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.
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.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
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.
Drugs that bind to and activate dopamine receptors.
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.
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.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
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.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
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.
Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.
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.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
Drugs that selectively bind to and activate alpha adrenergic receptors.
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.
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.
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.
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.
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.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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.
A selective D1 dopamine receptor agonist used primarily as a research tool.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
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 is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.
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.
Drugs that bind to and activate adrenergic receptors.
A dopamine D2/D3 receptor agonist.
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.
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).
Drugs that bind to and activate excitatory amino acid receptors.
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.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Compounds with BENZENE fused to AZEPINES.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
A family of hexahydropyridines.
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.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
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.
Drugs that selectively bind to and activate beta-adrenergic receptors.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
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.
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.
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.
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.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
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.
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)
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.
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.
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.
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.
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.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
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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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 ...
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The crystal structure of the α1B-adrenergic receptor has been determined in complex with the inverse agonist (+)-cyclazosin. ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1B adrenergic receptor (α1B-adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 2003). "The adaptor complex 2 directly interacts with the alpha 1b-adrenergic receptor and plays a role in receptor endocytosis ...
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... with alpha-adrenoceptor blocking and beta2-adrenoceptor agonist-associated vasorelaxant activities". J Cardiovasc Pharmacol. 34 ... Beta-adrenergic agonists, All stub articles, Cardiovascular system drug stubs). ... Eugenodilol is an alpha-1 blocker and beta blocker with weak β2-adrenergic receptor agonist activity derived from eugenol. ... 1): 10-20. doi:10.1097/00005344-199907000-00003. PMID 10413061. v t e (Articles with short description, Short description ...
Chen L, Du JB, Jin HF, Zhang QY, Li WZ, Wang L, Wang YL (September 2008). "[Effect of selective alpha1 receptor agonist in the ... A high number of patients has elevated levels of autoantibodies against the adrenergic alpha 1 receptor and against the ... Elevations of autoantibodies targeting adrenergic α1 receptor has been associated with symptoms severity in patients with POTS ... April 1999). "Abnormal norepinephrine clearance and adrenergic receptor sensitivity in idiopathic orthostatic intolerance". ...
"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 ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... Agonists (activators) of the α2-adrenergic receptor are frequently used in anaesthesia where they affect sedation, muscle ...
Angiotensin receptor blockers (ARB) and calcium channel blockers (CCB), alpha- and beta- adrenergic receptor blockers ... Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ... DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic+Blockers at the US National Library of Medicine Medical ... Silodosin is the most selective for alpha-1a receptors. The affinity and selectivity for alpha-1 receptors seems to be ...
... an α2A adrenergic receptor agonist. Medetomidine, an α2 adrenergic agonist. Nonspecific agonists act as agonists at both alpha- ... Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha ... Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... but there was an increased incidence of hypotension and bradycardia Alpha blocker Adrenergic agonist Beta-adrenergic agonist ...
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 ...
... 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 - ...
... is a selective α1-adrenergic receptor agonist which results in the constriction of both arteries and veins. ... Damage may be prevented or mitigated by infiltrating the tissue with the alpha blocker phentolamine by subcutaneous injection. ... Because this medication is a sympathomimetic amine without beta-adrenergic activity, it does not increase contractility force ... Phenylephrine selectively binds to alpha-1 receptors which cause blood vessels to constrict. Whereas pseudoephedrine causes ...
... is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, ... Arnsten, A.F.T.; Jentsch, J.D. (September 1997). "The Alpha-1 Adrenergic Agonist, Cirazoline, Impairs Spatial Working Memory ... Ruffolo, R. R. Jr.; Waddell, J. E. (1982). "Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist ... and a nonselective antagonist to the α2 adrenergic receptor. It is believed that this combination of properties could make ...
Alpha-2 adrenergic receptor agonists, Beta-adrenergic agonists, Catechol ethers, Catecholamines, Ophthalmology drugs, ... It increases outflow of the aqueous humour and also reduces its formation (mediated by its action on α1 and α2 receptors), thus ... It also increases the conductivity of trabecular filtering cells (a β2 receptor mediated action). It is preferred to ...
Alpha-2 adrenergic receptor agonists, Chloroarenes, Guanidines, Imidazolines, Sympathomimetic amines, Ophthalmology drugs). ... It is an α2 adrenergic receptor agonist and a weak α1 adrenergic receptor agonist.[citation needed] Topical apraclonidine is ... Apraclonidine is useful in this case due to its weak α1-adrenergic properties. When applied to the denervated (and thus hyper- ... The affected pupil is thus miotic and the pupillary dilator responds to denervation by increasing α1 receptors. ...
... is a sulfonamide α1-adrenergic receptor agonist. MacLean MR, Thomson M, Hiley CR (June 1989). "Pressor effects of the alpha 2- ... adrenoceptor agonist B-HT 933 in anaesthetized and haemorrhagic rats: comparison with the haemodynamic effects of amidephrine ... Alpha-1 adrenergic receptor agonists, Phenylethanolamines, Sulfonamides, All stub articles, Cardiovascular system drug stubs). ...
... compounds elicit smooth muscle activation leading to vasoconstriction by interacting with cell surface adrenergic receptors. ... Alpha-1 adrenergic receptor agonists, Sympathomimetic amines). ...
Alpha-2 adrenergic receptor agonists, Decongestants, Imidazolines, 1-Naphthyl compounds, Vasoconstrictors, Ophthalmology drugs) ... It is a sympathomimetic agent with marked alpha adrenergic activity that acts on alpha-receptors in the arterioles of the ... Naphazoline is a mixed α1- and α2-adrenergic receptor agonist. The non-hydrochloride form of Naphazoline has the molecular ...
It is an α1-adrenergic receptor agonist with some β effect. It is currently sold in its generic form by Slayback Pharma. ... Metaraminol at higher doses may have direct alpha-adrenergic agonist and beta-1 adrenergic agonist effects. However at doses ... McDonald M, Santucci R (2004). "Successful management of stuttering priapism using home self-injections of the alpha-agonist ... Beta-adrenergic agonists, Cardiac stimulants, Phenylethanolamines, Phenols, Substituted amphetamines, All stub articles, ...
Alpha-2 adrenergic receptor agonists, Allyl compounds, Azepanes, D2-receptor agonists, Dopamine agonists, Thiazoles, All stub ... Talipexole is a D2 dopamine receptor agonist and interacts both pre- and post-synaptic receptors. It also is an α2-adrenergic ... Talipexole (B-HT920, Domnin) is a dopamine agonist that is marketed as a treatment for Parkinson's Disease in Japan by ... Page accessed 9 December 2014 Benkert O, Müller-Siecheneder F, Wetzel H (1995). "Dopamine agonists in schizophrenia: a review ...
Alpha-1 adrenergic receptor agonists, Phenylethanolamines, Pivalate esters, Sympathomimetics, All stub articles, Nervous system ...
These receptors have mainly been studied in insects, where they can be divided into distinct types: OctαR (alpha-adrenergic- ... The Octopamine/Tyramine receptors (including Oct-TyrR) can bind both ligands, and display agonist-specific coupling. Oct-TyrR ... OctαR (OCTOPAMINE1 receptors) are more closely related to α-adrenergic receptors, while OctβR (OCTOPAMINE2 receptors) are more ... TyrR (mixed octopamine/tyramine receptors), which are structurally and functionally similar to noradrenergic alpha-2 receptors ...
