Wakefulness-Promoting Agents: A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.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.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.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.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.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.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.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Receptors, Adrenergic, alpha: One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.alpha 1-Antitrypsin: Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.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.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.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.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.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.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.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.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)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.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.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.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.Hypoxia-Inducible Factor 1, alpha Subunit: Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.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.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Quinpirole: A dopamine D2/D3 receptor agonist.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.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).Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.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.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).Benzazepines: Compounds with BENZENE fused to AZEPINES.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Piperidines: A family of hexahydropyridines.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.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.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.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.alpha7 Nicotinic Acetylcholine Receptor: A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.Receptors, Adrenergic, alpha-1: A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.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.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.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 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.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)PyrrolidinesReceptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.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.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.Mice, Inbred C57BLCalcium: 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.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.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.

Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat-1 fibroblasts stably expressing alpha1d-adrenoceptors. (1/223)

In rat-1 fibroblasts stably expressing alpha1d-adrenoceptors BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil decreased basal [Ca2+]i. WB 4101 induced a very small effect on this parameter but when added before the other antagonists it blocked their effect. All these agents inhibited the action of norepinephrine. Phorbol myristate acetate also blocked the effect of norepinephrine and decreased basal [Ca2+]i. Staurosporine inhibited these effects of the phorbol ester. Our results suggest that: (1) alpha1d-adrenoceptors exhibit spontaneous ligand-independent activity, (2) BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil act as inverse agonists and (3) protein kinase C activation blocks spontaneous and agonist-stimulated alpha1d-adrenoceptor activity.  (+info)

Regulation of growth in the adult cardiomyocytes. (2/223)

Cardiomyocytes of adult myocardium increase their cellular mass in response to growth stimuli. They undergo hypertrophic growth but they do not proliferate in contrast to immature cardiomyocytes. Growth stimuli of the adult cardiomyocytes include classical growth hormones, various neuroendocrine factors, and the increase in mechanical load. The signal transduction of alpha1-adrenoceptor stimulation has been investigated in greatest detail and may therefore be taken as a reference for other humoral stimuli. It involves the activation of protein kinase C (PKC) and, downstream of PKC activation, of two separate signaling pathways, one including the mitogen-activated protein kinase and another including PI3-kinase and p70(s6k) as key steps. Activation of the first pathway leads to re-expression of fetal genes, activation of the second pathway to a general activation of protein synthesis, and cellular growth. In neonatal cardiomyocytes, mechanical stretch causes growth by an activation of an autocrine mechanism including angiotensin II and endothelin. This mechanism does not operate, however, in adult cardiomyocytes. A mechanism of mechanotransduction has not yet been identified on adult cardiomyocytes but integrins may play a part. In microgravity, the scenario of myocardial growth stimulation is altered. On the systemic level, there are changes in hemodynamic and neuroendocrine regulation that exert indirect effects on the myocardium. Microgravity may also exert a direct cellular effect by the absence of a constant gravitational load component.  (+info)

alpha1-Adrenergic receptor stimulation of mitogenesis in human vascular smooth muscle cells: role of tyrosine protein kinases and calcium in activation of mitogen-activated protein kinase. (3/223)

Signaling pathways of many G protein-coupled receptors overlap with those of receptor tyrosine kinases. We have found previously that alpha1-adrenergic receptors stimulate DNA synthesis and cell proliferation in human vascular smooth muscle cells; these effects were attenuated by the tyrosine protein kinase (TPK) inhibitor genistein and the mitogen-activated protein kinase (MAPK) antagonist 2-aminopurine. Experiments were designed to determine if activation of alpha1 receptors directly stimulated TPKs and MAPKs in human vascular smooth muscle cells. Norepinephrine stimulated time- and concentration-dependent tyrosine phosphorylation of multiple proteins, including p52-, 75-, 85-, 120-, and 145-kDa proteins. Increased TPK activity was demonstrated in proteins precipitated by an antiphosphotyrosine antibody, both in autophosphorylation assays and with a peptide substrate. These effects of norepinephrine were completely blocked by alpha1 receptor antagonists. A membrane-permeable Ca2+ chelator [1,2-bis(o-aminophenoxy)ethane-N,N, N',N'-tetraacetic acid tetra(acetoxymethyl)ester], completely blocked norepinephrine stimulation of phosphorylation of tyrosine proteins, suggesting that intracellular Ca2+ plays a critical role in alpha1 receptor stimulation phosphorylation of tyrosine proteins. Of the tyrosine-phosphorylated proteins, the results suggest that two of them are PLCgamma1 and adapter protein Shc. Also, alpha1 receptor stimulation caused a time-dependent increase in MAPK activity due to increased phosphorylation of p42/44(ERK1/2). The alpha1 receptor-mediated activation of MAPK was also attenuated by TPK inhibitors and intracellular Ca2+ chelator [1, 2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetra(acetoxymethyl)ester]. These results suggest that phosphorylation of tyrosine proteins and intracellular Ca2+ plays a critical role in alpha1 receptor-stimulated MAPK signaling pathways, potentially contributing to increased DNA synthesis and cell proliferation.  (+info)

Analysis of alpha 1L-adrenoceptor pharmacology in rat small mesenteric artery. (4/223)

