Animal Communication: Communication between animals involving the giving off by one individual of some chemical or physical signal, that, on being received by another, influences its behavior.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.Administration, Inhalation: The administration of drugs by the respiratory route. It includes insufflation into the respiratory tract.Fenoterol: An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.Bronchodilator Agents: Agents that cause an increase in the expansion of a bronchus or bronchial tubes.Asthma: A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Estrogen Receptor beta: One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.Peak Expiratory Flow Rate: Measurement of the maximum rate of airflow attained during a FORCED VITAL CAPACITY determination. Common abbreviations are PEFR and PFR.Nebulizers and Vaporizers: Devices that cause a liquid or solid to be converted into an aerosol (spray) or a vapor. It is used in drug administration by inhalation, humidification of ambient air, and in certain analytical instruments.Anti-Asthmatic Agents: Drugs that are used to treat asthma.Ethanolamines: AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.Forced Expiratory Volume: Measure of the maximum amount of air that can be expelled in a given number of seconds during a FORCED VITAL CAPACITY determination . It is usually given as FEV followed by a subscript indicating the number of seconds over which the measurement is made, although it is sometimes given as a percentage of forced vital capacity.Adrenal Cortex HormonesIsoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Interleukin-1beta: An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Glucocorticoids: A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Pulmonary Disease, Chronic Obstructive: A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.Drug Therapy, Combination: Therapy with two or more separate preparations given for a combined effect.Estrogen Receptor alpha: One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. Its expression and function differs from, and in some ways opposes, ESTROGEN RECEPTOR BETA.beta 2-Microglobulin: An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Drug Administration Schedule: Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).Integrin beta3: An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.Nicotinic Agonists: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Collagen Type I: The most common form of fibrillar collagen. It is a major constituent of bone (BONE AND BONES) and SKIN and consists of a heterotrimer of two alpha1(I) and one alpha2(I) chains.Serotonin 5-HT1 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.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.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Signal 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.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Integrin alpha5beta1: An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.Integrin beta4: Also known as CD104 antigen, this protein is distinguished from other beta integrins by its relatively long cytoplasmic domain (approximately 1000 amino acids vs. approximately 50). Five alternatively spliced isoforms have been described.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Receptors, Adrenergic, beta-1: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.Integrin alpha6beta4: This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Integrin beta Chains: Integrin beta chains combine with integrin alpha chains to form heterodimeric cell surface receptors. Integrins have traditionally been classified into functional groups based on the identity of one of three beta chains present in the heterodimer. The beta chain is necessary and sufficient for integrin-dependent signaling. Its short cytoplasmic tail contains sequences critical for inside-out signaling.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.beta 2-Glycoprotein I: A 44-kDa highly glycosylated plasma protein that binds phospholipids including CARDIOLIPIN; APOLIPOPROTEIN E RECEPTOR; membrane phospholipids, and other anionic phospholipid-containing moieties. It plays a role in coagulation and apoptotic processes. Formerly known as apolipoprotein H, it is an autoantigen in patients with ANTIPHOSPHOLIPID ANTIBODIES.Integrin alpha4beta1: Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Receptors, Adrenergic, beta-3: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Integrin alpha2beta1: An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.Mice, Inbred C57BLCannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Kinetics: The rate dynamics in chemical or physical systems.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.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.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Receptors, Nicotinic: One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.Integrins: A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Transfection: The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Antigens, CD29: Integrin beta-1 chains which are expressed as heterodimers that are noncovalently associated with specific alpha-chains of the CD49 family (CD49a-f). CD29 is expressed on resting and activated leukocytes and is a marker for all of the very late activation antigens on cells. (from: Barclay et al., The Leukocyte Antigen FactsBook, 1993, p164)Recombinant Proteins: Proteins prepared by recombinant DNA technology.Interleukin-1: A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Integrin alpha6beta1: A cell surface receptor mediating cell adhesion to the EXTRACELLULAR MATRIX and to other cells via binding to LAMININ. It is involved in cell migration, embryonic development, leukocyte activation and tumor cell invasiveness. Integrin alpha6beta1 is the major laminin receptor on PLATELETS; LEUKOCYTES; and many EPITHELIAL CELLS, and ligand binding may activate a number of signal transduction pathways. Alternative splicing of the cytoplasmic domain of the alpha6 subunit (INTEGRIN ALPHA6) results in the formation of A and B isoforms of the heterodimer, which are expressed in a tissue-specific manner.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Gene Expression Regulation: Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Phosphorylation: The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.Glycogen Synthase Kinase 3: A glycogen synthase kinase that was originally described as a key enzyme involved in glycogen metabolism. It regulates a diverse array of functions such as CELL DIVISION, microtubule function and APOPTOSIS.Integrin alpha1beta1: Integrin alpha1beta1 functions as a receptor for LAMININ and COLLAGEN. It is widely expressed during development, but in the adult is the predominant laminin receptor (RECEPTORS, LAMININ) in mature SMOOTH MUSCLE CELLS, where it is important for maintenance of the differentiated phenotype of these cells. Integrin alpha1beta1 is also found in LYMPHOCYTES and microvascular endothelial cells, and may play a role in angiogenesis. In SCHWANN CELLS and neural crest cells, it is involved in cell migration. Integrin alpha1beta1 is also known as VLA-1 and CD49a-CD29.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.B-Cell Activation Factor Receptor: A member of the tumor necrosis factor receptor superfamily that specifically binds B-CELL ACTIVATING FACTOR. It is found on B-LYMPHOCYTES and plays a role in maturation and survival of B-cells. Signaling by the activated receptor occurs through its association with TNF RECEPTOR-ASSOCIATED FACTORS.Oligopeptides: Peptides composed of between two and twelve amino acids.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.Purinergic Agonists: Compounds that bind to and activate PURINERGIC RECEPTORS.Piperidines: A family of hexahydropyridines.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Neurons: The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.Cell Adhesion: Adherence of cells to surfaces or to other cells.Peptide Fragments: Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Adrenergic beta-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Calcium Channel Agonists: Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Gene Expression: The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Tetrahydronaphthalenes: Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Enzyme Activation: Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Blotting, Western: Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.Models, Molecular: Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.PPAR gamma: A nuclear transcription factor. Heterodimerization with RETINOID X RECEPTOR ALPHA is important in regulation of GLUCOSE metabolism and CELL GROWTH PROCESSES. It is a target of THIAZOLIDINEDIONES for control of DIABETES MELLITUS.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Benzazepines: Compounds with BENZENE fused to AZEPINES.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Beta Rhythm: Brain waves with frequency between 15-30 Hz seen on EEG during wakefulness and mental activity.Protein Subunits: Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.Parasympathomimetics: Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.PyrrolidinesReceptors, GABA-A: Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Reverse Transcriptase Polymerase Chain Reaction: A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.Quinpirole: A dopamine D2/D3 receptor agonist.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Protein Conformation: The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.beta Catenin: A multi-functional catenin that participates in CELL ADHESION and nuclear signaling. Beta catenin binds CADHERINS and helps link their cytoplasmic tails to the ACTIN in the CYTOSKELETON via ALPHA CATENIN. It also serves as a transcriptional co-activator and downstream component of WNT PROTEIN-mediated SIGNAL TRANSDUCTION PATHWAYS.Mutation: Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.DNA Polymerase beta: A DNA repair enzyme that catalyzes DNA synthesis during base excision DNA repair. EC 2.7.7.7.Acetylcholine: A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.Cricetulus: A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Receptors, Muscarinic: One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Macromolecular Substances: Compounds and molecular complexes that consist of very large numbers of atoms and are generally over 500 kDa in size. In biological systems macromolecular substances usually can be visualized using ELECTRON MICROSCOPY and are distinguished from ORGANELLES by the lack of a membrane structure.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Muscle, Smooth: Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)Cytokines: Non-antibody proteins secreted by inflammatory leukocytes and some non-leukocytic cells, that act as intercellular mediators. They differ from classical hormones in that they are produced by a number of tissue or cell types rather than by specialized glands. They generally act locally in a paracrine or autocrine rather than endocrine manner.Thiazolidinediones: THIAZOLES with two keto oxygens. Members are insulin-sensitizing agents which overcome INSULIN RESISTANCE by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).Dicamba: A chlorinated organic herbicide.Gonadotropin-Releasing Hormone: A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.Receptors, Transforming Growth Factor beta: Cell-surface proteins that bind transforming growth factor beta and trigger changes influencing the behavior of cells. Two types of transforming growth factor receptors have been recognized. They differ in affinity for different members of the transforming growth factor beta family and in cellular mechanisms of action.Recombinant Fusion Proteins: Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.Receptors, Purinergic P2: A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Immunohistochemistry: Histochemical localization of immunoreactive substances using labeled antibodies as reagents.Cloning, Molecular: The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.Purinergic P2X Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.Serotonin 5-HT3 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.AzocinesMice, Transgenic: Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.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.Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.Dietary Fats: Fats present in food, especially in animal products such as meat, meat products, butter, ghee. They are present in lower amounts in nuts, seeds, and avocados.QuinoxalinesMembrane Potentials: The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).Phospholipase C beta: A phosphoinositide phospholipase C subtype that is primarily regulated by its association with HETEROTRIMERIC G-PROTEINS. It is structurally related to PHOSPHOLIPASE C DELTA with the addition of C-terminal extension of 400 residues.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Cattle: Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.Baclofen: A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.Mutagenesis, Site-Directed: Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.Receptor, Cannabinoid, CB2: A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.Pertussis Toxin: One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.Behavior, Animal: The observable response an animal makes to any situation.Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Nicotinic Antagonists: Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.