GNTI has been found to act as a positive allosteric modulator of the α1A-adrenergic receptor (EC50 = 41 nM), and this may ... Alpha-1 adrenergic receptor agonists, Guanidines, Indolomorphinans, Irreversible antagonists, Kappa-opioid receptor antagonists ... Obara I, Mika J, Schafer MK, Przewlocka B (October 2003). "Antagonists of the kappa-opioid receptor enhance allodynia in rats ... April 2003). "Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats". The Journal of ...
Alpha-2 adrenergic receptor agonists, Antimigraine drugs, Biased ligands, Ergot alkaloids, Lactams, Lysergamides, ... Ergotamine interacts with serotonin, adrenergic, and dopamine receptors. It is an agonist of serotonin receptors including the ... Ergotamine is an agonist of the serotonin 5-HT2B receptor and has been associated with cardiac valvulopathy. Despite acting as ... or a 5-HT1 receptor agonist (e.g., sumatriptan). Side effects of ergotamine include nausea and vomiting. At higher doses, it ...
Alpha-2 adrenergic receptor agonists, Beta-adrenergic agonists, Catecholamines, Norepinephrine releasing agents, ... 275-. ISBN 978-3-88763-075-1. "DailyMed - Search results for levonordefrin". DailyMed. Retrieved 20 February 2016. Sjoerdsma A ...
Alpha-2 adrenergic receptor agonists, Bayer brands, Imidazolines, Merck & Co. brands, Phenols, Schering-Plough brands, Tert- ... A direct sympathomimetic, oxymetazoline binds to and activates α1 adrenergic receptors and α2 adrenergic receptors, most ... their primary effects appear on α adrenergic receptors, with little if any effect on β adrenergic receptors. Like other ... α2 adrenergic receptors. Since vascular beds widely express α1 receptors, the action of oxymetazoline results in ...
Alpha-2 adrenergic receptor agonists, Imidazolines, Tetralins, Topical decongestants, Vasoconstrictors). ... Tetryzoline is an alpha agonist for the alpha-2 receptor and an imidazoline receptor I-1 agonist. Mainly due to its alpha-2 ... Lowry JA, Brown JT (June 2014). "Significance of the imidazoline receptors in toxicology". Clinical Toxicology. 52 (5): 454-69 ... the dry mouth and sedating effects of tetryzoline are due to alpha-2 agonism. In a healthy person, the biological half-life of ...
Alpha-2 adrenergic receptor agonists, Antihypertensive agents, Chloroarenes, Chloropyrimidines, Imidazolines, Phenol ethers, ... Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of ... a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice". The Journal of ... Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). This receptor subtype is found in both the ...
Alpha-2 adrenergic receptor agonists, Phytocannabinoids, CB1 receptor antagonists, Resorcinols, Terpeno-phenolic compounds). ... It appears to be unique among cannabinoid compounds by also having high affinity and activity at alpha-2 adrenergic receptors ... the potent activity of cannabigerol at alpha-2 adrenergic receptors raises concerns about its safety for human consumption, ... that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor ...
Alpha2-adrenergic agonists, such as brimonidine and apraclonidine, work by a dual mechanism, decreasing aqueous humor ... Less-selective alpha agonists, such as epinephrine, decrease aqueous humor production through vasoconstriction of ciliary body ... Topical beta-adrenergic receptor antagonists, such as timolol, levobunolol, and betaxolol, decrease aqueous humor production by ... Alpha 2 agonists (brimonidine, apraclonidine) both decrease fluid production (via inhibition of AC) and increase drainage. ...
... the dopamine D2 receptor, and the α1-adrenergic receptor. The weak antiserotonergic effects of hydroxyzine likely underlie its ... Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action ... Alpha-1 blockers, Antiemetics, Anxiolytics, Belgian inventions, D2 antagonists, Ethers, H1 receptor antagonists, ... identification of 4-methylhistamine as the first potent and selective H4 receptor agonist". The Journal of Pharmacology and ...
... while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of ... rabbits respond to alpha and beta MSH's (therefore not using the ACTH receptor), and guinea pigs responding to both ACTH and ... the receptor is glycosylated and expressed on the cell plasma membrane. MCR's have both endogenous agonists and antagonists. α- ... The adrenocorticotropic hormone receptor or ACTH receptor also known as the melanocortin receptor 2 or MC2 receptor is a type ...
In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is ... Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be ... Martin SW, Broadley KJ (May 1995). "Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade". Br ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ...
February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... and dopamine D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and ... Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug ...
5-HT1A agonists, Adrenergic receptor modulators, Alpha-2 blockers, Aminotetralins, D1-receptor agonists, D2-receptor agonists, ... D5 receptor (Ki = 5.4 nM) α1A-adrenergic receptor (Ki = 176 nM) α1B-adrenergic receptor (Ki = 273 nM) α2A-adrenergic receptor ( ... α2B-adrenergic receptor (Ki = 27 nM) α2C-adrenergic receptor (Ki = 135 nM) 5-HT1A receptor (Ki = 30 nM) 5-HT7 receptor (Ki = 86 ... D3 receptor agonists, D4 receptor agonists, D5 receptor agonists, Phenols, Thiophenes). ...
Dual effects of yohimbine, rauwolscine and corynanthine as alpha-adrenoceptor antagonists and 5-HT-receptor agonists". Naunyn- ... Corynanthine acts as an α1-adrenergic and α2-adrenergic receptor antagonist with approximately 10-fold selectivity for the ... and rauwolscine which have around 30-fold higher affinity for the α2-adrenergic receptor over the α1-adrenergic receptor. As a ... Doxey JC, Lane AC, Roach AG, Virdee NK (February 1984). "Comparison of the alpha-adrenoceptor antagonist profiles of idazoxan ( ...
... binds to α2-adrenergic receptor and imidazoline receptor binding sites, and blocks NMDA receptors and other cation ... Nicotinic, imidazoline I1 and I2, α2-adrenergic (no intrinsic activity-neither agonist nor antagonist), glutamate NMDAr, and ... "Agmatine recognizes alpha 2-adrenoceptor binding sites but neither activates nor inhibits alpha 2-adrenoceptors". Naunyn- ... while agmatine binds to α2-adrenergic receptors, it exerts neither an agonistic nor antagonistic effect on these receptors, ...
Clinically, non-selective alpha antagonists block alpha receptors (but do not differentiate between alpha-1 and alpha-2). They ... Phenoxybenzamine also has irreversible antagonist/weak partial agonist properties at the serotonin 5-HT2A receptor. Due to its ... Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of ... As a non-selective alpha receptor antagonist, it will also affect both the postsynaptic alpha 1 and presynaptic alpha 2 ...
GnRH receptor agonists, such as leuprorelin and goserelin, were subsequently developed and used to treat prostate cancer. ... In general, treatment often begins with an alpha-1 adrenergic receptor antagonist medication such as tamsulosin, which reduces ... This is often done through the use of GnRH analogues or agents that block the receptors that androgens act at, such as ... or male chronic pelvic pain syndrome is treated by a large variety of modalities including the medications alpha blockers, ...
Inhalation of an agonist for the beta-2 adrenergic receptor, such as salbutamol (albuterol in the US), is the most common ... caused by alpha-adrenoceptor downregulation and desensitization. The mechanism may specifically include receptor ... July 2000). "The effect of polymorphisms of the beta(2)-adrenergic receptor on the response to regular use of albuterol in ... beta-2 agonists is more apparent in Arg-16 individuals because their receptors have not been downregulated prior to agonist ...
They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ... Alpha-2 blockers, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor antagonists). ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ... Iprindole also lacks significant alpha-blocking properties, and hence does not pose a risk of orthostatic hypotension. In ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ...