1. To illuminate the controversy on alpha 1A- or alpha 1L-adrenoceptor involvement in noradrenaline-mediated contractions of rat small mesenteric artery (SMA), we have studied the effects of subtype-selective alpha 1-adrenoceptor agonists and antagonists under different experimental conditions. 2. The agonist potency order in rat SMA was: A61603 >> SKF89748-A > cirazoline > noradrenaline > ST-587 > methoxamine. Prazosin antagonized all agonists with a low potency (pA2: 8.29-8.80) indicating the involvement of alpha 1L-rather than alpha 1A-adrenoceptors. 3. The putative alpha 1L-adrenoceptor antagonist JTH-601, but not the alpha 1B-adrenoceptor antagonist chloroethylclonidine (10 microM) antagonized noradrenaline-induced contractions of SMA. The potency of the selective alpha 1D-adrenoceptor antagonist BMY 7378 against noradrenaline (pA2 = 6.16 +/- 0.13) and of the selective alpha 1A-adrenoceptor antagonist RS-17053 against noradrenaline (pKB = 8.35 +/- 0.10) and against the selective alpha 1A-adrenoceptor agonist A-61603 (pKB = 8.40 +/- 0.09) were too low to account for alpha 1D- and alpha 1A-adrenoceptor involvement. 4. The potency of RS-17053 (pKB/pA2's = 7.72-8.46) was not affected by lowering temperature, changing experimental protocol or inducing myogenic tone via KCl or U46619. 5. Selective protection of a putative alpha 1A-adrenoceptor population against the irreversible action of phenoxybenzamine also failed to increase the potency of RS-17053 (pA2 = 8.25 +/- 0.06 against A61603). 6. Combined concentration-ratio analysis demonstrated that tamsulosin, which does not discriminate between alpha 1A- and alpha 1L-adrenoceptors, and RS-17053 competed for binding at the same site in the SMA. 7. In summary, data obtained in our experiments in rat SMA indicate that the alpha 1-adrenoceptor mediating noradrenaline-induced contraction displays a distinct alpha 1L-adrenoceptor pharmacology. This study does not provide evidence for the hypothesis that alpha 1L-adrenoceptors represent an affinity state of the alpha 1A-adrenoceptor in functional assays. Furthermore, there is no co-existing alpha 1A-adrenoceptor in the SMA.  (+info)

Modulation of the pacemaker current If by beta-adrenoceptor subtypes in ventricular myocytes isolated from hypertensive and normotensive rats. (5/223)

OBJECTIVE: Both beta 1- and beta 2-adrenoceptors (beta 1-AR and beta 2-AR) are functionally present in human and rat ventricular myocytes. The two receptor subtypes are differently regulated during the development of myocardial hypertrophy and failure. I(f) is expressed in human and rat ventricular myocytes. In hypertrophied myocytes isolated from old spontaneously hypertensive rats (SHR) the density is much larger than in age-matched normotensive Wistar Kyoto (WKY). Due to the possible relevance of I(f) as an arrhythmogenic mechanism in the rat and human ventricle, we studied and compared the effects of beta 1-AR and beta 2-AR stimulation on I(f) in both hypertrophied and normal left ventricular myocytes of 18-month old SHR and WKY. METHODS: The whole-cell configuration of the patch-clamp technique was employed. Noradrenaline (NA, 1 microM) was used to stimulate beta 1-AR and isoprenaline (ISO, 1 microM) in the presence of the beta 1-AR antagonist CGP 20712A (0.1 microM) to stimulate beta 2-AR. RESULTS: In SHR, NA increased I(f) by causing a 10.8 +/- 0.9 mV (n = 10) positive shift in the voltage of maximal activation (V1/2); this effect was completely reversed by CGP 20712A. beta 2-AR stimulation was effective in seven out of 13 cells tested, where it caused a small positive shift in V1/2 (4.0 +/- 1.7 mV). Cyclopentyladenosine (CPA), a selective A1-receptor agonist, reversed the effect of NA; the antiadrenergic action of CPA was abolished in cells pre-incubated with pertussis toxin (PTX) to block inhibitory G proteins (Gi). In PTX-treated cells the shift in V1/2 caused by both beta 2-AR (9.6 +/- 1.7 mV, n = 6, p < 0.05) and beta 1-AR (17.6 +/- 1.9 mV, n =7, p < 0.05) was significantly greater than in control cells. Both beta-AR subtypes modulated I(f) activation also in WKY: beta 1-AR shifted V1/2 by 16.0 +/- 1.4 mV (n = 15) and beta 2-AR by 4.2 +/- 1.1 mV (n = 7). However, in PTX-treated WKY cells only the beta 2-AR effect was potentiated (shift in V1/2: 11.4 +/- 1.4 mV, n = 9, p < 0.01), while the beta 1-AR response was unchanged (18.9 +/- 4.2 mV, n = 5, n.s.). CONCLUSIONS: I(f) expressed in SHR hypertrophied ventricular myocytes is modulated by catecholamines mainly through the stimulation of the beta 1-AR subtype. The beta 1-AR response is, however, significantly lower than that observed in myocytes from normotensive rats, probably as a consequence of the presence of an increased inhibitory activity of Gi proteins. This post-receptorial control may be seen as a mechanism to limit the arrhythmogenicity of beta-AR stimulation in myocardial hypertrophy and failure.  (+info)

Ovarian hormone dependence of alpha(1)-adrenoceptor activation of the nitric oxide-cGMP pathway: relevance for hormonal facilitation of lordosis behavior. (6/223)