Kinetic analysis of drug-receptor interactions of long-acting beta2 sympathomimetics in isolated receptor membranes: evidence against prolonged effects of salmeterol and formoterol on receptor-coupled adenylyl cyclase. (1/3669)

The long-acting beta2 sympathomimetics salmeterol and formoterol have been presumed to exert their prolonged action either by binding to an accessory binding site ("exo-site") near the beta2 adrenoceptor or by their high affinity for beta2 adrenoceptors and correspondingly slow dissociation. Whereas most studies with salmeterol had been done in intact tissues, which have slow diffusion and compartmentation of drugs in lipophilic phases, that restrict drug access to the receptor biophase, we used purified receptor membranes from rat lung and disaggregated calf tracheal myocytes as model systems. Binding experiments were designed to measure the slow dissociation of agonists by means of delayed association of (-)-[125I]iodopindolol. Rat lung membranes were pretreated with high concentrations of agonists (salmeterol, formoterol, isoprenaline) before dissociation was induced by 50-fold dilution. Half-times of association of (-)-[125I]iodopindolol remained unchanged compared with untreated controls, indicating that dissociation of agonists occurred in less than 2 min. Adenylyl cyclase experiments were designed to determine the on and off kinetics of agonists to beta2 adrenoceptors by measuring the rate of receptor-induced cyclic AMP (cAMP) formation. Experiments were performed in tracheal membranes characterized by high Vmax values of cAMP formation. Adenylyl cyclase activation occurred simultaneously with the addition of the agonist, continued linearly with time for 60 min, and ceased immediately after the antagonist was added. Similarly, when receptor membranes were preincubated in a small volume with high salmeterol concentrations, there was a linear increase in cAMP formation, which was immediately interrupted by a 100-fold dilution of the reaction mixture. This militates against the exo-site hypothesis. On the other hand, dissociation by dilution was much less when membranes were preincubated with a large volume of salmeterol at the same concentration, indicating that physicochemical effects, and not exo-site binding, underlie its prolonged mode of action.  (+info)

Mechanisms of prostaglandin E2 release by intact cells expressing cyclooxygenase-2: evidence for a 'two-component' model. (2/3669)

Prostaglandin (PG) release in cells expressing constitutive cyclooxygenase-1 is known to be regulated by liberation of arachidonic acid by phospholipase A2 followed by metabolism by cyclooxygenase. However, the relative contribution of phospholipase A2 to the release of PGs in cells expressing cyclooxygenase-2 is not clear. We addressed this question by using radioimmunoassay to measure PGE2 release by human cells (A549) induced to express cyclooxygenase-2 (measured by Western blot analysis) by interleukin-1beta. Cells were either unstimulated or stimulated with agents known to activate phospholipase A2 (bradykinin, Des-Arg10-kallidin, or the calcium ionophore A23187) or treated with exogenous arachidonic acid. When cells were treated to express cyclooxygenase-2, the levels of PGE2 released over 15 min were undetectable; however, in the same cells stimulated with bradykinin, A23187, or arachidonic acid, large amounts of prostanoid were produced. Using selective inhibitors/antagonists, we found that the effects of bradykinin were mediated by B2 receptor activation and that prostanoid release was due to cyclooxygenase-2, and not cyclooxygenase-1, activity. In addition, we show that the release of PGE2 stimulated by either bradykinin, A23187, or arachidonic acid was inhibited by the phospholipase A2 inhibitor arachidonate trifluoromethyl ketone. Hence, we have demonstrated that PGE2 is released by two components: induction of cyclooxygenase-2 and supply of substrate, probably via activation of phospholipase A2. This is illustrated in A549 cells by a clear synergy between the cytokine interleukin-1beta and the kinin bradykinin.  (+info)

Evidence for beta3-adrenoceptor subtypes in relaxation of the human urinary bladder detrusor: analysis by molecular biological and pharmacological methods. (3/3669)

The purpose of the present study was to confirm the presence of beta3-adrenoceptor subtype in the relaxation of human urinary bladder detrusor tissue by reverse transcription-polymerase chain reaction (PCR); direct sequencing of the PCR product, in situ hybridization; and isometric contraction. Using reverse transcription-PCR, the mRNAs of three receptor subtypes (beta1, beta2, and beta3) were expressed in the human urinary bladder detrusor tissue. Direct sequencing of the PCR product of the above beta3-adrenoceptor revealed no mutation in the amplified regions. In situ hybridization with digoxygenin-labeled oligonucleotide probe revealed the presence of the mRNA of beta3-adrenoceptor subtype in the smooth muscle of the urinary bladder. The relaxant effects of isoproterenol (a nonselective beta-adrenoceptor agonist); ZD7114, BRL37344, and CGP12177A (putative selective beta3-adrenoceptor agonists); and SR59230A (a putative selective beta3-adrenoceptor antagonist) were tested using an isometric contraction technique. Isoproterenol in either the presence or absence of both atenolol (a beta1-adrenoceptor-selective antagonist) and butoxamine (a beta2-adrenoceptor-selective antagonist) revealed a relaxant effect on the carbachol-induced contraction of the human urinary bladder detrusor. Both BRL37344 and CGP12177A also revealed relaxant effects on the human urinary bladder detrusor, but ZD7114 did not elicit any relaxation. These results suggest that beta3-adrenoceptor may have some role in urine storage in the human urinary bladder.  (+info)

Beta2-adrenoceptor polymorphism and bronchoprotective sensitivity with regular short- and long-acting beta2-agonist therapy. (4/3669)

The aim of the present study was to investigate bronchoprotective sensitivity in patients receiving regular treatment with short- and long-acting beta2-agonists and to evaluate any possible association with genetic polymorphism. Thirty-eight patients with stable mild to moderate asthma and receiving inhaled corticosteroids were randomized in a parallel group, double-blind, double-dummy fashion to receive 2 weeks of treatment with either formoterol (12 microg once daily, 6 microg twice daily or 24 microg twice daily) or terbutaline (500 microg four times daily). Bronchoprotection against methacholine challenge (as a provocative dose to produce a 20% fall in forced expiratory volume in 1.0 s: PD20) was measured at baseline (unprotected) after an initial 1 week run-in without beta2-agonist, and at 1 h after the first and last doses of each treatment. The PD20 values were log-transformed and calculated as change from baseline. Percentage desensitization of log PD20 for first- versus last-dose bronchoprotection was calculated and analysed according to effects of treatment and beta2-adrenoceptor polymorphism at codon 16 or 27. The mean degree of desensitization for bronchoprotection was comparable with all four treatments and there were no significant differences in absolute PD20 values after 2 weeks of chronic dosing. The PD20 values were (as microg of methacholine, geometric means+/-S. E.M.): formoterol, 12 microg once daily, 99+/-42 microg; formoterol, 6 microg twice daily, 107+/-44 microg; formoterol, 24 microg twice daily, 108+/-45 microg; terbutaline, 500 microg four times daily, 88+/-37 microg. All patients receiving formoterol, 24 microg twice daily, exhibited a loss of protection greater than 30% which was unrelated to polymorphism at codon 16 or 27. For codon 16, the use of lower doses of formoterol (12 microg once daily or 6 microg twice daily) showed wider variability in the propensity for protection loss in patients who were heterozygous, in contrast to a more uniform protection loss seen with homozygous glycine patients. The amount of protection loss was not significantly related to polymorphism at codon 16 or 27, expressed as values (mean+/-S.E.M.) for percentage desensitization according to each genotype (pooled treatments): Gly-16, 66+/-11%; Het-16, 53+/-8%; Arg-16, 69+/-18%; Glu-27, 68+/-12%; Het-27, 58+/-8%; Gln-27, 52+/-12%. The results of this preliminary study showed that bronchoprotective desensitization occurred readily in response to short- or long-acting beta2-agonist exposure irrespective of beta2-adrenoceptor polymorphism at codon 16 or 27. Further studies with larger patient numbers are required to further evaluate the effects of polymorphisms with lower doses of regular formoterol.  (+info)

The contribution of extraneuronal uptake to the trachea-blood vessel selectivity of beta-adrenoceptor stimulants in vitro in guinea-pigs. (5/3669)