... dopamine mainly triggers dopamine receptors and β1-adrenergic receptors while at high doses it works via α-adrenergic receptors ... Alpha-1 adrenergic receptor stimulation on vascular smooth muscle, leads to vasoconstriction and results in an increase in ... Dopamine agonists, Vasoconstrictors, Inotropic agents, World Health Organization essential medicines, Wikipedia medicine ... and β2 adrenergic receptors. Cruickshank, Laura; Kennedy, Alan R.; Shankland, Norman (2013). "Tautomeric and ionisation forms ...
Alpha-2 adrenergic receptor agonists, Beta-adrenergic agonists, Cardiac stimulants, Phenylethanolamines, Phenols). ... adrenaline and some phenylephrine derivatives on alpha-, beta- and beta- adrenergic receptors". South African Medical Journal ... suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much ... These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. Nusser E, Donath H, Russ W (August 1965 ...
... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 22 (1): 54-60. ISSN 0090-838X. PMC 6761819. PMID 15706734. Taivainen, H.; Laitinen, K.; Tähtelä, R.; Kilanmaa, K.; Välimäki, M ...
... adrenergic agonists MeSH D27.505.519.625.050.100.100 - adrenergic alpha-agonists MeSH D27.505.519.625.050.100.200 - adrenergic ... estrogen receptor modulators MeSH D27.505.696.399.450.360.315 - estrogen antagonists MeSH D27.505.696.399.450.360.315.300 - ... adrenergic agonists MeSH D27.505.696.577.050.100.100 - adrenergic alpha-agonists MeSH D27.505.696.577.050.100.200 - adrenergic ... beta-agonists MeSH D27.505.519.625.050.200 - adrenergic antagonists MeSH D27.505.519.625.050.200.100 - adrenergic alpha- ...
... is a drug which acts as a selective agonist of the β3 adrenergic receptor, which has been investigated for various ... "Agonist and antagonist characterization of a putative adrenoceptor with distinct pharmacological properties from the alpha- and ... Afeli SA, Rovner ES, Petkov GV (September 2013). "BRL37344, a β3-adrenergic receptor agonist, decreases nerve-evoked ... September 2018). "β3-adrenergic receptor activation induces TGFβ1 expression in cardiomyocytes via the PKG/JNK/c-Jun pathway". ...
... is an alpha agonist that is selective to the alpha-2 adrenergic receptor. Guanabenz is used as an antihypertensive drug, i.e. ... Alpha-2 adrenergic receptor agonists, Chloroarenes, Guanidines, All stub articles, Antihypertensive agent stubs). ... 10 (1): 6-14. doi:10.1177/030006058201000102. PMID 7037502. S2CID 2139809.[permanent dead link] Bonham AC, Trapani AJ, Portis ...
... an adrenergic alpha-agonist, or an antihistamine nasal spray without risk of rhinitis medicamentosa. Nasal saline irrigation (a ... Kamekura R, Kojima T, Takano K, Go M, Sawada N, Himi T (2012). "The Role of IL-33 and Its Receptor ST2 in Human Nasal ... Th2 cells contribute to the body's inflammatory response to allergens, and specific ST2 receptors, also known as IL1RL1, on ... Another study focusing on Han Chinese children found that certain SNPs in the protein tyrosine phosphatase non-receptor 22 ( ...
Ephedrine Pseudoephedrine Adrenergic receptor Alpha adrenergic agonist List of adrenergic drugs Siegel, George J; et al. (2006 ... the adrenergic receptors). Directly acting adrenergic agonists act on adrenergic receptors. All adrenergic receptors are G- ... An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of ... Agonists of each class of receptor elicit these downstream responses. Indirectly acting adrenergic agonists affect the uptake ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Recombinant activated protein C (drotrecogin alpha) was originally introduced for severe sepsis (as identified by a high APACHE ... There are four families of PRRs: the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I- ... This forced receptor interaction induces the production of pro-inflammatory chemical signals (cytokines) by T-cells. There are ...
Ligand-activated DP1 also mobilizes G protein-coupled receptor kinase 2 (GRK2, also known as β-Adrenergic receptor kinase 2 [ ... 2007). "Synergistic effect of PGD2 via prostanoid DP receptor on TNF-alpha-induced production of MCP-1 and IL-8 in human ... "Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ...
Increased level of norepinephrine increases the basal activity of alpha-2 adrenergic receptors, which mediate an analgesic ... Serotonin receptor antagonists, Sigma agonists, Sodium channel blockers, Tricyclic antidepressants, TrkB agonists, World Health ... Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K (June 2009). "Amitriptyline is a TrkA and TrkB receptor agonist ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ...
Receptors, Adrenergic, alpha-2/agonists. Adrenergic alpha-2 Receptor Agonists. Receptors, Adrenergic, alpha-2/antagonists & ... Receptors, Adrenergic, beta-2/agonists. Adrenergic beta-2 Receptor Agonists. Receptors, Adrenergic, beta-2/antagonists & ... Receptors, Adrenergic, beta-3/agonists. Adrenergic beta-3 Receptor Agonists. Receptors, Adrenergic, beta-3/antagonists & ...
... also called alpha-blockers) are a family of agents that bind to and inhibit type 1 alpha-adrenergic receptors and thus inhibit ... Adrenergic agonists and antagonists. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilmans the pharmacological basis ... alpha-1b receptors) and in the bladder neck and prostate (alpha-1a receptors), they are also useful in the therapy of symptoms ... Recently, selective alpha-1a adrenergic receptors blockers have been developed for use in benign prostatic hypertrophy that are ...
... also called alpha-blockers) are a family of agents that bind to and inhibit type 1 alpha-adrenergic receptors and thus inhibit ... Adrenergic agonists and antagonists. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilmans the pharmacological basis ... alpha-1b receptors) and in the bladder neck and prostate (alpha-1a receptors), they are also useful in the therapy of symptoms ... Recently, selective alpha-1a adrenergic receptors blockers have been developed for use in benign prostatic hypertrophy that are ...
α-adrenergic antagonists *Phosphodiesterase Type 5 inhibitors *Mixed α- and β-receptor antagonists ... Phenylephrine is an alpha-1 adrenergic receptor agonist. Phenylephrine Hydrochloride Injection, USP 10 mg per mL, is a clear, ... Antagonistic effects (decrease in phenylephrine hydrochloride blood pressure effect) can occur with α-adrenergic antagonists, ... Phenylephrine Hydrochloride Injection is an alpha-1 adrenergic receptor agonist indicated for the treatment of clinically ...
Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRF R1, CRF R2; ... Molecular targets for which radioligands (agonist, antagonist, allosteric modulator) are needed include, but are not limited to ... neurokinin receptors: NK1, NK2, NK3; neuronal nicotinic receptor subunits: alpha 7 & alpha 4 beta 2; NMDA subunits; opioid ... This FOA is intended to stimulate the development of radioligands for molecular targets (e.g., receptors, cell adhesion ...
Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRF R1, CRF R2; ... Molecular targets for which radioligands (agonist, antagonist, allosteric modulator) are needed include, but are not limited to ... neurokinin receptors: NK1, NK2, NK3; neuronal nicotinic receptor subunits: alpha 7 & alpha 4 beta 2; NMDA subunits; opioid ... This FOA is intended to stimulate the development of radioligands for molecular targets (e.g., receptors, cell adhesion ...