The ovarian hormones estradiol (E(2)) and progesterone (P) facilitate rat lordosis behavior in part by regulating the expression of and signal transduction by adrenoceptors in the hypothalamus (HYP) and preoptic area (POA). The major adrenoceptor subtype mediating E(2) and P facilitation of lordosis is the alpha(1)-adrenoceptor. In the present studies, we tested the hypotheses that (1) alpha(1)-adrenoceptors in the HYP enhance lordosis responses by activating the nitric oxide (NO)-cGMP signaling pathway, and (2) coupling of alpha(1)-adrenoceptors to this signal transduction pathway is hormone-dependent. Basal levels of cGMP were significantly higher in HYP and POA slices from animals treated with E(2) and P when compared with slices from ovariectomized controls or females treated with only E(2) or P. When slices of HYP and POA from ovariectomized female rats were incubated with norepinephrine or the selective alpha(1)-adrenoceptor agonist phenylephrine, cGMP accumulation was observed only if slices had been derived from females treated with both E(2) and P before experimentation. Moreover, alpha(1)-adrenoceptor stimulation of cGMP synthesis was blocked by an inhibitor of NO synthase, confirming that these receptors act by NO-mediated stimulation of soluble guanylyl cyclase. Behavioral studies demonstrated further that the cell-permeable cGMP analog 8-bromoadenosine-cGMP reverses the inhibitory effects of the alpha(1)-adrenoceptor antagonist prazosin on lordosis behavior in E(2)- and P-treated female rats. Thus, the NO-cGMP pathway mediates the facilitatory effects of alpha(1)-adrenoceptors on lordosis behavior in female rats, and previous exposure of the HYP and POA to both E(2) and P are required to link alpha(1)-adrenoceptors to this pathway.  (+info)

Direct effects of alpha1- and alpha2-adrenergic agonists on spinal and cerebral pial vessels in dogs. (7/223)

BACKGROUND: The effects of adrenergic agonists, often used as local anesthetic additives or spinal analgesics, on spinal vessels have not been firmly established. The authors investigated the effects of alpha2- and alpha1-adrenergic agonists on spinal and cerebral pial vessels in vivo. METHODS: Pentobarbital-anesthetized dogs (n = 28) were prepared for measurement of spinal pial-vessel diameter in a spinal-window preparation. The authors applied dexmedetomidine, clonidine, phenylephrine, or epinephrine in three different concentrations (0.5, 5.0, and 50 microg/ml; [2.1, 1.9, 2.5, and 2.3] x [10(-6), 10(-5), and 10(-4)] M, respectively) under the window (one drug in each dog) and measured spinal pial arteriolar and venular diameters in a sequential manner. To enable the comparison of their effects on cerebral vessels, the authors also administered these drugs under a cranial window. RESULTS: On topical administration, each drug constricted spinal pial arterioles in a concentration-dependent manner. Phenylephrine and epinephrine induced a significantly larger arteriolar constriction than dexmedetomidine or clonidine at 5 microg/ml (8%, 11%, 0%, and 1%, respectively). Spinal pial venules tended to be less constricted than arterioles. In cerebral arterioles, greater constrictions were induced by dexmedetomidine and clonidine than those induced by phenylephrine and epinephrine (14%, 8%, 0%, and 1%, respectively). Cerebral pial venules tended to exhibit larger constrictions than cerebral arterioles (unlike in spinal vessels). CONCLUSION: Dexmedetomidine and clonidine constricted spinal vessels in a concentration-dependent manner, but such vasoconstrictions were smaller than those induced by phenylephrine and epinephrine.  (+info)

Modulation of norepinephrine release by ATP-dependent K(+)-channel activators and inhibitors in guinea-pig and human isolated right atrium. (8/223)

OBJECTIVE: The aim of this study was to show, whether ATP sensitive K+ channels (KATP channels), are involved in the modulation of norepinephrine (NE) release from the sympathetic nerves innervating the guinea-pig and human right atrium. METHODS: The resting and stimulation-evoked release of [3H]norepinephrine ([3H]NE) was measured from the isolated guinea-pig and human right atrium and the effect of activators and inhibitors of ATP sensitive K+ channels was studied. RESULTS: Cromakalim (30-300 microM), a KATP channel-agonist decreased concentration-dependently the stimulation-evoked release of NE from the guinea-pig atrium, an effect, antagonized by glibenclamide, a KATP channel-antagonist (30 microM). Diazoxide (30-300 microM), another activator of the KATP channels reduced the resting release of NE, and also attenuated the evoked release at a single concentration (100 microM), and this latter action was also counteracted by glibenclamide (30 microM). Pinacidil, increased dose-dependently the resting and stimulation-evoked release of NE in a glibenclamide-sensitive manner and reversed the inhibitory effect of cromakalim (100 microM), suggesting that it acts as an antagonist. Glibenclamide (30-300 microM), by itself enhanced the stimulation-evoked release of [3H]NE, and also increased the resting release of NE. On the other hand, 5-hydroxydecanoate, an ischemia-selective inhibitor of cardiac KATP channels did not change NE release. Adenosine, (30-300 microM), an A1-receptor agonist, clonidine (3 microM), an alpha 2-adrenoceptor agonist and oxotremorine, a muscarinic receptor agonist (30 microM) all reduced the evoked release of [3H]NE, but these effects were not modified by glibenclamide (300 microM), indicating that neuronal adenosine (A1), adrenergic (alpha 2) and muscarinic (M3) receptors do not act on KATP channels. In the human right atrium, cromakalim, and diazoxide did not affect significantly the release of [3H]NE. However, glibenclamide (30-300 microM) and pinacidil (30-300 microM) enhanced dose-dependently the evoked-release of NE, and pinacidil also augmented the resting release. CONCLUSIONS: Our results indicate that sympathetic nerve endings of the human and guinea-pig atrium are endowed with ATP-sensitive K+ channels. These channels responded to agonists and antagonists under the experimental conditions applied and they could modulate the release of NE thereby affecting the autonomic control of cardiac function under various physiological and pathophysiological conditions.  (+info)