1 The potencies relative to isoprenaline of isoetharine, tertiary butyl noradrenaline, salbutamol, orciprenaline, Me 506, rimiterol, fenoterol, carbuterol and terbutaline on isolated preparations of guinea-pig trachea and blood vessels (perfused hind limb) were determined. All the compounds were selective for trachea and selectivity values, i.e. relative potency on trachea divided by relative potency on hind limb, ranged from 2.3 to 21.4. 2 Responses to isoprenaline (the reference compound), tertiary butyl noradrenaline and isoetharine were potentiated on trachea by 50 muM phenoxybenzamine (PHB) and by other inhibitors of extraneuronal uptake (ENU). Under these conditions the selectivity values of all the compounds was close to unity. 3 Selectivity values were also close to unity if they were calculated from data obtained without ENU inhibition, provided that only those compounds not potentiated by PHB on trachea were used. 4 It is proposed that the trachea-blood vessel selectivity shown by beta-adrenoceptor stimulants can be caused by the influence of ENU upon them, rather than by their ability to distinguish between two beta2-adrenoceptors. 5 The suggestion that differences exist between beta2-adrenoceptors in respiratory and vascular smooth muscle is not supported by the in vitro experiments described.  (+info)

The cat lung strip as an in vitro preparation of peripheral airways: a comparison of beta-adrenoceptor agonists, autacoids and anaphylactic challenge on the lung strip and trachea. (6/3669)

1 A new in vitro preparation, the isolated lung strip of the cat, is described for investigating the direct effect of drugs on the smooth muscle of the peripheral airways of the lung. The preparation comprises a thin strip of lung parenchyma which can be mounted in a conventional organ bath for isometric tension recording. Its pharmacological responses have been characterized and compared with the isolated tracheal preparation of the cat. 2 The lung strip exhibited an intrinsic tone which was relaxed by catecholamines, aminophylline and flufenamate. It was contracted strongly by histamine, prostaglandin F2alpha, acetylcholine, compound 48/80, potassium depolarizing solution and alternating current field stimulation. In contrast, the cat trachea was unresponsive to histamine and prostaglandin F2alpha and did not exhibit an intrinsic tone. 3 (-)-Isoprenaline and (-)-adrenaline were much more potent in relaxing the lung strip than the trachea. The potency order of relaxation responses to isoprenaline, adrenaline and (+/-)-noradrenaline in the lung strip was isoprenaline greater than adrenaline greater than noradrenaline but in the trachea was isoprenaline greater than noradrenaline greater than or equal to adrenaline. 4 beta2-Adrenoceptor selective agonists salbutamol and terbutaline were more potent in the lung strip than the trachea, suggesting beta2-adrenoceptors predominated in the lung strip. Propranolol was equipotent in inhibiting isoprenaline relexations of the lung strip and trachea, whereas practolol was much less effective in inhibiting lung strip than trachea, further supporting a predominance of beta2-adrenoceptors in lung strip and beta1-adrenoceptors in trachea. 5 Strong Schultz-Dale type contractions were elicited in both lung strips and trachea by Ascaris lumbricoides antigen in actively sensitized cats. The initial phase of the contractile response of the lung strip following challenge was shown to be due to histamine release and was absent in the trachea. The delayed phase of the contraction which took several minutes to develop in both the mepyramine-treated lung strip and trachea was not due to prostaglandins E1, F2alpha or bradykinin, the probable mediator being slow reacting substance of anaphylaxis (SRS-A). 6 It is concluded that the isolated lung strip of the cat is useful as an in vitro model for investigating the effect of drugs on the smooth muscle of the peripheral airways of the lungs.  (+info)

Reversal of severe pulmonary hypertension with beta blockade in a patient with end stage left ventricular failure. (7/3669)

A 52 year old man with severe chronic left ventricular failure (New York Heart Association class IV) was considered unsuitable for cardiac transplantation because of high and irreversible pulmonary vascular resistance (PVR). In an attempt to produce symptomatic improvement, metoprolol was cautiously introduced, initially at 6.25 mg twice daily. This was slowly increased to 50 mg twice daily over a two month period and continued thereafter. After four months of treatment the patient's symptoms had improved dramatically. His exercise tolerance had increased and diuretic requirements reduced to frusemide 160 mg/day only. Assessment of right heart pressures was repeated and, other than a drop in resting heart rate, there was little change in his pulmonary artery pressure or PVR. His right heart pressures were reassessed showing a pronounced reduction in pulmonary artery pressure and a significant reduction in PVR, which fell further with inhaled oxygen and sublingual nitrates. He was then accepted onto the active waiting list for cardiac transplantation. A possible mechanism of action was investigated by assessing responses to beta agonists during treatment. Not only was there pronounced improvement in PVR but it was also demonstrated that beta receptor subtype cross-regulation may have contributed to the mechanism of benefit.  (+info)

As-required versus regular nebulized salbutamol for the treatment of acute severe asthma. (8/3669)

Current British guidelines for the administration of beta2-agonists in acute severe asthma recommend regular nebulized therapy in hospitalized patients, followed by as-required (p.r.n.) use via hand-held devices after discharge. Since beta2-agonists do not possess anti-inflammatory activity in vivo, and are thus unlikely to influence the rate of recovery from an asthma exacerbation, it was hypothesized that patients given the short-acting beta2-agonist salbutamol on an as-required basis after admission to hospital would recover as quickly as those on regular treatment, but with potential reductions in the total dose delivered. Forty-six patients with acute severe asthma were randomly assigned to either regular prescriptions of nebulized salbutamol or to usage on a p.r.n. basis, from 24 h after hospital admission. The primary outcome measures were length of hospital stay, time to recovery, and frequency of salbutamol nebulization from 24 h after admission to discharge. Secondary outcome measures were treatment side-effects (tremor, palpitations), and patient satisfaction. Length of hospital stay was reduced in those patients allocated to p.r.n. salbutamol (geometric mean (GM) 3.7 days) versus regular salbutamol (GM 4.7 days). Time taken for peak expiratory flow to reach 75% of recent best was the same in both groups. There was a highly significant reduction in the number of times nebulized therapy was delivered to the p.r.n. group (GM 7.0, range 1-30) compared with the regular treatment group (GM 14.0, range 4-57; p=0.003; 95% confidence interval for ratio of GMs 1.29-3.09). In addition, patients reported less tremor (p=0.062) and fewer palpitations (p=0.049) in the p.r.n. group. Of the patients in the p.r.n. group who had received regular nebulized therapy on previous admissions (n=12), all preferred the p.r.n. regimen. Prescribing beta2-agonists on a p.r.n. basis from 24 h after hospital admission is associated with reduced amount of drug delivered, incidence of side-effects, and possibly length of hospital stay. This has implications for the efficient use of healthcare resources.  (+info)