MeSH Terms: Acetylcholine/pharmacology; Adrenergic alpha-1 Receptor Agonists/pharmacology; Animals; Aorta/enzymology; Aorta/ ... metabolism; Aorta/physiology*; Cholinergic Agonists/pharmacology; Cyclic GMP/metabolism; Glutamate-Cysteine Ligase/genetics*; ...
Distribution of alpha 1C-adrenergic receptor mRNA in adult rat tissues by RNase protection assay and comparison with alpha 1B ... 5. Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes.. Minneman KP; Theroux TL; Hollinger S; Han C; ... 4. The rat homologue of the bovine alpha 1c-adrenergic receptor shows the pharmacological properties of the classical alpha 1A ... 2. Cloning of the human alpha 1d-adrenergic receptor and inducible expression of three human subtypes in SK-N-MC cells. ...
... alpha-2 adrenergic receptor agonist; may reduce acqueous humor formation. Pharmacokinetics. Peak Plasma Time: 3-5 hr (reduction ... APRACLONIDINE SOLUTION 1% - OPHTHALMIC (A-pra-KLOE-ni-deen) COMMON BRAND NAME(S): Iopidine USES: This medication is used to ... 1 gtt of a 1% solution onto the eye undergoing surgery 1 hour before surgery & repeated immediately upon completion of surgery ... Place one finger at the corner of your eye (near the nose) and apply gentle pressure for 1 to 2 minutes. This will prevent the ...
Adrenergic Agonists [D27.505.519.625.050.100] * Adrenergic alpha-Agonists [D27.505.519.625.050.100.100] * Adrenergic alpha-1 ... Receptor Agonists [D27.505.519.625.] * Adrenergic alpha-2 Receptor Agonists [D27.505.519.625.] ... Adrenergic Agonists [D27.505.696.577.050.100] * Adrenergic alpha-Agonists [D27.505.696.577.050.100.100] * Adrenergic alpha-1 ... Adrenergic alpha1-Agonists Registry Number. 0. Previous Indexing. Adrenergic alpha-Agonists (1995-2010). Sympathomimetics (1966 ...
Prostaglandin F2-alpha analog. Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral ... Alpha 2-adrenergic agonists. Class Summary. Act to decrease aqueous humor formation. ... A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. Has minimal ... Prostaglandin F2-alpha analog. Selective FP prostanoid receptor agonist believed to reduce IOP by increasing uveoscleral ...
Neural regulation of the effects of alpha adrenergic agonists On automaticity. Circ Res (1986) 57(3):415-423. ... Trophic influence of sympathetic neurons on the cardiac alpha-adrenergic response requires close nerve-muscle association. Dev ... where she studied the role of sympathetic innervation on the alpha-adrenergic chronotropic response of cultured cardiac ... The results of this project identified a functional pertussis toxin substrate by which the alpha 1-adrenergic response becomes ...
Phenylephrine possesses predominantly Alpha-adrenergic effects. In the eye, phenylephrine acts locally as a potent ... Phenylephrine Hydrochloride Ophthalmic Solution, USP 2.5 percent and 10 percent is an alpha-1 adrenergic receptor agonist used ...
Adrenergic alpha Agonist. Adrenergic alpha Agonists. Adrenergic alpha Receptor Agonist. Adrenergic alpha Receptor Agonists. ... Adrenergic alpha-Agonist. Adrenergic alpha-Receptor Agonist. Adrenergic alpha-Receptor Agonists. Agonist, Adrenergic alpha- ... Agonists, alpha-Adrenergic. Agonists, alpha-Adrenergic Receptor. alpha Adrenergic Agonist. alpha Adrenergic Agonists. alpha ... alpha Adrenergic Receptor Agonists. alpha-Adrenergic Agonist. alpha-Adrenergic Agonists. alpha-Adrenergic Receptor Agonist. ...
Adrenergic Agonists [D27.505.519.625.050.100] * Adrenergic alpha-Agonists [D27.505.519.625.050.100.100] * Adrenergic alpha-1 ... Receptor Agonists [D27.505.519.625.] * Adrenergic alpha-2 Receptor Agonists [D27.505.519.625.] ... Adrenergic Agonists [D27.505.696.577.050.100] * Adrenergic alpha-Agonists [D27.505.696.577.050.100.100] * Adrenergic alpha-1 ... Adrenergic alpha1-Agonists Registry Number. 0. Previous Indexing. Adrenergic alpha-Agonists (1995-2010). Sympathomimetics (1966 ...
Human PIVs (HPIVs) are currently divided into 5 serotypes-HPIV-1, HPIV-2, HPIV-3, HPIV-4a, and HPIV-4b-in 2 different genera: ... Respirovirus (HPIV-1 and HPIV-3) and Rubulavirus (HPIV-2 and HPIV-4). ... Racemic epinephrine solution causes alpha-adrenergic receptor-mediated vasoconstriction of edematous tissues, thereby reversing ... Alpha/Beta Agonists. Class Summary. When delivered by air or oxygen-powered devices, epinephrine is directly delivered to ...
Matched Categories: … Alpha-and Beta-adrenergic Agonists … Matched Products: … Pseudoephedrine Hydrochloride ... ... agonist and N-methyl-d-aspartate (NMDA) receptor antagonist. As a full MOR agonist, methadone mimics the natural effects of the ... It is a highly lipophilic synthetic phenylpiperidine opioid that is structurally similar to opiate receptor agonists such as ... Matched Categories: … Alpha and Beta Blocking Agents and Thiazides ... labetalol and thiazides ... Alpha and Beta Blocking ...
Dexmedetomidine hydrochloride in 0.9% sodium chloride injection is a alpha 2-adrenergic receptor agonist indicated for: (1) ... Dexmedetomidine is a relatively selective centrally acting alpha 2-adrenergic agonist with sedative properties. Alpha 2 ... Dexmedetomidine hydrochloride is a central alpha2-adrenergic agonist. Dexmedetomidine hydrochloride is the S-enantiomer of ... Both alpha 1 and alpha 2 activity is observed following slow intravenous infusion of high doses (≥1,000 mcg/kg) or with rapid ...
Receptors, Antigen, T-Cell, alpha-beta. *Receptors, Estrogen. *Receptors, Growth Factor. *Receptors, Vascular Endothelial ... Adrenergic alpha-1 Receptor Agonists. *Adult. *Advisory Committees. *Age Factors. *Age of Onset ...
... and an alpha 2 adrenergic receptor agonist (Brimonidine Tartrate 0.2%).[1],[4] It combines the two drugs into one multi-dose ... 1],[2] In both studies, Simbrinza achieved a 5mm Hg to 9mm Hg reduction from baseline to Month 3. Patients mean IOP at ... 1],[3]. About Glaucoma. More than 67 million people worldwide have glaucoma, which is the second-leading cause of preventable ... 1],[2],[3]. In the two, three-month clinical trials, the most frequently reported adverse reactions in patients treated with ...
... adrenergic receptor agonist. The relaxant effect of HSE was partly dependent on the presence of a functional endothelium as the ... with a greater potency against the alpha(1)- ... by a non selective opioid receptor antagonist, naloxone. Subhan ... 1. Clinical efficacy of the co-administration of Turmeric and Black seeds (Kalongi) in metabolic syndrome - a double blind ... activity of Ac.Cr in the gut though the preferential binding of the constituents of betel nut extract at muscarinic receptor ...
