.aspetjournals.org/content/38/5/610

oxatomide - meddicoxatomide - meddic

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ranitidine - meddicranitidine - 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.[2]. Ranitidine can be administered preoperatively to reduce the risk of aspiration pneumonia. The drug not ...
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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.[2] The mean elimination half life is 12 hours.[3] 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.[4]. ...
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3H]-thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex.  - PubMed - NCBI3H]-thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex. - PubMed - NCBI

... and burimamide) and biphasic displacement curves were obtained; the Ki values for the high affinity site corresponded well with ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/8864541?dopt=Abstract

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imidazole-type, burimamide, metiamide, cimetidine, oxmetidine, famotidine Serotonin Antagonists piperidine-type, ketanserin, ...
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Patent US4449983 - Simultaneous delivery of two drugs from unit delivery device - Google PatentsPatent US4449983 - Simultaneous delivery of two drugs from unit delivery device - Google Patents

... burimamide and pirenzepine, cimetidine and propantheline, cimetidine and isopropamide, and the like. ...
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McNeill, J. H., and Verma, S. C., 1974, Blockade by burimamide of the effects of histamine and histamine analogues on cardiac ...
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Oromucosal suspensions are dened as a infection leads to burimamide. Also the quantities of synthetic compounds rivaling ...
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... burimamide, cimetidine, ebrotidine, etintidine, famotidine, lafutidine, loxtidine, metiamide, mifentidine, nizatidine, ...
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The first H2 receptor antagonist developed was burimamide, followed by metiamide. With minimal structural alterations, ...
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Peptic Ulcer Disease Treatment and ManagementPeptic Ulcer Disease Treatment and Management

The first H2 receptor antagonist developed was burimamide, followed by metiamide. With minimal structural alterations, ...
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Sir James Black (1972) developedthe first H2 blocker burimamide and confirmedthis classification. This class of drugs was ...
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  • 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)
  • 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)
  • 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)