The researchers did a computer-based search of the medical literature and collected all of the articles that reported on testing the effects of long-acting beta-agonists in asthmatic patients. To be included in this study, the articles had to report that patients were assigned to a group that received a long-acting beta-agonist or to a group that received placebo (an ineffective substance used in place of the active medicine). Assignment to one group or the other had to be done completely by chance. In addition, the study had to have lasted at least 3 months. After retrieving the articles, the researchers judged the quality of each study. They then analyzed the pooled results from all the patients they had been able to gather from all the studies combined and calculated the proportion of patients who had had 1 of the complications listed earlier ...
Although asthma is highly variable in presentation, regular daily treatment is often required. Tolerance to the bronchoprotective effect of both long and short acting β2 agonists has been shown.1. Walters et al examined studies that compared the effects of regular use of inhaled long acting β2 agonists with inhaled short acting β2 agonists. This important clinical question has dimensions of benefits, harms, and costs. The review addressed a clear question, had a comprehensive search strategy, clear inclusion and exclusion criteria, and used the Jadad scale for rating methodological quality. 3 studies involved children ,12 years of age, and data from these studies were combined with studies of adults for the results reported in the tables. The review provides comparisons of some outcomes for children, but each comparison is based on only 1 study, limiting the applicability of the results for children.. Sears reports that the pharmacologically predictable effects of both short and long acting ...
Cathecholamines increase heart rate and contraction force. This effect is mainly mediated by their interaction with the β-adrenergic receptor...
Quick-relief medications relax the muscles around the bronchial tubes so that air can flow freely through them. As noted earlier, these medications are called bronchodilators or beta-agonists because
If you do ok with everyday living and socializing but need the boost to read jornals, write theses or pay bills, arent there some advantages? My Dr acknowledges the reality of tolerance and the desire to use as little drugs as possible as legitimate reasons to go with the IRs…. They are unpredictable…but so is long-acting. A lot of folks like the precision and the feeling that goes on like a light switch when it starts working…whereas the long acting can often leave you feeling like you have taken nothing…. ...
Overuse of inhaled bronchodilator beta agonist medication results in a loss of effectiveness (i.e. tolerance). This has been shown for the short acting beta agonist salbutamol and the long acting beta agonist salmeterol. Tolerance to salmeterol is present within 24 hours. The onset of tolerance to salbutamol is not known ...
165 trials were reviewed and eight were included; a total of 461 patients have been studied (229 with CBA; 232 with intermittent beta-agonists). Overall, admission to hospital was reduced with CBA compared to intermittent beta-agonists (RR: 0.68; 95% CI: 0.5 to 0.9); patients with severe airway obstruction at presentation appeared to benefit most from this intervention (RR: 0.64; 95% CI: 0.5 to 0.9). Patients receiving CBA demonstrated small but statistically significant improvements in pulmonary function tests when all studies were pooled. Patients receiving CBA had greater improvements in % predicted FEV-1 (SMD: 0.3; 95% CI: 0.03 to 0.5) and PEFR (SMD: 0.33; 95% CI: 0.1 to 0.5); this effect was observed by 2-3 hours. Continuous treatment was generally well tolerated, with no clinically important differences observed in pulse rate (WMD: -2.87; 95% CI: -6.0 to 0.3) or blood pressure (WMD: -1.75; 95% CI: -5.6 to 2.1) between the treatment groups. Tremor was equally common in both groups (OR: ...
A major new study shows that, contrary to previously published reports, regular daily use of so-called beta-agonists such as albuterol for mild asthma does no harm to patients. The study, reported
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The species, which eluted at 6.75 min and produced a molecular ion of m/z 255.13 (Fig. 4E), was assigned to a mono-nitrated salbutamol derivative 3 (Fig. 1). This assignment is consistent with elemental analysis (C12H19N2O4+, exact mass 255.13397) and further supported by MS/MS spectrum obtained from this molecular ion (Fig. 4G). Formation of this nitrophenol was unexpected as it required the side chain at C3 of the aromatic ring, -CH2OH, to be eliminated. We verified that the putative phenolic precursor of 3, a salbutamol analog, in which the -CH2OH moiety was replaced with -H, (m/z 210), was not present as an impurity in salbutamol samples. This indicates that the corresponding radical (1d in Fig. 11) had to be produced in situ, during enzymatic oxidation of salbutamol itself. In the proposed mechanism (Fig. 11), the initially generated phenoxyl radical, 1a, undergoes intramolecular hydrogen atom transfer from the adjacent -CH2OH moiety to generate the aryl-methoxyl-type radical 1c. After ...
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Amibegron, a highly selective β3-adrenoceptor agonist originated by Sanofi (now sanofi-aventis), stimulates neuronal activity in a specific area of the
TY - JOUR. T1 - Impaired beta-adrenergic receptor activation of adenylyl cyclase in airway smooth muscle in the basenji-greyhound dog model of airway hyperresponsiveness.. AU - Emala, C.. AU - Black, C.. AU - Curry, C.. AU - Levine, M. A.. AU - Hirshman, C. A.. PY - 1993/6. Y1 - 1993/6. N2 - Previous studies in human asthmatics have suggested a defect in the beta-adrenergic pathway leading to cyclic adenosine monophosphate (cAMP) generation. Although these studies have suggested normal or increased numbers of beta-adrenergic receptors, limitations in the quantity of tissue available have not allowed further delineation of the biochemical or molecular mechanisms of human asthma. The basenji-greyhound (BG) dog model of nonspecific airway hyperreactivity displays similarities to human asthma, and altered functional response to beta-adrenergic agonists has been previously shown in airway tissue from this model. We have now correlated this functional impairment in beta-adrenergic response with a ...
Repeated administration of the centrally acting beta adrenoceptor agonist, clenbuterol, to rats reduced the ability of isoproterenol to increase the concentration of cyclic AMP (cAMP) in slices of cerebellum. This reduced responsiveness to isoproterenol was accompanied by a marked reduction in the density of beta adrenoceptors as measured by the binding of the beta adrenoceptor antagonist [125I]iodopindolol. In addition, the agonist-binding properties of remaining cerebellar beta adrenoceptors were altered after clenbuterol treatment. The clenbuterol-induced reduction in the density of beta adrenoceptors in the cerebellum is in marked contrast to its inability to do this in cerebral cortex. Comparison of the ability of clenbuterol to that of isoproterenol to increase levels of cAMP in slices of cerebral cortex or cerebellum showed that clenbuterol is a weakly potent agonist in both brain regions. The increase in cAMP induced by isoproterenol in the cortex was significantly reduced in the ...
INTRODUCTION: Clenbuterol has been used to alleviate chronic obstructive pulmonary disease and elicit an anabolic response in muscles. The aim of this study was to determine the influence of muscle mass variation on physical capacities in rats.. METHODS: The left hindlimbs of Wistar rats were immobilized for 20 days in plantarflexion with a splint and then remobilized for 16 days. The effect of a non-myotoxic dose of clenbuterol during the immobilization period was evaluated. Physical capacities were coordination, free locomotion, grip strength, and bilateral deficit.. RESULTS: Immobilization induced a loss of muscle mass, coordination, and strength without any effect on free locomotion. The positive anabolic effect of clenbuterol did not prevent a loss of physical capacities resulting from immobilization.. CONCLUSIONS: Muscle mass correlated strongly with coordination and isometric strength in untreated rats. Anabolic effect, fiber phenotype modification, and perturbation in neuromuscular ...
Pirbuterol is a beta-2 adrenergic bronchodilator. In vitro studies and in vivo pharmacologic studies have demonstrated that pirbuterol has a preferential effect on beta-2 Adrenergic receptors compared with isoproterenol. While it is recognized that beta-2 adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta-2 receptors in the human heart, existing in a concentration between 10-50%. The precise function of these receptors has not been established. The pharmacologic effects of beta adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (AlP) to cyclic-3† ,5†-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells,
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Background. Sex differences in LV mechanics exist at rest and during acute physiological stress. Differences in cardiac autonomic and adrenergic control may contribute to sex differences in LV mechanics and LV hemodynamics. Accordingly, this study aimed to investigate sex differences in LV mechanics with altered adrenergic stimulation achieved through post handgrip exercise ischemia (PEI) and ß1-adrenergic receptor (AR) blockade. Methods and Results. 20 males (23±5 yr) and 20 females (22±3 yr) were specifically matched for LV length (males: 8.5±0.5 cm, females: 8.2±0.6 cm, p=0.163), and 2-dimensional speckle-tracking echocardiography was used to assess LV structure and function at baseline, during PEI and following administration of 5mg bisoprolol (ß1-AR antagonist). During PEI, LV end-diastolic volume and stroke volume were increased in both groups (p,0.001), as was end-systolic wall stress (p,0.001). LV twist and apical rotation werent altered from baseline or different between the ...