Montgomery (2017) An Alpha-1A Adrenergic Receptor Agonist Prevents Acute dox. Cardiomyopathy in Male Mice. Plos One 12 e0168409 ... α1-adrenergic, alpha1-adrenergic, a1-Adrenergic, alpha2a-Adrenergic, a2a-Adrenergic, Receptors, Adrenergic, Alpha-1, Alpha-2, ... Home / Pharmacology / GPCRs / 7-TM Receptors / Adrenergic Receptors / Adrenergic α1 Receptors / Adrenergic α1 Receptor Agonists ... Partial α2A adrenoceptor agonist and α1A agonist. Agonist/antagonist activity at 5-HT receptors. ...
Phenylephrine Hydrochloride Ophthalmic Solution, USP 2.5% and 10% is an alpha-1 adrenergic receptor agonist indicated to dilate ...
Soluble Amyloid Precursor Protein alpha (sAPP alpha). beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) ... Repurposing beta-3 adrenergic receptor agonists for Alzheimers disease: beneficial effects in a mouse model BIBLIOGRAPHIC ... through β3 adrenergic receptor (β3AR) agonists or cold acclimation, counteracts metabolic deficits in rodents and humans. ... Methods: CL-316,243, a specific β3AR agonist, was administered to the triple transgenic mouse model of AD (3xTg-AD) and non- ...
Alpha-adrenergic agonists.). Antipsychotics - Quetiapine is by far the most common antipsychotic medication prescribed for ... Melatonin receptor agonist (ramelteon) - Ramelteon is a melatonin receptor agonist approved for the treatment of insomnia in ... Benzodiazepine receptor agonists - Benzodiazepine receptor agonists (BZRAs) for insomnia include five older benzodiazepines ( ... a melatonin receptor agonist; low-dose doxepin, a histamine receptor antagonist; and the dual orexin receptor antagonists ( ...
3.3.3. Alpha-2-adrenergic agonists. Perioperative systemic use of alpha-2 agonists such as clonidine and dexmedetomidine also ... These include the NMDA receptor ketamine, the alpha-2-delta ligands pregabalin and gabapentin and the alpha-2-adrenergic ... Other components such as ketamine and alpha-2 agonists are used in specific indications. The role of corticosteroids is not yet ... 3.3.2. Alpha-2-delta ligands. The alpha-2-delta ligands pregabalin and gabapentin, which were developed for the treatment of ...
An wonderful instance of the response of adrenergic receptors to different plasma concentrations of agonist. Shows up to 75- ... Alpha 1-adrenergic receptor subtypes, inositol phosphates, and sources of cell Ca2. Vasopressin: mechanisms of motion on the ... Dopamine receptors are G-protein� coupled receptors that exist in a number of subtypes (Table 12. Akathisia is an unpleasant ... adrenergic receptors by vessel mattress and age. Surviving sepsis campaign: International pointers for management of severe ...
... alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, ... it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. ... binding assays at concentrations up to 100 microM and did not exhibit affinity for a number of other common receptor sites, ... or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not ...
... selective alpha2-adrenergic receptor agonist that is 1000-fold more selective for the alpha2-adrenergic receptor than the alpha ... The concomitant use of other systemic alpha adrenergic receptor agonists may potentiate the undesirable effects of this class ... Alcon Brimonidine® P (brimonidine tartrate ophthalmic solution) 0.1% or 0.15% is an alpha adrenergic receptor agonist indicated ... Cutaneous facial application of a highly selective alpha2-adrenergic receptor agonist reduces erythema through direct cutaneous ...
  • The alpha-1 adrenergic receptor antagonists (also called alpha-blockers) are a family of agents that bind to and inhibit type 1 alpha-adrenergic receptors and thus inhibit smooth muscle contraction. (nih.gov)
  • At present, however, the alpha-1 adrenergic antagonists are recommended only as adjunctive therapy of hypertension and not as monotherapy. (nih.gov)
  • Because the nonselective alpha-1 adrenergic antagonists cause a relaxation of smooth muscle both in arterioles (alpha-1b receptors) and in the bladder neck and prostate (alpha-1a receptors), they are also useful in the therapy of symptoms of urinary obstruction due to benign prostatic hypertrophy. (nih.gov)
  • Antagonistic effects (decrease in phenylephrine hydrochloride blood pressure effect) can occur with α-adrenergic antagonists, phosphodiesterase Type 5 inhibitors, mixed α- and β-receptor antagonists, calcium channel blockers, benzodiazepines and ACE inhibitors, centrally acting sympatholytic agents. (nih.gov)
  • 17. Phenylalanine in the second membrane-spanning domain of alpha 1A-adrenergic receptor determines subtype selectivity of dihydropyridine antagonists. (nih.gov)
  • Pretreatment of macrophage cultures with beta(2)- (ICI-118551) but not beta(1)-adrenergic (atenolol) receptor antagonists reversed the epinephrine-mediated cytokine attenuation following LPS treatment. (nih.gov)
  • The alpha-2B preferential antagonists ARC-239, prazosin or chlorpromazine failed to block the modifications in both glycemic and insulin levels induced by alpha-2 adrenoceptor stimulation. (aspetjournals.org)
  • The nonselective antagonists rauwolscine, yohimbine, WY 26703, phentolamine and corynanthine, as well as the receptor antagonists with alpha-2A selectivity like WB 4101, idazoxan and tolazoline, dose-dependently antagonized both the glycemic and the insulin responses to UK 14.304. (aspetjournals.org)
  • This increase in M2 receptor density is consistent with the change in affinity of the antagonists for inhibition of carbachol induced contractions and may indicate that M2 receptors or a combination of M2 and M3 receptors directly mediate smooth muscle contraction in bladders from DEN and NV SCI rats. (inra.fr)
  • Studies on the specificity of receptor antagonists showed that both the inhibition of adenylate cyclase by norepinephrine and the subsequent increase in adenylate cyclase activity are mediated by alpha-receptors. (nih.gov)
  • Proposed Course: The potencies of alpha-receptor activators and antagonists with respect to inhibition of adenylate cyclase will be compared with the effects of ligand binding to NG108-15 alpha-receptors. (nih.gov)
  • Effects of alpha-adrenergic activators and antagonists on [3H] dihydroergocryptine binding will be determined to define the specificity of the alpha-receptor and the kinetics of binding. (nih.gov)
  • To determine the sites through which dexmedetomidine injection into the LC produces antinociception, the authors examined whether this response could be perturbed by the specific alpha(2)-adrenergic antagonists atipamezole and L659,066 and pertussis toxin administered either into the LC or intrathecally before injection of dexmedetomidine systemically or directly into the LC. (asahq.org)
  • This antinociceptive effect was blocked by pertussis toxin and by the alpha(2) antagonists atipamezole and L659,066 placed in the LC. (asahq.org)
  • Part of the mechanism by which dexmedetomidine produces an antinociceptive effect is by an action directly on the LC, demonstrated by these studies in which antinociception produced by injection of this drug into the LC can be blocked by specific alpha(2) antagonists injected into the LC. (asahq.org)
  • MATERIAL AND METHODS: Effect of melatonin (25-100 mg/kg, ip) and its interaction with putative melatonin receptor antagonists and opioidergic and serotoninergic agents have been studied in formalin test, a model of tonic continuous pain. (who.int)
  • Both mianserin and ondansetron the 5HT2 and 5HT3 receptor antagonists, respectively increased the analgesic effect of melatonin. (who.int)
  • Postural hypotension is particularly common after the initial dose of the alpha-1 adrenergic antagonist. (nih.gov)