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TY - JOUR. T1 - Gender differences in the effect of age on electrical field stimulation (EFS)-induced adrenergic vasoconstriction in rat mesenteric resistance arteries. AU - Sullivan, Jennifer C. AU - Davison, Cathy A.. PY - 2001/3/14. Y1 - 2001/3/14. N2 - The objective of this study was to examine the effects of gender and age on electrical field stimulation (EFS)-induced vasoconstriction. Fisher 344 rats were studied: young females (YF, n = 38), young males (YM, n = 29), old females (OF, n = 33), and old males (OM, n = 30). Isolated mesenteric resistance arteries (endothelium-intact or denuded) were pressurized, and outer diameter was monitored. Dose-response curves were performed to KCl and phenylephrine (PE). EFS (0.1-16 Hz) responses were expressed as percentage of constriction from baseline. Area under the curve (AUC) was calculated and comparisons were made using analysis of variance and t tests. Females became less responsive to EFS-induced constriction with age, whereas constrictor ...
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Abstract: As shown by previous studies, adaptation to short-term stress exposure developed the phenomenon of adaptive stabilization of structures (PhASS), including such as elevation in resistance to impairing effects of isolated animal hearts and the heart nuclear fraction of elements of the sarcoplasmic reticulum. Studies of the role of inositol phosphate regulatory cycle in the development of the ASS phenomenon showed that the inositol triphosphate-diacyl glycerol (ITP-DAG) step of regulation was activated at the peak of PhASS development within 15 days after the adaptation onset. The activation observed was accompanied by enhanced activity of phospholipase C as well as by positive inotropic responses of heart tissue to phenylephrine stimulation, which was determined by ITP and DAG accumulation. Within 30 days the inositol phosphate cycle activation was decreased with simultaneous reduction of PhASS. The data obtained suggest that the ITP-DAG step of regulation involved in development of ...
After this repeated doses at steady state, equivalent plasma concentrations are maintained when a Family wellness hemorrhoidal is likely taken every 12 hours as women compared to phenylephrine hbr every 6 hours. Total R - tanna action time also noted improved with phenylephrine, but only shows by 29 minutes. phenylephrine and this possibly of other low potency antipsychotics may therefore reverse the pressor effec
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Clenbuterol is a selective beta-2 adrenoreceptor agonist perfect for fat loss. Like most fat loss medications the body adapts to Clenbuterol rapidly
Indications for VAZCULEP (phenylephrine hydrochloride injection) refers to the medical reasons for why Vazculep is used and recommended as a treatment.
TY - JOUR. T1 - α-1 Adrenergic receptors stimulation induces the proliferation of neural progenitor cells in vitro. AU - Hiramoto, Takeshi. AU - Ihara, Yoshiaki. AU - Watanabe, Yasuhiro. PY - 2006/11/6. Y1 - 2006/11/6. N2 - The proliferation of neural progenitor cells (NPCs) is regulated by classical neurotransmitters such as dopamine, serotonin and acetylcholine, via its own receptors. Previous studies have reported that the depletion of l-norepinephrine decreases the proliferation of NPCs in the adult rat hippocampus and it has been suggested that l-norepinephrine regulates the proliferation of NPCs. However, it remains unknown whether or not adrenergic receptors are involved in the increased proliferation of NPCs. In the present study, an MTT cell proliferation assay was carried out in order to investigate the roles played by adrenergic receptors in the proliferation of NPCs. We demonstrated that l-epinephrine enhanced the proliferation of embryonic NPCs in vitro. In addition, the α-1 ...
TY - JOUR. T1 - Cooling and α1- and α2-adrenergic responses in cutaneous veins. T2 - Role of receptor reserve. AU - Flavahan, Nicholas. AU - Lindblad, L. E.. AU - Verbeuren, T. J.. PY - 1985. Y1 - 1985. N2 - Experiments were designed to determine the effects of cooling on α1- and α2-adrenergic responses in isolated canine cutaneous veins. Rings of saphenous veins were suspended for isometric tension recording in physiological salt solution. Cooling (from 37 to 24°C) augmented contractions to norepinephrine under control conditions and after α1-adrenergic blockade (prazosin) but not following α2-adrenergic blockade (rauwolscine). Cooling augmented contractions evoked by the α2-adrenergic agonists B-HT 920 and UK 14304 but did not affect responses to the full α1-adrenergic agonist phenylephrine. These experiments suggest that cooling augments α2-adrenergic responsiveness without affecting α1-adrenergic responsiveness. However, the contractions evoked by the partial α1-adrenergic ...
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The FDA (Food and Drug Administration, USA) has recommended withdrawing the approval of ProAmatine (midodrine hydrochloride), a Shire Development Inc.
Each caplet of Hemorrhoidal suppositories has 250 mg bid of phenylephrine. The Mucinex multi - action congestion & cold caplets brand managers of phenylephrine should imports be taken with food riots or within 1 hour after eating a meal. I had knelt the choice to go inward with the phenylephrine but after some extended research decided on dronabinol and been on
Phenylephrine is a selective ?1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood...
Aktivierte G-Protein gekoppelte Rezeptoren aktivieren heterotrimere GProteine, in dem sie den Austausch von GDP zu GTP am G-Protein katalysieren. Theoretische Untersuchungen mittels eines vereinfachten kinetischen Modells des Gi/o-Protein Zyklus legen nahe, dass nicht nur GDP-,sondern auch GTP-gebundene Gi/o-Proteine mit aktivierten α2A-adrenergen Rezeptoren (α2A-AR) interagieren können. Demgemäß sollten aktivierte Gi/o-Proteine mit aktivierten α2A-AR vermehrt interagieren, wenn mehr α2A-AR aktiviert werden als für eine maximale G-Protein Aktivierung nötig sind. Dies sollte zu einer paradoxen Deaktivierung von Gi/o-Proteinen und deren Effektorproteinen, z.B. dem G-Protein gekoppelten, einwärtsgleichrichtenden Kaliumkanal (GIRK-Kanal) führen. Mittels FRET lässt sich in lebenden und in permeabilisierten Zellen unter Kontrolle der intrazellulären Nukleotide die Aktivierung von α2A-AR, die Interaktion von Gi/o-Proteinen mit α2A-AR und die Aktivierung von Gi/o-Proteinen bestimmen. Die ...