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The Boxed Warning, the most prominent warning, about asthma-related death has been removed from these drug labels Read More.... In 2011, the FDA required that drug companies that market long-acting beta agonists (LABAs) in combination with inhaled corticosteroids (ICS) conduct trials to evaluate the safety of these agents. After review of four large studies, the FDA has determined that treating asthma with ICS/LABA does not result in significantly more serious asthma-related side effects than treatment with ICS alone. Four trials also assessed efficacy of the ICS/LABA products, and demonstrated that the ICS/LABA combination reduced asthma exacerbations compared to ICS alone. Using LABAs alone without an ICS for asthma is linked with an increased risk of asthma-related death and this Boxed Warning will remain on single ingredient LABA medicine. Labels on combo inhalers such as Advair, Breo Ellipta, Dulera, AirDuo, and Symbicort will be updated.. ...
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... is a beta-2 adrenergic agonist with some similarities to ephedrine, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug. Clenbuterol causes an increase in aerobic capacity, central nervous system stimulation, and an increase in blood pressure and oxygen transportation. Clenbuterol increases the rate at which fat and protein are metabolized, simultaneously slowing the bodys BMR. Clenbuterol is commonly used for smooth muscle relaxant properties.
... is a beta-2 adrenergic agonist with some similarities to ephedrine, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug. Clenbuterol causes an increase in aerobic capacity, central nervous system stimulation, and an increase in blood pressure and oxygen transportation. Clenbuterol increases the rate at which fat and protein are metabolized, simultaneously slowing the bodys BMR. Clenbuterol is commonly used for smooth muscle relaxant properties.
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Background. Persistent asthma is characterized by airway remodeling. Whereas we have previously shown that neither β(2)-agonists nor corticosteroids inhibit extracellular matrix (ECM) protein release from airway smooth muscle (ASM) cells, the effect
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It is now well established that any given ligand for a G-protein-couple receptor (GPCR) does not simply possess a single defined efficacy. Rather, a ligand possesses multiple efficacies, depending on the specific down-stream signal transduction pathway analyzed. This diversity may be based on ligand-specific GPCR conformations and is often referred to as "functional selectivity." It has been known for a century that stereoisomers of catecholamines differ in their potency and, in some systems, also in their efficacy. However, the molecular basis for efficacy differences of GPCR ligand stereoisomers has remained poorly defined. In an elegant study published in this issue of Molecular Pharmacology, Woo et al. (p. 158) show that stereoisomers of the β2-adrenoceptor selective agonist fenoterol differentially activates Gs- and Gi-proteins in native rat cardiomyocytes. This study is so important because it is the first report to show that even the subtle structural differences within a ligand ...
The beta-2 agonist Clenbuterol is used for treating asthma, since it is a bronchodilator, in many countries. However, it is more commonly used to burn fat
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Clen, short for Clenbuterol, is a widespread terminology that is used to refer to a well-known bronchodilator, Clenbuterol Hydrochloride. Clen - which is also coined as Ventipulmin, Spiropent, and Dilaterol in the market - is typically used by people who have chronic asthma or other breathing disorders as a decongestant. Aside from its common use,…
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Terbutaline works by relaxing the muscles surrounding the airways so that air can pass through more easily to help relieve symptoms of asthma or COPD.
I have Earlier stated that your body will adapt to clenbuterol dosing, thus necessitating an increase of dosage in the course of the cycle to run it most properly. The mostly used way of clenbuterol dosing is that of 2 months on and 2 months off with a steady, incremental dosing plan. Using this process necessitates the Original dosing start very low, usually forty mcg for men and 20 mcg for Women of all ages, and will raise quickly promptly, generally every single 2 days, and may reach max consumption once the Preliminary two months of dosing. ...
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The principal mechanism by which bronchodilator β-adrenoceptor agonists act is to relax airways smooth muscle although they may also be anti-inflammatory. However, the extent of anti-inflammatory activity and the cell types affected by these agonists are uncertain. The purpose of this study was to evaluate whether β-adrenoceptor agonists prevent pro-inflammatory cytokine generation from activated human lung macrophages. Macrophages were isolated and purified from human lung. The cells were pre-treated with both short-acting (isoprenaline, salbutamol, terbutaline) and long-acting (formoterol, salmeterol, indacaterol) β-agonists before activation with lipopolysaccharide (LPS) to induce cytokine (TNFα, IL-6, IL-8 and IL-10) generation. The experiments showed that short-acting β-agonists were poor inhibitors of cytokine generation. Of the long-acting β-agonists studied, formoterol was also a weak inhibitor of cytokine generation whereas only indacaterol and salmeterol showed moderate ...
Chronic beta1-adrenergic stimulation leads to progressive heart failure. In mice overexpressing human beta1-adrenergic receptor (b1-OE), increased cytosolic Ca load in cardiomyocytes at early age is pivotal for the development of heart failure. The mechanisms leading to impaired intracellular Ca handling are unclear. We examined spatially resolved Ca release (1 Hz stim, Fluo4-AM), L-type Ca current (ICa), Na-Ca-exchanger (NCX) expression and function, cytosolic [Na] (SBFI) and T-tubule structures (Di8-ANEPPS) in cardiomyocytes from young (8-16 wks) b1-OE mice and wildtype (WT) littermates. Systolic [Ca] amplitude was unchanged, whereas time to peak [Ca] (140±5 vs. 127±3 ms) and [Ca] decay (time constant, 223±16 vs. 182±9 ms) were significantly prolonged in TG vs. WT (n=29 and 43 cells, resp.). SR Ca content was increased (114±14 vs. 64±15 μmol/L, n=14 and 16,resp.). Diastolic Ca leak from the SR, quantified as tetracaine (1 μmol/L)-sensitive change in diastolic [Ca] (14.4±6.0 vs. 22.1 ...
FDA-approved beta-agonists in cattle feed are widely used to help feedlot cattle efficiently produce more lean muscle, but one beta-agonist, Zilmax, was voluntarily suspended by its manufacturer due to animal welfare concerns. K-State researchers are looking into how heat stress and other environmental factors might play a role in this issue and affect cattle mobility and feed intake.
Ractopamine is sold under three brand names, all made by the same company: Paylean, Optaflexx and Tomax. Paylean is fed to pigs for the last 28 days of their lives, Optaflexx to cattle for the last 28 to 42 days of their lives, and Tomax to turkeys for the last 7 to 14 days of their lives. According to manufacturer Elanco Animal Health (a division of Eli Lilly), fully 45 percent of U.S. pigs and 30 percent of non-grass-fed cattle receive some form of ractopamine.. The drug works by increasing the bodys synthesis of protein - thereby causing animals to bulk up and yield more meat. Ractopamine is in the family of drugs known as beta-agonists, which contains many asthma drugs. Bottemiller writes, that its use in livestock agriculture produces up to 10 percent more meat, raising profits $2 per head. Though the drug has not been considered for human use, it is administered up until slaughter, and minute traces have been found in meat.. Ractopamine is so dangerous to human health that the FDArequires ...
When treating patients, the best treatment strategy is prevention. Patients should be instructed to be aware of what situations prompt an attack, such as exposure to allergens, respiratory infections, and cold weather, and should be encouraged to avoid these situations. Beyond this, if a patient has asthma attacks that are severe, unpredictable, or occur more than twice a week, then the recommendation is for treatment with a long-term control medication. These preventive medications are taken daily to achieve and maintain control of asthma symptoms. A common and effective medication type for controlling asthma is inhaled corticosteroids. These anti-inflammatory medications can improve asthma control and normalize lung function. Other medications typically used for long-term control of asthma are long-acting beta-agonists (LABAs), cromolyn, theophylline, leukotriene modifiers, and immunomodulators. Quick-relief medications include short-acting beta-agonists (SABAs), which relax airway muscles to ...
Objective and Design: To investigate the effects of β2- adrenoceptor (β2-AR) stimulation on endotoxin-induced liver damage and systemic cytokine levels in rats. Subjects: Standard male Wistar rats. Treatment: A disease-model of lipolysaccharide (LPS)-induced acute systemic inflammation was used. The β2-selective AR agonist clenbuterol was administered before, during, and after LPS-challenge to investigate its effects on the acute inflammatory response and associated liver-failure. Methods: The following parameters have been measured in plasma: TNFα, IL-1β, IL-6, IL-10, AST, ALT, and Bilirubin. Liver histological examination was performed to look for changes in tissue morphology. Results: Administration of clenbuterol (p.o.) one hour before, or intravenous at the same time as LPS-challenge resulted in a marked reduction of plasma levels of TNFα, IL-1β, and IL-6. A change both in plasma-level and in time-concentration profile of the anti-inflammatory cytokine IL-10 was found. Clenbuterol ...
Postprandial release of peptide YY (PYY) and glucagon-like peptide-1 (GLP-1) from L cells results from both nutrient transit in the ileal lumen and neural drive of endocrine cells. The adrenosympathetic system and its effectors have been shown to induce secretion of L cells in vivo or in vitro. Because these transmitters act through three receptors, beta, alpha1, alpha2, coupled to different intracellular pathways, we evaluated the responses of L cells to specific agonists, using the model of isolated vascularly perfused rat ileum. General stimulation of adrenergic receptors with epinephrine (10(-7) M) induced significant GLP-1 and PYY secretions (94+/-38 and 257+/-59 fmol/8 min respectively) which were abolished upon propranolol (10(-7) M) pretreatment and strongly decreased upon infusion with 10(-8) M prazosin. Blockade of alpha2-receptors with idazoxan (10(-8) M) did not alter epinephrine-induced peptide secretion. The beta-adrenergic agonist isoproterenol (10(-6) M) infused for 30 min ...