  • 3. Identification of critical extracellular loop residues involved in alpha 1-adrenergic receptor subtype-selective antagonist binding. (nih.gov)
  • Agonist/antagonist activity at 5-HT receptors. (tocris.com)
  • These include the alpha-2 adrenergic agonists clonidine and guanfacine, the nonselective beta-adrenergic agent propranolol, and most promising prazosin, which is an alpha-1 adrenergic receptor antagonist that blocks the actions of NE on alpha-1 receptors(Petrakis, 2016). (professionalacademictutors.com)
  • Both the effect on glycemic level and the inhibition of insulin release by oxymetazoline were antagonized by the alpha-2 adrenoceptor antagonist idazoxan. (aspetjournals.org)
  • PTAC was highly selective for muscarinic receptors, was a partial agonist at muscarinic M2/M4 receptors and an antagonist at M1, M3 and M5 receptors. (inra.fr)
  • Cells were cultured in the presence of norepinephrine for 0-48 hours, then the effects of withdrawal of norepinephrine either by replacing the medium or by the addition of a receptor antagonist was tested. (nih.gov)
  • Luzindole, a ML1 receptor antagonist did not block but rather enhanced the antinociceptive activity of melatonin. (who.int)
  • However, prazosin, a ML2 receptor antagonist in the low dose (0.5 mg/kg) significantly attenuated but in higher dose (1 mg/kg) enhanced the analgesic effect of melatonin. (who.int)
  • Naloxone, an opioid receptor antagonist did not reverse but morphine, an opioid agonist enhanced the antinociceptive activity of melatonin. (who.int)
  • Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous humor production and possibly increases outflow of aqueous humor. (medscape.com)
  • The alpha-2A preferential agonist oxymetazoline induced in the mouse a hyperglycemic response similar to that of the nonselective alpha-2 adrenoceptor agonist UK 14.304. (aspetjournals.org)
  • Labetalol hydrochloride (HCl) is an adrenergic receptor blocking agent that has both selective alpha 1 -adrenergic and nonselective beta-adrenergic receptor blocking actions in a single substance. (nih.gov)
  • Labetalol HCl combines both selective, competitive, alpha 1 -adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. (nih.gov)
  • indeed at least one study has shown an increase in heart failure, stroke and cardiovascular disease with long term therapy with alpha-blockers. (nih.gov)
  • Recently, selective alpha-1a adrenergic receptors blockers have been developed for use in benign prostatic hypertrophy that are claimed to have less effect on blood pressure. (nih.gov)
  • Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or oral), and alpha 2-agonists. (medscape.com)
  • beta 1-blockers with beta 2 agonist activity are vasodilatory because they activate postsynaptic beta 2 receptors on vascular smooth muscle cell membranes, via the formation of cyclic AMP. (eleanorrigby-movie.com)
  • Beta blockers, also known as beta-adrenergic blocking agents, are a class of drugs that works by blocking the neurotransmitters norepinephrine and epinephrine from binding to receptors. (eleanorrigby-movie.com)
  • The two main beta receptors that are targeted by beta blockers are the beta 1 receptor and the beta 2 receptor. (eleanorrigby-movie.com)
  • 11. Identification of alpha 1-adrenergic receptor subtypes in human corpus cavernosum tissue and in cultured trabecular smooth muscle cells. (nih.gov)
  • Subtype selective immunoprecipitation of muscarinic receptors revealed an increase in total and an increase in M2 receptor density with no change in M3 receptor density in bladders from DEN and NV SCI animals compared to normal or sham operated controls. (inra.fr)
  • The specific cellular response to muscarinic receptor activation is dependent upon appropriate expression of each of the five muscarinic receptor genes by individual cells. (inra.fr)
  • The role of muscarinic receptors in schizophrenia was investigated using the muscarinic agonist PTAC. (inra.fr)
  • The drug has minimal to no binding affinity for 5-HT 3 , dopamine, muscarinic, histamine (H 1 ), opioid, or alpha-1 or alpha-2 adrenergic receptors. (drugtopics.com)
  • Similar rapid inhibitions and compensatory increases elicited by opiate and muscarinic cholinergic receptor agonists have been recently observed by others. (nih.gov)
  • Partial α 2A adrenoceptor agonist and α 1A agonist. (tocris.com)
  • Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36. (hdhpharma.com)
  • Blocks beta 1- and beta 2-receptors and has mild intrinsic sympathomimetic effects. (medscape.com)
  • Selectively blocks beta 1-adrenergic receptors with little or no effect on beta 2-receptors. (medscape.com)
  • The beta-2 receptors are located in the bronchioles of the lungs and the arteries of the skeletal muscles. (eleanorrigby-movie.com)
  • Dr. Drugge received a doctoral degree in Pharmacology from Columbia, P & S, where she studied the role of sympathetic innervation on the alpha-adrenergic chronotropic response of cultured cardiac myocytes. (nymc.edu)
  • 1. Cloning, expression, and tissue distribution of the rat homolog of the bovine alpha 1C-adrenergic receptor provide evidence for its classification as the alpha 1A subtype. (nih.gov)
  • 4. The rat homologue of the bovine alpha 1c-adrenergic receptor shows the pharmacological properties of the classical alpha 1A subtype. (nih.gov)
  • 6. Expression of alpha 1-adrenergic receptor subtype mRNA in rat tissues and human SK-N-MC neuronal cells: implications for alpha 1-adrenergic receptor subtype classification. (nih.gov)
  • 13. Pharmacological properties of the cloned alpha 1A/D-adrenoceptor subtype are consistent with the alpha 1A-adrenoceptor characterized in rat cerebral cortex and vas deferens. (nih.gov)
  • Guanfacine is a selective alpha-2A adrenergic receptor agonist in that it has 15-20 times higher affinity for this receptor subtype than for the alpha-2B or alpha-2C subtypes. (allsales.in)
  • 5. Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. (nih.gov)
  • To test the possibility that one of the postulated subtypes of alpha-2 adrenoceptors is preferentially implicated in this response, we compared the interaction of several drugs with known selectivity toward alpha-2A or alpha-2B adrenoceptor subtypes in our model. (aspetjournals.org)
  • Phenylephrine Hydrochloride Ophthalmic Solution, USP 2.5 percent and 10 percent is an alpha-1 adrenergic receptor agonist used for dilation of the pupil due to its vasoconstrictor and mydriatic action. (send2press.com)
  • Phenylephrine Hydrochloride Ophthalmic Solution, USP 2.5% and 10% is an alpha-1 adrenergic receptor agonist indicated to dilate the pupil. (paragonbioteck.com)
  • Alcon Brimonidine® P (brimonidine tartrate ophthalmic solution) 0.1% or 0.15% is an alpha adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (pillintrip.com)
  • Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS . (nih.gov)
  • Such regulation may modulate the cell's responsiveness to ligands for other species of receptors which activate adenylate cyclase and thus may affect information transfer in the nervous system. (nih.gov)
  • Through various cellular signaling mechanisms, hormones and medications activate the beta-1 receptor. (eleanorrigby-movie.com)
  • Dopamine and dobutamine activate the myocardial beta1 receptor and thus increase the force of contraction of the failing heart. (eleanorrigby-movie.com)
  • ß2-Adrenergic receptor agonists (ß2-agonists) activate PKA, and we hypothesized that ß2-agonists would beneficially impact HDE-induced adverse airway inflammatory consequences. (cdc.gov)
  • Three subtypes of melatonin receptors, i.e. (who.int)