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Phenylephrine or Neo-Synephrine is an α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure. Phenylephrine has recently been marketed as a substitute for pseudoephedrine but there are recent claims that oral phenylephrine may be no more effective as a decongestant than a placebo.
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All Participants visited the laboratory on 3 occasions for a 4-5 hour observation of blood pressure following administration of a non-selective inhibitor of nitric oxide synthase (L-NAME) an alpha-agonist (midodrine) or placebo. The interventions were administered in random order on separate laboratory visits ...
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Peak plasma adrenaline levels of phenylephrine given as Triacting night time after suspension are ordinarily attained in 1 to 4 hours. Drymax af, containing phenylephrine, is still available as OTC upon who your honourable request to the pharmacist, at on this time. Murfreesboro pharmaceutical and nursing supply filter is a reputed company offering phe
What should I discuss with my healthcare provider before taking codeine and phenylephrine (Ala-Hist AC, Notuss-PE)? How should I take codeine and phenylephrine (Ala-Hist AC, Notuss-PE)?
Removal of endothelial cells on rings of rat aorta increased the sensitivity to the selective alpha-1 adrenoceptor agonist phenylephrine, to the nonselective alpha adrenoceptor agonist norepinephrine and to the selective alpha-2 adrenoceptor agonist clonidine. In the case of the first two, which are strong agonists for the alpha-1 adrenoceptor-mediating contraction, removal of endothelium increased sensitivity 4- and 6-fold at the EC30 level, but produced little or no increase in maximum. In the case of clonidine, a partial agonist for the alpha-1 adrenoceptor, which gave only about 15% of the maximum given by phenylephrine on endothelium-containing rings, removal of the endothelium not only shifted the curve to the left but also increased the maximum to about 50% of that given by phenylephrine. The depression of sensitivity to these agonists in rings with endothelium appeared to be due to the vasodepressor action of endothelium-derived relaxing factor (EDRF), as hemoglobin, a specific blocking ...
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Author: Allen Loyd V Jr, Year: 2013, Abstract: A formulation for preparing Phenylephrine Hydrochloride 10-mg/mL Injection. Includes ingredients, method of preparation, discussion, and references for the compounding pharmacist.
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About 20% of adults faint recurrently. These patients are often highly symptomatic, have problems with employment and driving and have reduced quality of life. There are no therapies that have withstood the test of adequately designed and conducted randomized clinical trials. Midodrine is a prodrug whose metabolite is an alpha-1 adrenergic agonist that increases venous return to the heart and raises blood pressure. There is considerable lower level evidence that it might prevent vasovagal syncope.. The investigators will test the hypothesis that Midodrine prevents recurrences of syncope in patients with moderate to severe vasovagal syncope. ...
Alpha 1 agonists (such as midodrine) cause vasoconstriction (they increase peripheral vascular resistance and decrease venous capacitance) and help to decrease venous pooling. This may be beneficial because some patients have excessive blood pooling in the their extremities when they are upright. ...
and alpha1adrenergic agonists are common ingredients in over-the-counter (OTC) cough and cold preparations. Phenylephrine is also available as nasal drops. Following overdose in children, these agents have the potential to cause serious toxicity incl
Indirect agonists do not physically bind adrenergic receptors. Instead, these compounds indirectly lead to receptor activation through a variety of possible mechanisms which include promoting release of endogenously-stored norepinephrine from presynaptic terminals as well as inhibition of norepinephrine re-uptake and degradation from the synapse ...
It exhibits agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with ... It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ... It exhibits binding affinity against rat 5-hydroxytryptamine 2C receptors using [3H]mesulergine as a radioligand. As of October ... and 5-HT2A receptors in rats. It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat ...
Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ... Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ...
... alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy. 13 (2): ... It is an α1-blocker which acts as an inverse agonist at alpha-1 adrenergic receptors. These receptors are found on vascular ... and syncope are associated with the body's poor ability to control blood pressure without active alpha-adrenergic receptors. ... A larger controlled Phase II "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently ...
... is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Formerly, it was also used to prolong the ... It is the ketone form of epinephrine (adrenaline). Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic ... receptors, but has little affinity for beta receptors. The drug is largely obsolete, being superseded by other hemostatics such ... which is partly a consequence of the vasoconstriction caused by the drug via alpha-1 adrenergic receptors. In an (unspecified) ...
The selective alpha 1 agonist phenylephrine has been used successfully to enhance venous return and stroke volume in some ... "Ganglionic acetylcholine receptor autoantibody: oncological, neurological, and serological accompaniments". Archives of ... In these patients the selective Alpha-1 Adrenergic receptor agonist Midodrine may increase venous return, enhance stroke volume ... POTS is more common in women, with a female-to-male ratio of 5:1. Most people with POTS are aged between 20 and 40, with an ...
... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - ... interferon receptor - interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - ...
Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP- ... Repinotan has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor ... Repinotan acts as a selective high-affinity full receptor agonist at the 5-HT1A receptor subtype. It increases the activity of ...
Alpha-2 Adrenergic Receptor Agonists: A Review of Current Clinical Applications, Giovannitti Jr, J. A., Thoms, S. M., & ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Alpha-2 Adrenergic Receptor Agonists: A Review of Current Clinical Applications, Giovannitti Jr, J. A., Thoms, S. M., & ... This is because adrenergic stimulation by agonists, results in normal calcium channel regulation. If these adrenergic receptors ...
2001). "Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin". J. Biol. Chem. 276 (18): 15003-8. ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic ... "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor". Roberts LR, Fish PV, Ian Storer R, Whitlock GA (April 2009). "6,7-Dihydro ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation". The Journal of Biological ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...
"Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men". The American Journal of ...
... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... ADRA2A adrenergic, alpha-2A-, receptor". "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union ...
See also receptor antagonist) α 2 {\displaystyle \alpha _{2}} receptors. Agonists of α 2 {\displaystyle \alpha _{2}} receptors ... The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... alpha _{2}} receptors in the vascular smooth muscle cells). Usage of β 2 {\displaystyle \beta _{2}} receptor agonists as ... However, in clinical practice drugs applied intravenously that are agonists of α 2 {\displaystyle \alpha _{2}} receptors ( ...
... ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic receptors. ... SN-22, partial agonist at all three 5-HT2 subtypes. Peripherally selective agonistsEdit. One effect of 5-HT2A receptor ... G-protein coupled receptor activity. • virus receptor activity. • signal transducer activity. • drug binding. • G-protein alpha ... The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G ...
Labetalol - an alpha- and beta-adrenergic blocker, given as an intravenous bolus or infusion. Bolus followed by infusion. ... converting enzyme inhibitor or angiotensin II receptor blocker, which can interfere with renal autoregulation and produce acute ... Electroencephalographic examination detects the absence of alpha waves, signifying impaired consciousness. In people with ... J Chronic Dis 1: 33-42. Strandgaard S, Paulson OB (1989) Cerebral blood flow and its pathophysiology in hypertension. Am J ...
local anesthetics) Activators:Agonist: 4-chloro-m-cresol and suramin are direct agonists, i.e., direct activators. Xanthines ... Non-mammalian vertebrates typically express two RyR isoforms, referred to as RyR-alpha and RyR-beta. Many invertebrates, ... Ryanodine receptors are similar to the inositol trisphosphate (IP3) receptor, and stimulated to transport Ca2+ into the cytosol ... It has been shown that calcium release from a number of ryanodine receptors in a ryanodine receptor cluster results in a ...
... is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ... In particular, it is a partial agonist at beta2- receptors located in the vascular smooth muscle. Labetalol relaxes vascular ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ... Labetalol acts by blocking alpha and beta adrenergic receptors, resulting in decreased peripheral vascular resistance without ...
"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 ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ...
3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist". Journal of Medicinal Chemistry. 50 (16 ... The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes ... "Human alpha 2-adrenergic receptor subtype distribution: widespread and subtype-selective expression of alpha 2C10, alpha 2C4, ... Alpha-2-adrenergic receptors include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a ...
... is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi ... also acts as a moderate affinity 5-HT1A receptor agonist, and low affinity CB1 receptor antagonist). Clonidine (also I1 agonist ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... Selective agonists to the beta-1 receptor are: Denopamine Dobutamine (in cardiogenic shock) Xamoterol (cardiac stimulant) (Beta ... "GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation". The Journal ... is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with ...
... or alpha-adrenergic agonists) are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Alpha 2 receptors are associated with sympatholytic properties. α Adrenergic agonists have the opposite function of alpha ... Alpha blocker Adrenergic agonist Beta-adrenergic agonist Declerck I, Himpens B, Droogmans G, Casteels R (September 1990). "The ... MeSH list of agents 82000316 Adrenergic alpha-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH). ...
... which is an α1-receptor agonist and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and ... Desglymidodrine does not stimulate cardiac beta-adrenergic receptors. Desglymidodrine diffuses poorly across the blood-brain ... This is a racemate, ie a 1: 1 mixture of ( R ) - and the ( S ) - form: Midodrine is a prodrug which forms an active metabolite ... Retrieved 1 April 2011. . Midodrine (ProAmatine, generic) Proposed Market Withdrawal - Update September 10, 2010. Shire ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine due to lack of alpha-2 receptor negative feedback and decreased fat accumulation due to epinephrine/ ...