This network meta-analysis compares four different classes of long-acting inhalers for people with COPD who need more than short-acting bronchodilators. Quality of life and lung function were improved most on combination inhalers (LABA and ICS) and least on ICS alone at 6 and at 12 months. Overall L …
This trial will investigate the effectiveness and cost effectiveness of beclometasone, versus inhaled corticosteroids and long-acting beta agonist (fixed or
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The active substance of the drug with a name close to it clenbuterol hydrochloride is initially a drug. Its drugs in medicine are actively used in the treatment of bronchial asthma and related diseases (safely and practically without adjustment of doses are prescribed to patients of different sex and age).. What effect does Clenbuterol (packing 100 tablets) have on the athlete? The drug acts as a selective b2-adrenostimulator (excites β2-adrenoreceptors). After application (orally) under its influence, lipolysis increases and the best use of fats as an energy source is observed. It is also known that clenbuterol can enhance the release of norepinephrine and epinephrine, which are actually strong natural fat burners (stimulate weight loss).. Important detail:. Clenbuterol (40mg / tab, 100tab) from the Balkans, like analogues from other producers, helps to increase the level of metabolism to 20-30% of the original. At a parallel reception with ketotifenum the effect only amplifies (about ...
Ractopamine ELISA [R-RT3451] - Ractopamine is a phenethanolamine belonging to a class of drugs known as β-Adrenergic agonists (beta agonists) and has been found to increase muscle growth and decrease fat deposition. Due to the nature of this group of compounds, they have a history of being used illegally, particularly by livestock producers. Improper
Ractopamine ELISA [R-RT3451] - Ractopamine is a phenethanolamine belonging to a class of drugs known as β-Adrenergic agonists (beta agonists) and has been found to increase muscle growth and decrease fat deposition. Due to the nature of this group of compounds, they have a history of being used illegally, particularly by livestock producers. Improper
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This drug combines two primary active ingredients: salmeterol and fluticasone. Salmeterol is a member of the drug family known as long-acting, beta-adrenergic bronchodilators (also called beta-agonists). It is inhaled by mouth, into the lungs, to treat asthma and prevent bronchospasm. Salmeterol is also used to...
Dupilumab, an injectable monoclonal antibody that inhibits signaling by interleukin-4 and interleukin-13, reduced asthma exacerbations by almost 90% while also improving asthma symptoms in a randomized trial. Participants had moderate-to-severe asthma that had previously been uncontrolled despite use of inhaled corticosteroids with long-acting beta-agonists. Twenty five million people in the U.S. - 8% of the population [… read more]. ...
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Clenbuterol Hydrochloride is a sympathomimetic that works around the sympathomimetic central nerovosu system. There are several pain in the body some sort of sympathomimetic can certainly act on. Regarding Clenbuterol, the particular beta-2 beneficiario is the specialized niche and actions. Clen, because its typically known, definitely stimulates the beta-2 radio. Through this sort of stimulation, this actively dos airway interferences and provides superior breathing for people who need it. This same stimulation can also be used to enhance the particular metabolic rate of the individual. Clenbuterol does not make an effort to burn fat simply by attacking excess fat cells, but instead stimulates the metabolism by simply increasing typically the bodys temp. This takes place due to the beta-2 stimulation stimulating the mitochondria of the cellular material to produce and release a lot more heat. Therefore, this gets hotter14957 the bodys temperature (slightly), enhances the metabolism and ...
Side effects of Clenbuterol Cycles:. Since usage of Clenbuterol comes with lot of side effects, it has been banned for human use in USA. But the side effects will depend on the dosage and how it is been used. One good thing about Clen is side effects will disappear once the dosage has been stopped.. One thing that user should keep in mind is that user must be very careful when Clenbuterol is used with other adrenoreceptor antagonists. This is because there is chance that side effects may cumulative. Some of the common side effects are insomnia, nervousness, anxiety, muscle cramps, high blood pressure, increased appetite, nausea, excessive sweating. When Clen is used for long term, user may experience side effects like cardiac hypertrophy.. This is the reason use of Clen must be avoided if the person is suffering from hypertension or any other cardiac issues. If the user is already taking some supplements which is similar to this, then he must avoid taking Clen.. ...
Data Synthesis:. Pooled results of 22 trials showed that regular β2-agonist use, compared with placebo, did not change the mean FEV1 after treatment or the net FEV1 treatment effect but substantially reduced the following: the peak FEV1 response to subsequent β2-agonist administration (change, −17.8% [95% CI, −27.2% to −8.5%]); the FEV1 dose response to subsequent β2-agonists (−34.8% [CI, −45.7% to −24%]); the PC20 to combined bronchoconstrictive stimuli (−26% [CI, −37% to −11%]); and leukocyte β2-receptor density (−18.3% [CI, −31.6% to −5.1%]), binding affinity (−23.1% [CI, −39.4% to −6.8%]), and in vitro response to isoproterenol (−32.7% [CI, −56.5% to −9.0%]). ...
Quick-relief or rescue medications are used to quickly relax and open the airways and relieve symptoms during an asthma flare-up, or are taken before exercising if prescribed. These include: short-acting beta-agonists . These inhaled bronchodilator
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What Else Do I Need to Know?. Before you look for Clenbuterol for sale and especially before you take it… you really must start out slow when you begin taking this workout aid. That cannot be stressed enough. You should start out at 20/mcg per day, never going over 200/mcg per day. The most common dose for men is 60-100 mcg per day. In women, the dose is normally 10-40 mcg per day.. Some people prefer to buy Clen with the plan to take it for 2 weeks on and 2 weeks off. There is no real scientific reasoning behind that but if rumors are true, some builders feel there is a benefit to this method. With that said, studies do show that after a 6 week period, fat free mass increased by 5% in some groups. This suggests that the best of your results will come after you have been on this drug for 2 weeks and longer.. Around the third week of Clenbuterol use, you will need to begin taken some form of anti-histamine to continue to see results. This is because deregulation begins to occur in the Central ...
When you feel symptoms on asthma after exercising or doing sports, this can be an indication that you have EIA. The best way to treat this is pre-treatment. Even before you start a physical activity, you should take medication so the narrowing of airway can be blocked. You may opt for short-acting inhaled beta-agonists or rescue drugs which can be effectively used to prevent symptoms. Eighty percent of asthma patients have eliminated their symptoms on EIA ...
Clenbuterol - Stimulator (3 2 -adrenoceptor and has a bronchodilator effect sekretoliticheskoe turn r.. 2 -adrenergic receptors stimulates adenylate
Asthma deaths are the highest they have been for a decade, statistics show. Data from The Office for National Statistics (ONS) reveals fatalities from the common lung condition have risen by more than a third over the past 10 years.
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Albuterol is one of the popular bronchodilators available in the market which has been designed to initiate increase the air flow to the lungs by relaxing the airway muscles.
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... is a beta-adrenergic agonist.[1] Its structure is based on soterenol (antiarrhythmic) and phentermine. ...
Combination with beta-adrenergic agonists increases the dilating effect on the bronchi. ...
In October 2006, ractopamine was banned in Taiwan along with other beta-adrenergic agonists.[6] In August 2007, the Department ...
... is a beta-adrenergic agonist. "Synthesis of 6,7-dihydrox-1,2,3,4-tetrahydroisoquinoline derivatives". Tetrahedron. ...
"Assessment of compliance in children using inhaled beta adrenergic agonists". Ann Allergy. 62 (5): 406-9. PMID 2566291. Herpes ...
... is a partial beta-adrenergic agonist. Effects of the novel beta-adrenergic partial agonist alifedrine on cardiac ...
... is a beta-adrenergic agonist. Dichloroisoprenaline Byrem TM, Beermann DH, Robinson TF (April 1998). "The beta-agonist cimaterol ...
... where it serves as a full agonist at mouse (not necessarily human) TAAR1. It is also an agonist at beta-adrenergic receptors. A ... Taiwan banned ractopamine along with other beta-adrenergic agonists in October 2006, but in 2012, its legislature passed ... Pharmacologically, it is a TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors. It is the ... "Beta-agonists hog the limelight". The Star. November 5, 2006. Retrieved January 25, 2012. "Vet Dept seals 10 pig farms". The ...
"Beta-3 Adrenergic Agonist, BRL-26830A, and Alpha/Beta Blocker, Arotinolol, Markedly Increase Regional Blood Flow in the Brown ... "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol. 79 (7): 585- ... Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts ... "β-adrenergic blocking, antiarrhythmic compound S-596". It is used in the treatment of high blood pressure and essential tremor ...