  • AIM: To investigate the antinociceptive activity of melatonin and to unravel the underlying receptor mechanisms involved in this action. (who.int)
  • CONCLUSION: The present results suggest the involvement of ML2 receptors in mediating the antinociceptive activity of melatonin in formalin-induced pain response. (who.int)
  • Further an interplay between melatonin, alpha-1 adrenergic and 5HT2 and 5HT3 serotoninergic receptors may also be participating in this action. (who.int)
  • These studies demonstrate that beta(1)-adrenergic receptors play a dominant role in the murine vascular system to mediate vasodilation. (eleanorrigby-movie.com)
  • The authors examined whether alpha(2)-adrenergic receptors in the LC mediate an antinociceptive effect. (asahq.org)
  • Racemic epinephrine solution causes alpha-adrenergic receptor-mediated vasoconstriction of edematous tissues, thereby reversing upper airway edema. (medscape.com)
  • In concentrations of 1:1000, L-epinephrine may be used in place of racemic epinephrine for nebulized administration. (medscape.com)
  • Macrophage cultures from CLP animals incubated with either epinephrine or IL-10 for 2 h had significantly reduced TNF-alpha and IL-6 release in response to LPS. (nih.gov)
  • Glucocorticoids alter the sensitivity of epinephrine in influencing memory consolidation and, conversely, adrenergic activation induced by emotional arousal appears to be essential in enabling glucocorticoid modulation of memory consolidation. (scholarpedia.org)
  • 1 ] Guanfacine is a non-stimulant. (allsales.in)
  • Preclinical research suggests guanfacine modulates signalling in the prefrontal cortex and basal ganglia through direct modification of synaptic noradrenalin transmission at the alpha 2- adrenergic receptors. (allsales.in)
  • Which medication selectively antagonizes alpha-1 adrenergic receptors and antagonizes beta-1 and beta-2 adrenergic receptors? (eleanorrigby-movie.com)
  • Tegaserod, by acting as an agonist at neuronal 5-HT 4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. (drugtopics.com)
  • Their use in therapy of hypertension is based on the inhibition of vascular resistance in arterioles from alpha-adrenergic blockade, which results in an increase in venous capacitance and lowering of blood pressure. (nih.gov)
  • Alpha-2 adrenoceptor stimulation induces in the mouse a hyperglycemic response which is accompanied by a concomitant inhibition of insulin secretion. (aspetjournals.org)
  • Beta 2 -receptor blockade was demonstrated by inhibition of the isoproterenol-induced fall in diastolic blood pressure. (nih.gov)
  • Furthermore, prolonged exposure of cells to alpha receptor agonists results in an increase in adenylate cyclase activity which compensates for the inhibition. (nih.gov)
  • Alpha(2)-Adrenergic agonists such as clonidine and dexmedetomidine are known to produce sedation and analgesia in humans. (asahq.org)
  • Phenylephrine possesses predominantly Alpha-adrenergic effects. (send2press.com)
  • Tegaserod is a selective partial agonist at the serotonin-4 (5-HT 4 ) receptor and possesses gastrointestinal prokinetic activity. (drugtopics.com)
  • The average NG108-15 cell possesses 60,000 alpha-receptors. (nih.gov)
  • 9. Quantification of steady state expression of mRNA for alpha-1 adrenergic receptor subtypes using reverse transcription and a competitive polymerase chain reaction. (nih.gov)
  • 15. Distribution of alpha 1C-adrenergic receptor mRNA in adult rat tissues by RNase protection assay and comparison with alpha 1B and alpha 1D. (nih.gov)
  • Ablation of the Stimulatory G Protein α-Subunit in Renal Proximal Tubules Leads to Parathyroid Hormone-Resistance With Increased Renal Cyp24a1 mRNA Abundance and Reduced Serum 1,25-Dihydroxyvitamin D. (nih.gov)
  • The fact that dual regulation of NG108-15 adenylate cyclase has been observed now with three classes of inhibitors each mediated by a different species of receptor, suggests that dual regulation may be a general phenomenon. (nih.gov)
  • Brown adipose tissue (BAT) is the main thermogenic driver in mammals and its stimulation, through β3 adrenergic receptor (β3AR) agonists or cold acclimation, counteracts metabolic deficits in rodents and humans. (nih.gov)
  • Since metabolic disorders and AD share strong pathogenic links, we hypothesized that BAT stimulation through a β3AR agonist could exert benefits in AD as well. (nih.gov)
  • Enhanced adrenergic stimulation and catecholamine release are important components of the pathophysiology of sepsis. (nih.gov)
  • Under physiological conditions, adrenergic stimulation has been shown to be a negative regulator of proinflammatory cytokine production through increasing IL-10 production. (nih.gov)
  • Here we have investigated if adrenergic stimulation similarly inhibits TNF-alpha and IL-6 production by splenic macrophages isolated from a polymicrobial sepsis model. (nih.gov)
  • Data are also presented that demonstrate the involvement of protein kinase A activation with adrenergic agonist but not with IL-10 stimulation. (nih.gov)
  • Bronchial epithelial cells were cultured with the short-acting ß2-agonist salbutamol or the long-acting ß2-agonist salmeterol prior to stimulation with HDE. (cdc.gov)
  • 1],[2] The studies evaluated the safety and efficacy of a fixed-dose combination of Brinzolamide 1.0% and Brimonidine 0.2%, administered three times daily, compared to separate three-times-per-day dosing of one or the other component. (europeanpharmaceuticalreview.com)
  • Three-month randomized trial of fixed-combination Brinzolamide 1%/Brimonidine 0.2% versus Brinzolamide 1% versus Brimonidine 0.2% in patients with open-angle glaucoma or ocular hypertension. (europeanpharmaceuticalreview.com)
  • Solution containing 1 or 1.5 mg/mL brimonidine tartrate. (nih.gov)
  • Taken together, these findings suggest that adrenergic mechanisms may influence peripheral tissue macrophage inflammatory cytokine response following trauma and sepsis, independent of the effects of IL-10. (nih.gov)
  • Major Findings: NG108-15 hybrid cells possess alpha-adrengeric receptors which in concert with receptor activators inhibit adenylate cyclase. (nih.gov)
  • Beta-adrenergic blocker that has little or no intrinsic sympathomimetic effects and membrane-stabilizing activity. (medscape.com)
  • In animals, at doses greater than those required for alpha-or beta-adrenergic blockade, a membrane stabilizing effect has been demonstrated. (nih.gov)
  • However, glucocorticoids may also act more rapidly by interacting with membrane receptors and/or potentiating the efficacy of the norepinephrine-signal cascade via an interaction with G-protein-mediated actions. (scholarpedia.org)
  • An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent. (reference.md)
  • In man, the ratios of alpha- to beta-blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. (nih.gov)
  • Labetalol HCl's beta 1 -receptor blockade in man was demonstrated by a small decrease in the resting heart rate, attenuation of tachycardia produced by isoproterenol or exercise, and by attenuation of the reflex tachycardia to the hypotension produced by amyl nitrite. (nih.gov)
  • p-F-HHSiD inhibited carbachol induced contraction with an affinity consistent with M2 receptors in bladders from NV SCI (pKb=6.4) animals and M3 receptors in bladders from SPV SCI animals (pKb=7.9). (inra.fr)
  • When beta-1 receptors are stimulated they increase the heart rate and increase the heart's strength of contraction or contractility. (eleanorrigby-movie.com)
  • Several randomized controlled trials have found that the alpha-1 blocker prazosin is effective in reducing symptoms of posttraumatic stress disorder (PTSD) among active-duty soldiers(Roundup, 2017). (professionalacademictutors.com)