Agonists (−)-Dibromophakellin Antagonists Imiloxan Yohimbine Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000274286 - ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ...
Serotonin Receptor Agonists. Serotonin Agents. Neurotransmitter Agents. Physiological Effects of Drugs. Adrenergic alpha-1 ... Urapidil (Eupressyl*) :IV (PSE) 1 microg/kg/min° until reduction PAM 15 %. Reduction ¼ of the posology to obtain PAM between ...
Adrenergic alpha-1 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Time Frame: Days 1 to 3/4 through patient diary, and followup at days 3/4 an 10/11. ]. ... Time Frame: Assessed during treatment (day 1 to 3/4) by patient diary and questioned by investigator at 1st followup visit. ]. ... Improval of fever by reduction of axillary temperature to less than 38,1°C. [ Time Frame: Assessed by investigator at baseline ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... is a potent vasopressor characterized by both α adrenergic agonistic activity in addition to a weak β adrenergic agonistic ...
Adrenergic alpha-1 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Angiotensin Receptor Antagonists. Molecular Mechanisms of Pharmacological Action. Cardiotonic Agents. Mydriatics. Autonomic ... current treatment with clonidine, beta blockers, angiotensin-converting-enzyme (ACE) inhibitors, or angiotensin II receptor ... Subjects hand will be submerged in cold water (~0-1°C) up to the wrist for 1 minute. ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Norepinephrine Infusion Versus Midodrine & Octreotide in Patients With Hepatorenal Syndrome Type 1.. The safety and scientific ... Sixty patients will be enrolled in the study & randomly assigned in a 1:1 manner to receive either intravenous infusion (IVi) ... Pros & Cons of Norepinephrine Infusion Versus Midodrine & Octreotide in Patients With Hepatorenal Syndrome Type 1 in Intensive ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Drug: 1% tropicamide and 2.5% phenylephrine For the eyes receiving lower conjunctival fornix packing (study group), one small ... Drug: 1% tropicamide and 2.5% phenylephrine For the eyes receiving lower conjunctival fornix packing (study group), one small ... Experimental: 1 Lower conjunctival fornix packing arm. For the eyes receiving lower conjunctival fornix packing (study group), ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Single dose phenylephrine HCl extended release tablet administered after a high-fat, high-calorie breakfast on Day 1 in one of ... Single dose phenylephrine HCl extended release tablet administered under fasted conditions on Day 1 in one of four study ... with the first dose administered under fasted conditions on Day 1 in one of four study periods ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Timeframe is 1 day. ]. A continuous measurement during surgery will be performed. However for further analysis only a short ... cerebral perfusion (rSO2) measured using Near Infrared Spectroscopy [ Time Frame: (day 1) Monitoring will take place only on ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Noradrenaline is a strong-alpha agonist with weak beta-action, too. Therefore, it might prove superior in maintaining cardiac ... neonatal Apgar score will be recorded at 1 min after delivery. The Apgar score is determined by evaluating the newborn baby on ... glucose in neonatal blood [ Time Frame: 1 min post delivery ]. glucose will be measured in the cord blood gas sample taken ...
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Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... The subject is taking medications such as vasodilators, pressors, diuretics, ACE inhibitors, angiotensin receptor blockers, ... beta-blockers, combined alpha and beta-blockers, MAOIs, herbals or specific mixed effect medications. ... Heart Rate at 1 Minute and 10 Minutes Into The Tilt Table Test Conducted 1 and 3 Hours Post-dose at Treatment Visit 2 [ Time ...
Adrenergic neurotransmission as measured by Muscle Sympathetic Nerve Activity(MSNA), doppler ultrasound blood flow, venous ... Heart rate and blood pressure in response to Lower Body Negative Pressure(LBNP) [ Time Frame: 1 year ]. ... Our approach is two-fold: 1) We will use intradermal microdialysis and laser Doppler flowmetry (LDF) to delineate the ... Phenylephrine dose-response comprises infusion of 0.5, 1, 2, 3, 4 micrograms/kg/min for 10 min at each dose. ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Proportion of subjects who used at least once the rescue medication [ Time Frame: Within 2 days and the period of 5 (± 1) days ... Time Frame: Will be evaluated during the 5(± 1) days of treatment ]. Collection of safety data throughout the whole study ... Participants were evaluated (self-assessment) for pain intensity by using a 4-point rating scale: 0=none, 1=mild, 2=moderate, ...
Adrenergic alpha-Agonists. Hypothermia. Cognitive Dysfunction. Cognition Disorders. Neurocognitive Disorders. Mental Disorders ... Adrenergic alpha-1 Receptor Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Primary Hypotheses: Based on our pilot data: (1) 66% of persons with tetraplegia and none of the matched controls will ... Tertiary Aim: To determine if a 10 mg dose of an approved blood pressure-raising medicine (midodrine hydrochloride) will (1) ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Midodrine is a prodrug whose metabolite is an alpha-1 adrenergic agonist that increases venous return to the heart and raises ... Time Frame: 1 year. ]. Secondary Outcome Measures: *A secondary outcome will be the time between the first and second syncope ... Time Frame: 1 year ]. *A secondary outcome will be the frequency of syncopal spells. [ Time Frame: 1 year ]. *A secondary ...