Beta2-adrenergic agonists act on beta-2 receptors to drive potassium into the cells. Therefore, beta blockers can raise ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propanolol and labetalol. Beta-1 ... adrenaline and noradrenaline have a protective effect on the cardiac electrophysiology because they bind to beta 2 adrenergic ... Examples of medications that can cause hyperkalemia include ACE inhibitors, angiotensin receptor blockers, beta blockers, and ...
doi:10.1016/S0378-5173(02)00541-0. Koike, K; Takayanagi, I (October 1986). "A beta-adrenergic partial agonist (befunolol) ... Takayanagi, I; Koike, K (January 1985). "A beta-adrenoceptor blocking agent, befunolol as a partial agonist in isolated organs ... It also acts as a β adrenoreceptor partial agonist. Befunolol was introduced in Japan in 1983 by Kakenyaku Kako Co. under the ... Befunolol (INN) is a beta blocker with intrinsic sympathomimetic activity used in the management of open-angle glaucoma. ...
Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... Khan ZP, Ferguson CN, Jones RM (1999). „alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role". ... Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ...
... has modest beta-adrenergic agonist activity and is therefore used with caution in angina pectoris. Pindolol is a non- ... selective beta blocker or β-adrenergic receptor antagonist with partial agonist activity and also possesses intrinsic ... Hoffmann C, Leitz MR, Oberdorf-Maass S, Lohse MJ, Klotz KN (2004). "Comparative pharmacology of human beta-adrenergic receptor ... "Blood pressure lowering efficacy of partial agonist beta blocker monotherapy for primary hypertension". Cochrane Database Syst ...
Beta2-adrenergic agonist acts on beta-2 receptor to drive potassium into the cells. Therefore, beta blockers can cause the rise ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propanolol and labetalol. Beta-1 ... adrenaline and noradrenaline have a protective effect on the cardiac electrophysiology because they bind to beta 2 adrenergic ... in potassium levels due to blockage of beta-2 receptors. However, the rise potassium levels is not marked unless there are ...
Shimizu, W; Antzelevitch, C (2015-09-28). "Differential effects of beta-adrenergic agonists and antagonists in LQT1, LQT2 and ...
"Interaction between the antidepressant-like behavioral effects of beta adrenergic agonists and the cyclic AMP PDE inhibitor ... "Effects of serotonin and serotonergic agonists and antagonists on the production of tumor necrosis factor α and interleukin-6 ...
... is a beta-adrenergic agonist which has effects on the function of trachea and heart muscles. During a study of acute ... In animal models, higenamine has been demonstrated to be a β2 adrenoreceptor agonist. Adrenergic receptors, or adrenoceptors, ... Along with many other β2 agonists, higenamine is prohibited by World Anti-Doping Agency for use in sports. In 2016, French ... In particular, higenamine, via a beta-adrenoceptor mechanism, induced relaxation in rat corpus cavernosum, leading to improved ...
Verhoeckx KC, Doornbos RP, Witkamp RF, van der Greef J, Rodenburg RJ (January 2006). "Beta-adrenergic receptor agonists induce ... Zilpaterol (zilpaterol hydrochloride; codenamed RU 42173) is a β2 adrenergic agonist. Under its trade name, Zilmax, it is used ... A. Plascencia; N. Torrentera & R.A. Zinn (1999). "Influence of the β-Agonist, Zilpaterol, on Growth Performance and Carcass ...
Thyroid hormones increase the contractility but suppres the effects of beta-adrenergic agonist by decreasing phospholamban ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
... s must not be used in the treatment of selective alpha-adrenergic agonist overdose. The blockade of only beta ... beta-blockers, β-blockers, beta-adrenergic blocking agents, beta antagonists, beta-adrenergic antagonists, beta-adrenoreceptor ... Beta-Adrenoceptor Antagonists (Beta-Blockers); "CV Pharmacology , Beta-Adrenoceptor Antagonists (Beta-Blockers)". Archived from ... Beta blockers, due to their antagonism at beta-1 adrenergic receptors, inhibit both the synthesis of new melatonin and its ...
The three types of prescription bronchodilating drugs are β2("beta two")-adrenergic agonists (short- and long-acting), ... Some short-acting β-agonists, such as salbutamol, are specific to the lungs; they are called β2-adrenergic agonists and can ... Because it has no effect on asthma symptoms when used alone, it is most often paired with a short-acting β2-adrenergic agonist ... have bronchodilating effects and were used often for asthma due to the lack of effective β2-adrenergic agonists for use as ...
Propranolol - Sympatholytic, beta blocker. Clonidine - Sympatholytic, α2-adrenergic receptor agonist. Guanfacine - ... α2-adrenergic receptor agonist. Prazosin - Sympatholytic, alpha blocker. In the National Comorbidity Survey (2005), 58 percent ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone. Serotonin-norepinephrine reuptake inhibitors (SNRIs), ...
... a selective alpha-2 adrenergic receptor agonist, and timolol, a non-selective beta-adrenergic receptor inhibitor. Elevated IOP ... It is a combination of brimonidine (an α2 adrenergic agonist) and timolol (a β adrenergic blocker), in concentrations of 0.2% ...
Inhalation of an agonist for the beta-2 adrenergic receptor, such as Salbutamol, Albuterol (US), is the most common treatment ... However, with regular beta-2 agonist use, asthmatic Arg-16 individuals experience a significant decline in bronchodilator ... It has been proposed that the tachyphylactic effect of regular exposure to exogenous beta-2 agonists is more apparent in Arg-16 ... July 2000). "The effect of polymorphisms of the beta(2)-adrenergic receptor on the response to regular use of albuterol in ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... Khan ZP, Ferguson CN, Jones RM (1999). "alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role". ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ...
SEARCH RESULTS for: Adrenergic beta-Agonists [Drug Class] (655 results) * Share : JavaScript needed for Sharing tools. Bookmark ...
These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?) and What is the role of beta-adrenergic ... Mirabegron (Myrbetriq), a beta-3 adrenergic receptor agonist, causes relaxation of the detrusor miuscle and increases bladder ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?. Updated: Sep 23, 2019 ...
Alpha/Beta Adrenergic Agonists. Class Summary. These agents augment coronary and cerebral blood flow during the low-flow states ... Its beta-agonist effects include bronchodilatation, chronotropic cardiac activity, and positive inotropic effects. ... It has alpha-agonist effects that include increased peripheral vascular resistance, reversed peripheral vasodilatation, ... Phi Beta Kappa. Disclosure: Nothing to disclose. ...
Beta-adrenergic agonists, or β-agonists, are non-hormonal growth promotants that help animals put on muscle instead of fat. ... "Beta-agonists: What are they and should I be concerned?". Retrieved 9 January 2017. "Beta agonists in cattle debate beefs up". ... "Temple Grandin Explains Animal Welfare Problems With Beta-Agonists". Retrieved 9 January 2017. "Use of Beta-Agonists in Cattle ... But problems may exist with all β-agonists supplementation, and not just for animals. The family of β-agonists includes β1-, β2 ...
In general, pure beta-adrenergic agonists have the opposite function of beta blockers. Beta adrenoreceptor agonist ligands ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, which widen the airways and result ... "WHAT ARE BETA-AGONISTS?". Thoracic.org. American Thoracic Society. Retrieved 17 October 2014. Adrenergic beta-Agonists at the ... Most agonists of the beta receptors are selective for one or more beta-adrenoreceptors. For example, patients with low heart ...
... www.mayoclinic.org/drugs-supplements/beta-2-adrenergic-agonist-oral-route-injection-route/side-effects/DRG-20069364 ... Adrenergic bronchodilators are medicines that stimulate the nerves in many parts of the body, causing different effects. ... All of the other adrenergic bronchodilators are available only with your doctors prescription. ...
Although not all of the side effects listed above have been reported for each of these medicines, they have been reported for at least one of them. All of these medicines are similar, so many of the above side effects may occur with any of the medicines.. Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.. ...
Alpha/Beta Adrenergic Agonists. Class Summary. Before or simultaneously with the use of vasopressors, perform adequate volume ...
Selectively blocks beta 1-adrenergic receptors with little or no effect on beta 2-receptors. Reduces IOP by reducing production ... Levobunolol 0.25% or 0.5% (AK Beta, Betagan). Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous ... Beta-adrenergic blockers. Class Summary. Decrease IOP by reducing aqueous production. Reduce elevated and normal IOP, with or ... Alpha 2-adrenergic agonists. Class Summary. Act to decrease aqueous humor formation. ...
Beta 2 adrenergic receptor · Beta 2 adrenergic receptor blocking agent · Beta 2 adrenergic receptor stimulating agent · ... beta 2 adrenergic receptor · beta 2 adrenergic receptor blocking agent · beta 2 adrenergic receptor stimulating agent · ... beta 1 adrenergic receptor blocking agent · beta 2 adrenergic receptor blocking agent · beta 2 adrenergic receptor stimulating ... Adrenergic beta-Agonists · Adrenergic beta-Antagonists · Atenolol · Clenbuterol · Cytokines · Humans · Interleukin-10 · ...
Here we report that prevention of agonist-stimulated beta 2-adrenergic receptor (beta 2AR) phosphorylation by truncation of its ... Removal of phosphorylation sites from the beta 2-adrenergic receptor delays onset of agonist-promoted desensitization.. Bouvier ... Highly specific receptor kinases, such as rhodopsin kinase and beta-adrenergic receptor kinase, which show stimulus-dependent ... the first direct evidence that one molecular mechanism of desensitization of G-protein-coupled receptors involves their agonist ...
... beta..sub.3 adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to ... sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... beta..sub.1, .beta..sub.2, or .beta..sub.3 adrenergic receptor. Thenon-selective, full .beta.-adrenergic agonist isoproterenol ... beta..sub.1 and .beta..sub.2 Adrenergic Receptors. In vitro .beta..sub.3 receptor agonist activity and selectivity over .beta.. ...