  • J Clin Invest (2017 Feb 1) 127:500-510. (nih.gov)
  • Selective alpha 2-receptor that reduces aqueous humor formation and increases uveoscleral outflow. (medscape.com)
  • A relatively selective alpha-adrenergic agonist that does not have significant local anesthetic activity. (medscape.com)
  • That is, labetalol is a selective alpha and non-selective beta blocker. (eleanorrigby-movie.com)
  • All of the approved medications have been evaluated for efficacy and safety in short-term placebo-controlled randomized trials in adults with insomnia disorder [ 1 ]. (uptodatefree.ir)
  • To date, a number of adrenergic agents have been tested for their efficacy in treating PTSD. (professionalacademictutors.com)
  • Tegaserod is a 5-HT 4 agonist that has demonstrated efficacy in the short-term treatment of women with IBS whose primary bowel symptom is constipation. (drugtopics.com)
  • 14. Increased voltage-dependent calcium influx produced by alpha 1B-adrenergic receptor activation in rat medullary thyroid carcinoma 6-23 cells. (nih.gov)
  • The memory-modulating effects of glucocorticoids appear to involve the selective activation of the low-affinity glucocorticoid receptor. (scholarpedia.org)
  • Activation of 5-HT 4 receptors in the GI tract by tegaserod stimulates the peristaltic reflex and intestinal secretion, in addition to inhibiting visceral sensitivity. (drugtopics.com)
  • Targeted activation of the beta-1 receptor increases heart rate, renin release, and lipolysis. (eleanorrigby-movie.com)
  • Targeted activation of the beta-1 receptor in the heart increases sinoatrial (SA) nodal, atrioventricular (AV) nodal, and ventricular muscular firing, thus increasing heart rate and contractility. (eleanorrigby-movie.com)
  • Furthermore, the action of dexmedetomidine in the LC in turn may result in an increase in activation of alpha(2) adrenoceptors in the spinal cord, because the antinociceptive effect of LC dexmedetomidine injection also can be blocked by intrathecal injection of antipamezole and pertussis toxin. (asahq.org)
  • ß2-Agonist treatment significantly increased PKA activation and significantly decreased HDE-stimulated IL-6 and IL-8 production in a concentration- and time-dependent manner. (cdc.gov)
  • While the antinociceptive response to alpha(2) agonists, given intrathecally, is mediated predominantly in the spinal cord, other sites of action have not been systematically studied. (asahq.org)
  • Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia. (aspetjournals.org)
  • The beta-adrenergic receptors belong to the family of G-protein coupled receptors. (eleanorrigby-movie.com)
  • G-protein stimulatory subunit alpha and Gq/11α G-proteins are both required to maintain quiescent stem-like chondrocytes. (nih.gov)
  • 1],[2],[3] In addition, it is the only available, fixed-dose combination therapy for glaucoma in the US without a beta blocker. (europeanpharmaceuticalreview.com)
  • 1],[4] It combines the two drugs into one multi-dose bottle, helping to reduce the medication burden for glaucoma patients. (europeanpharmaceuticalreview.com)
  • ALPHAGAN ® P is an alpha adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (nih.gov)
  • Glucocorticoids act through intracellular and intranuclear receptors and can affect gene transcription by direct binding of receptor homodimers to DNA . (scholarpedia.org)
  • Salbutamol treatment significantly reduced HDE-induced intracellular adhesion molecule-1 expression and neutrophil adhesion to epithelial cells. (cdc.gov)
  • Phenylephrine Hydrochloride Injection is an alpha-1 adrenergic receptor agonist indicated for the treatment of clinically important hypotension resulting primarily from vasodilation in the setting of anesthesia. (nih.gov)
  • As β3AR agonists are being clinically developed for metabolic disorders, repurposing them in AD could be a valuable therapeutic strategy. (nih.gov)
  • Project Description: Objectives: Alpha-receptor activators such as norepinephrine rapidly lower cAMP levels of NG108-15 cells by inhibiting adenylate cyclase activity. (nih.gov)
  • 2. Norepinephrine released at adrenergic synapses may regulate cAMP levels in post-synaptic or pre-synaptic cells by the mechanism discussed here. (nih.gov)
  • Unlike CBT with a trauma focus, EMDR does not involve (a) detailed descriptions of the event, (b) direct challenging of beliefs, (c) extended exposure, or (d) homework" (p. 1)(Hurley, 2018). (professionalacademictutors.com)
  • Using an established intranasal inhalation exposure model, we found that salbutamol pretreatment reduced airway neutrophil influx and IL-6, TNF-alpha, CXCL1, and CXCL2 release in bronchoalveolar lavage fluid following a one-time exposure to HDE. (cdc.gov)
  • Together, these results support the need for future clinical investigations to evaluate the utility of ß2-agonist therapies in the treatment of airway inflammation associated with CAFO dust exposure. (cdc.gov)
  • The results of this project identified a functional pertussis toxin substrate by which the alpha 1-adrenergic response becomes linked to a decrease in automaticity present only in myocytes co-cultured with sympathetic neurons. (nymc.edu)
  • Both the alpha-and beta-blocking actions of orally administered labetalol HCl contribute to a decrease in blood pressure in hypertensive patients. (nih.gov)
  • Thus an alpha-blocker medication causes vasodilation and can be used to treat hypertension. (eleanorrigby-movie.com)
  • The beta 1 receptor is vital for the normal physiological function of the sympathetic nervous system. (eleanorrigby-movie.com)
  • Here, we show that β3AR agonist administration decreased body weight and improved peripheral glucose metabolism and BAT thermogenesis in both non-transgenic and 3xTg-AD mice. (nih.gov)
  • Glucocorticoids are highly lipophilic and, thus, readily enter the brain and bind directly to mineralocorticoid receptors and glucocorticoid receptors. (scholarpedia.org)
  • 12. Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. (nih.gov)
  • An adrenergic agonist primarily of α1 and β1 receptors used as an anti-hypotensive. (eleanorrigby-movie.com)
  • A beta-1 agonist used to treat cardiac decompensation in patients with organic heart disease or from cardiac surgery. (eleanorrigby-movie.com)
  • One-month treatment with a β3AR agonist increased recognition index by 19% in 16-month-old 3xTg-AD mice compared to pre-treatment (14-month-old). (nih.gov)
  • Male B(6)D(2)F(1) mice were subjected to sham (S), laparotomy (Lap), and cecal ligation and puncture (CLP) under anesthesia. (nih.gov)
  • Formalin (0.1 ml of 1% solution) was injected under the plantar surface of right hind paw of mice and the time an animal spent in licking the injected paw was measured. (who.int)
  • β2-adrenergic agonists attenuate organic dust-induced lung inflammation. (cdc.gov)
  • CL-316,243, a specific β3AR agonist, was administered to the triple transgenic mouse model of AD (3xTg-AD) and non-transgenic controls from 15 to 16 months of age at a dose of 1 mg/kg/day i.p. (nih.gov)
  • The maximum daily recommended dose is 1 g of gel in total weight, which corresponds to approximately five pea sized amounts. (pillintrip.com)
  • Labetalol HCl produces dose-related falls in blood pressure without reflex tachycardia and without significant reduction in heart rate, presumably through a mixture of its alpha- and beta-blocking effects. (nih.gov)
  • Due to the alpha 1 -receptor blocking activity of labetalol HCl, blood pressure is lowered more in the standing than in the supine position, and symptoms of postural hypotension (2%), including rare instances of syncope, can occur. (nih.gov)

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