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Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Experimental: Group 1 Fixed dose combination of brompheniramine + phenylephrine.. Drug: Group 1 Brompheniramine + phenylephrine ... Proportion of subjects who used at least once the rescue medication [ Time Frame: Within 2 days and the period of 5 (± 1) days ... Time Frame: Will be evaluated during the 5(± 1) days of treatment ]. Collection of safety data throughout the whole study ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic alpha-Agonists * Adrenergic beta-Agonists * Enzyme Inhibitors * Receptors, Adrenergic, alpha-1 ... we examined the effects of adrenoceptor agonists on firing properties and the intracellular mechanism for alpha(1)-adrenoceptor ... Phenylephrine (100microM), an alpha(1)-adrenoceptor agonist, also increased firing rate, which was inhibited by 100microM ... In agreement with previous reports, bath application of 100microM isoproterenol, a beta-adrenoceptor agonist, increased firing ...
Adrenergic Agonist Agent, Ophthalmic. *Nonsteroidal Anti-inflammatory Drug (NSAID), Ophthalmic. *Ophthalmic Agent, Mydriatic ... Phenylephrine: Alpha1-adrenergic receptor agonist; it causes dilation of the pupil by contracting the radial muscle of the iris ... Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1- ... Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. ...
Traditional Chinese remedy for asthma that is a non-selective adrenergic agonist ... Muscarinic receptor that is mostly active in airway smooth muscle contraction and mucus hyper-secretion ... 3 effects of alpha adrenergic stimulation 1. smooth muscle contraction. 2. vasoconstriction. 3. slight bronchoconstriction ... 1. NO-mediated relaxation of smooth muscle, vasodilation. 2. MLCK-mediated contraction capillary endothelium, making ...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic alpha-1 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. To Top ... Number of patients who will receive diuretics in both groups [ Time Frame: 1 year ]. *Adverse effects of drugs in both groups ... Survival in both groups [ Time Frame: 1 year ]. *Incidence of therapeutic paracentesis in both groups [ Time Frame: Day 30 ]. * ...
  • The primary psychoactive component of Cannabis, delta 9-tetrahydrocannabinol (Δ9-THC), demonstrates its effects through weak partial agonist activity at Cannabinoid-1 (CB1R) and Cannabinoid-2 (CB2R) receptors. (drugbank.ca)
  • NE, after pretreatment with hexamethonium and phentolamine, reduced mean arterial pressure 40 +/- 5% from 117 +/- 9 mmHg and TPR 60 +/- 5% from 0.058 +/- 0.007 mmHg X ml-1 X min and increased cardiac output 55 +/- 11% from 2,159 +/- 188 ml/min. (biomedsearch.com)
  • α1-AR gain-of-function in cardiac transgenic models generally supports the KO results, although phenotypes vary greatly with receptor level, promoter, and absence or presence of an activating mutation. (pubmedcentralcanada.ca)
  • 19 Recently, we found that modest augmentation of cardiac α1A signaling with a subpressor dose of an α1A-selective agonist can prevent doxorubicin-induced cardiomyopathy in mice. (pubmedcentralcanada.ca)
  • Actions of the β2 receptor include: Heart muscle contraction increase cardiac output (minor degree compared to β1). (wikipedia.org)
  • On the other hand, constantly active alpha 1 b adrenergic receptor mice have rather opposite effects, with more cardiac issues, and an increase in neurodegeneration . (scientificamerican.com)
  • DesglyMidodrine does not stimulate cardiac beta-adrenergic receptors. (drugs.com)
  • In skeletal muscle, activation of ryanodine receptors occurs via a physical coupling to the dihydropyridine receptor (a voltage-dependent, L-type calcium channel), whereas, in cardiac muscle, the primary mechanism of activation is calcium-induced calcium release, which causes calcium outflow from the sarcoplasmic reticulum. (wikipedia.org)
  • The cardiac-specific isoform of the receptor (RyR2) is known to form a quaternary complex with luminal calsequestrin, junctin, and triadin. (wikipedia.org)
  • Labetalol acts by blocking alpha and beta adrenergic receptors, resulting in decreased peripheral vascular resistance without significant alteration of heart rate or cardiac output. (wikipedia.org)
  • Actions of the β1 receptor include: stimulate viscous, amylase-filled secretions from salivary glands Increase cardiac output Increase heart rate in sinoatrial node (SA node) (chronotropic effect) Increase atrial cardiac muscle contractility. (wikipedia.org)
  • Aminophylline competitively antagonizes the cardiac actions of adenosine at the cell surface receptors. (wikipedia.org)
  • The block on alpha-2 receptors further potentiates beta-effects, increasing cardiac output. (wikipedia.org)
  • Individuals with cocaine overdose should be transported immediately to the nearest emergency department, preferably by ambulance in case cardiac arrest occurs en route. (wikipedia.org)
  • Alpha actin is also expressed as distinct genetic isoforms such as smooth muscle, cardiac muscle and skeletal muscle specific isoforms of alpha actin. (wikipedia.org)
  • The ratio of actin to myosin is between 2:1 and 10:1 in smooth muscle, compared to ~6:1 in skeletal muscle and 4:1 in cardiac muscle. (wikipedia.org)
  • Just as in A1 receptors, this normally serves as a protective mechanism, but may be destructive in altered cardiac function. (wikipedia.org)
  • Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
  • The building of the wave is done by the feedback mechanism of the ryanodine receptor the activation of phospholipase C by GPCR or RTK, which leads to the production of inositol trisphosphate, which in turn activates the InsP3 receptor. (wikipedia.org)
  • Dihydroergocryptine (DHEC, trade names Almirid, Cripar) is a dopamine agonist of the ergoline chemical class that is used as an antiparkinson agent. (wikipedia.org)
  • Initial monotherapy with a dopamine agonist (other examples include pergolide, pramipexole, and ropinirole) is associated with reduced risk for motor complications in Parkinson patients relative to levodopa. (wikipedia.org)
  • Pramipexole (Mirapex, Mirapexin, Sifrol) is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS). (wikipedia.org)
  • L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. (wikipedia.org)
  • Because PGE2 activates multiple prostanoid receptors and has a short half-life in vivo due to its rapidly metabolism in cells by omega oxidation and beta oxidation], metabolically resistant EP1-selective activators are useful for the study of EP1's function and could be clinically useful for the treatment of certain diseases. (wikipedia.org)