You use a Beta-2 (B2) adrenergic stimulator (a type of drug used to treat asthma), a beta adrenergic blocker (a type of drug ... Association of Beta-2 Adrenergic Agonist and Corticosteroid Injection in the Treatment of Lipomas. The safety and scientific ... Beta-adrenergic agonists and corticosteroid. Drug: Prednisolone synthetic cortisone and Isoproterenol together Approximately ... A Pilot Study: Association of Beta-2 Adrenergic Agonist and Corticosteroid Injection in the Treatment of Lipomas. ...
Alpha/Beta Adrenergic Agonists. Class Summary. These agents augment blood pressure by stimulating dopamine, alpha-adrenergic ... Management of beta-adrenergic blocker and calcium channel antagonist toxicity. Emerg Med Clin North Am. 2007 May. 25(2):309-31 ... The drugs beta-agonist effects include bronchodilatation, chronotropic cardiac activity, and positive inotropic effects. Mix 1 ... This agent does not have beta-adrenergic activity. It produces systemic arterial vasoconstriction, which, in turn, increases ...
Beta-blockers. Class Summary. Topical beta-adrenergic receptor antagonists decrease aqueous humor production by the ciliary ... Adrenergic agonists. Class Summary. Topical agents (sympathomimetics) decrease aqueous production and reduce resistance to ... Beta-adrenergic blocker that has little or no intrinsic sympathomimetic effects and membrane stabilizing activity. Has little ... Timolol is nonselective beta-adrenergic receptor blocker that decreases IOP by decreasing aqueous humor secretion. ...
STUDY DESIGN: beta-Receptor function (response to beta-agonist or forskolin) was tested in monon ... Our purpose was to investigate whether attenuation of beta-adrenergic agonist efficacy during labor is due to elevated ... 31515 - Beta-adrenergic receptors: regulatory role of agonists.. 6286505 - Effect of bordetella pertussis on alpha 1 and beta- ... Adrenergic beta-Agonists / pharmacology*. Cyclic AMP / metabolism. Dinoprostone / pharmacology. Female. Humans. Isoproterenol ...
You can now download VisualDx for your iOS and Android devices. Launch the VisualDx app from your device and sign in using your VisualDx personal account username and password.. ...
Novel Beta Adrenergic Receptor Agonist in the Treatment of Diabetic Retinopathy K. P. Williams; J. Pagadala; D. D. Miller; J. J ... Novel Beta Adrenergic Receptor Agonist in the Treatment of Diabetic Retinopathy You will receive an email whenever this article ... Purpose: : The goal of this study was to test whether a novel beta-adrenergic receptor agonist can reduce apoptosis and TNFα in ... K. P. Williams, J. Pagadala, D. D. Miller, J. J. Steinle; Novel Beta Adrenergic Receptor Agonist in the Treatment of Diabetic ...
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor. ...
... Hydroxybenzylpindolol and Hydroxybenzylpropranolol: Partial Beta Adrenergic Agonists of Adenylate Cyclase in the Rat Adipocyte ... Hydroxybenzylpindolol and Hydroxybenzylpropranolol: Partial Beta Adrenergic Agonists of Adenylate Cyclase in the Rat Adipocyte ... Hydroxybenzylpindolol and Hydroxybenzylpropranolol: Partial Beta Adrenergic Agonists of Adenylate Cyclase in the Rat Adipocyte ...
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation relative to ...
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level relative to isoproterenol. ...
Thus, interference with agonist-occupied beta-adrenergic receptor coupling to adenylate cyclase to produce cAMP and subsequent ... Mechanism of cytokine inhibition of beta-adrenergic agonist stimulation of cyclic AMP in rat cardiac myocytes. Impairment of ... Mechanism of cytokine inhibition of beta-adrenergic agonist stimulation of cyclic AMP in rat cardiac myocytes. Impairment of ... Mechanism of cytokine inhibition of beta-adrenergic agonist stimulation of cyclic AMP in rat cardiac myocytes. Impairment of ...
Beta-1 Adrenergic Agonist Treatment Mitigates Negative Changes in Cancellous Bone Microarchitecture and Inhibits Osteocyte ... Beta-1 Adrenergic Agonist Treatment Mitigates Negative Changes in Cancellous Bone Microarchitecture and Inhibits Osteocyte ... Cite As: Beta-1 adrenergic agonist treatment mitigates negative changes in cancellous bone microarchitecture and inhibits ... However, the exact role that beta-1 adrenergic receptors (beta1AR) have in this process has not been elucidated. We have ...
... adrenergic agonist (βAA) drugs clenbuterol, salbutamol, and terbutaline on metal surfaces has been investigated in this work by ... Improved simultaneous enantioseparation of beta-agonists in CE using beta-CD and ionic liquids.. *Lu Huang, Jin-Ming Lin, ... Adsorption of beta-adrenergic agonists used in sport doping on metal nanoparticles: a detection study based on surface-enhanced ... The adsorption of beta(2)-adrenergic agonist (βAA) drugs clenbuterol, salbutamol, and terbutaline on metal surfaces has been ...
  • also known as L-DOPS, L-threo-dihydroxyphenylserine, L-threo-DOPS and SM-5688), to norepinephrine bypasses the dopamine beta-hydroxylation step of catecholamine synthesis, L-Threo-DOPS is the ideal therapeutic agent. (wikipedia.org)
  • The β 2 adrenoceptor has been cloned and sequenced, and details of how agonist stimulation ultimately results in clinically evident effects are now known. (elsevier.com)
  • The uncertainty was particularly great for people who might be thought to be more susceptible than most to an increase in β adrenergic stimulation from consuming the additive, such as people with cardiovascular disease or children, and that simply increasing the "uncertainty factor" built into the calculation as a safety factor would rapidly become arbitrary. (wikipedia.org)
  • Protein kinase A then goes on to phosphorylate (and thus inactivate) myosin light-chain kinase, which causes smooth muscle relaxation, accounting for the vasodilatory effects of beta 2 stimulation. (wikipedia.org)
  • Stimulation of the D1 receptor by dopaminergic agonists such as fenoldopam is used intravenously to treat hypertensive crisis. (wikipedia.org)
  • ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor. (wikipedia.org)
  • The mechanism of homologous desensitization for the β2 receptor is as follows: Agonist binds and activates the receptor, which changes to an active conformational state. (wikipedia.org)
  • It has been suggested that it may act by making FKBP12.6 (12.6 kilodalton FK506 binding protein, as opposed to 12 kDa FKBP12 which binds to RyR1) which normally bind (and blocks) RyR2 channel tetramer in an average stoichiometry of 3.6, to fall off RyR2 (which is the predominant RyR in pancreatic beta cells, cardiomyocytes and smooth muscles). (wikipedia.org)
  • When differentiated U937 cells were incubated with both LPS and the β-agonist clenbuterol the production of TNF-α and IL-6 was significantly reduced. (tudelft.nl)
  • Objective and Design: To investigate the suppressive effects of the β-agonist clenbuterol on the release of TNF-α and IL-6 in a lipopolysaccharide (LPS)-model of inflammation, both in vitro and in vivo. (tudelft.nl)
  • Conclusions: The β-agonist clenbuterol very potently suppresses the LPS-induced release of the pro-inflammatory cytokines TNF-α and IL-6 both in vitro and in vivo. (tudelft.nl)
  • The β2-selective AR agonist clenbuterol was administered before, during, and after LPS-challenge to investigate its effects on the acute inflammatory response and associated liver-failure. (tudelft.nl)
  • Harefield Recovery Protocol Study (HARPS): A Nonrandomized, Open Label, Multicenter Evaluation of Potential Recovery of Heart Function in Patients With Refractory Chronic Heart Failure by Treatment With Combination of Left Ventricular Assist Device (LVAD), Drugs to Induce Maximal Reverse Remodeling and the Beta-2 Adrenergic Receptor Agonist Clenbuterol. (clinicaltrials.gov)
  • Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) with duration of action of 12 hours or more. (elsevier.com)
  • They were treated with high dose inhaled corticosteroids (500 g fluticasone bid), combined inhaled steroids+long-acting ß2-agonist (500 µg fluticasone+50 µg salmeterol) or placebo for 6 months. (clinicaltrials.gov)
  • The pharmaceutical company Glaxo discovered salmeterol, a long-acting β2-agonist that had bronchodilation activity for up to 12 hours. (wikipedia.org)
  • Inhaled salmeterol works like other β2 agonists, causing bronchodilation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. (wikipedia.org)
  • An aromatic residue, tyrosine 326 in the prototypical human beta 2-adrenergic receptor, exists in a highly conserved sequence motif in virtually all members of the G protein-coupled receptor family. (duke.edu)
  • Increase outflow of aqueous humor through trabecular meshwork and possibly through uveoscleral outflow pathway, probably by a beta2-agonist action. (medscape.com)
  • Shortterm Versus Longterm Treatment With Inhaled Corticosteroids, Either or Not Combined With a Long-Acting Beta2-Agonist. (clinicaltrials.gov)
  • In the early 1960s, James Black, a Scottish pharmacologist, and associates of his at the Imperial Chemical Industries (ICI) in Great Britain were working on a series of β-adrenergic blocking compounds, pronethalol and propranolol. (wikipedia.org)
  • medical citation needed] Metoclopramide[medical citation needed] Dobutamine, a direct-acting beta agonist used in congestive heart failure, also demonstrates tachyphylaxis. (wikipedia.org)
  • citation needed] Today, the FDA defines calamus as 'not intended for human consumption' due to its beta-Asarone content. (wikipedia.org)
  • All effects of the catecholamines adrenaline, noradrenaline, dopamine and isoprenaline could be accounted for by an action as agonists, activating substances, on α- und β-adrenoceptors co-existing in vascular smooth muscle. (wikipedia.org)
  • one for the β-adrenoceptors in the neighbourhood of COMT whose activity is the main factor determining the concentration of the agonist available for the β-effect. (wikipedia.org)
  • The kinetics of airway smooth muscle relaxation, as long as the onset and duration of bronchodilation in asthmatic patients, are reflected by the difference in the mechanism of interaction of short- (SABAs) and longacting β2-agonists (LABAs) and the β2-receptor. (wikipedia.org)
  • This effect could be induced in mononuclear leukocytes from nonlaboring women by preincubation with prostaglandin E but not oxytocin or prostaglandin F. CONCLUSIONS: Prostaglandin E induces heterologous desensitization of the beta-adrenergic receptor system in mononuclear leukocytes, comparable to that seen during labor. (biomedsearch.com)