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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In conclusion, physicians should be mindful of the possibility that α2-adrenoreceptor agonists might produce paradoxical pain in the same way that administration of opioid receptor agonists sometimes does. The clinical correlate of an increase in thermal sensitivity is not clear; however, tactile hypersensitivity (tactile allodynia) has been noted in patients with opioid-induced hyperalgesia. An α2-adrenoreceptor agonist-induced increase in pain sensitivity might worsen existing pains, cause new pains, or interfere with the analgesic effectiveness of α2-receptor agonists or other drugs used for pain treatment. These considerations might suggest that we should stop using α2-adrenoreceptor agonists for pain therapy. However, it would be unfortunate to prematurely discontinue this use of α2agonists, because our options for treating pain are limited and because opioid receptor agonists, the most important drugs used for the treatment of moderate-to-severe pain, produce a similar paradoxical ...
TY - JOUR. T1 - Gender differences in the effect of age on electrical field stimulation (EFS)-induced adrenergic vasoconstriction in rat mesenteric resistance arteries. AU - Sullivan, Jennifer C. AU - Davison, Cathy A.. PY - 2001/3/14. Y1 - 2001/3/14. N2 - The objective of this study was to examine the effects of gender and age on electrical field stimulation (EFS)-induced vasoconstriction. Fisher 344 rats were studied: young females (YF, n = 38), young males (YM, n = 29), old females (OF, n = 33), and old males (OM, n = 30). Isolated mesenteric resistance arteries (endothelium-intact or denuded) were pressurized, and outer diameter was monitored. Dose-response curves were performed to KCl and phenylephrine (PE). EFS (0.1-16 Hz) responses were expressed as percentage of constriction from baseline. Area under the curve (AUC) was calculated and comparisons were made using analysis of variance and t tests. Females became less responsive to EFS-induced constriction with age, whereas constrictor ...
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O:13:\PanistOpenUrl\:36:{s:10:\\u0000*\u0000openUrl\;N;s:6:\\u0000*\u0000idc\;N;s:6:\\u0000*\u0000fmt\;s:7:\journal\;s:6:\\u0000*\u0000doi\;s:0:\\;s:6:\\u0000*\u0000pii\;s:0:\\;s:7:\\u0000*\u0000pmid\;s:0:\\;s:9:\\u0000*\u0000atitle\;s:123:\COMPARISON OF THE EFFECTS OF METHOXAMINE WITH THOSE OF NORADRENALINE AND PHENYLEPHRINE ON SINGLE CEREBRAL CORTICAL NEURONES\;s:9:\\u0000*\u0000jtitle\;s:0:\\;s:9:\\u0000*\u0000stitle\;s:0:\\;s:7:\\u0000*\u0000date\;s:4:\1981\;s:9:\\u0000*\u0000volume\;s:0:\\;s:8:\\u0000*\u0000issue\;s:0:\\;s:8:\\u0000*\u0000spage\;s:0:\\;s:8:\\u0000*\u0000epage\;s:0:\\;s:8:\\u0000*\u0000pages\;s:0:\\;s:7:\\u0000*\u0000issn\;s:0:\\;s:8:\\u0000*\u0000eissn\;s:0:\\;s:9:\\u0000*\u0000aulast\;s:8:\BRADSHAW\;s:10:\\u0000*\u0000aufirst\;s:2:\CM\;s:9:\\u0000*\u0000auinit\;N;s:10:\\u0000*\u0000auinitm\;N;s:5:\\u0000*\u0000au\;a:4:{i:0;s:11:\BRADSHAW CM\;i:1;s:7:\PUN RYK\;i:2;s:9:\SLATER ...
J. S. Smith, D. J. Benefiel, P. N. Beaupre, Y. J. Sohn, F. W. Lurz, B. Byrd, A. Bouchard, N. B. Schiller, M. K. Cahalan, M. F. Roizen; EFFECT OF PHENYLEPHRINE ON MYOCARDIAL PERFORMANCE DURING CAROTID ENDARTERECTOMY. Anesthesiology 1984; 61:A56 doi: https://doi.org/10.1097/00000542-198409001-00056. Download citation file:. ...
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Indications for VAZCULEP (phenylephrine hydrochloride injection) refers to the medical reasons for why Vazculep is used and recommended as a treatment.
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TY - JOUR. T1 - α-1 Adrenergic receptors stimulation induces the proliferation of neural progenitor cells in vitro. AU - Hiramoto, Takeshi. AU - Ihara, Yoshiaki. AU - Watanabe, Yasuhiro. PY - 2006/11/6. Y1 - 2006/11/6. N2 - The proliferation of neural progenitor cells (NPCs) is regulated by classical neurotransmitters such as dopamine, serotonin and acetylcholine, via its own receptors. Previous studies have reported that the depletion of l-norepinephrine decreases the proliferation of NPCs in the adult rat hippocampus and it has been suggested that l-norepinephrine regulates the proliferation of NPCs. However, it remains unknown whether or not adrenergic receptors are involved in the increased proliferation of NPCs. In the present study, an MTT cell proliferation assay was carried out in order to investigate the roles played by adrenergic receptors in the proliferation of NPCs. We demonstrated that l-epinephrine enhanced the proliferation of embryonic NPCs in vitro. In addition, the α-1 ...
TY - JOUR. T1 - Cooling and α1- and α2-adrenergic responses in cutaneous veins. T2 - Role of receptor reserve. AU - Flavahan, Nicholas. AU - Lindblad, L. E.. AU - Verbeuren, T. J.. PY - 1985. Y1 - 1985. N2 - Experiments were designed to determine the effects of cooling on α1- and α2-adrenergic responses in isolated canine cutaneous veins. Rings of saphenous veins were suspended for isometric tension recording in physiological salt solution. Cooling (from 37 to 24°C) augmented contractions to norepinephrine under control conditions and after α1-adrenergic blockade (prazosin) but not following α2-adrenergic blockade (rauwolscine). Cooling augmented contractions evoked by the α2-adrenergic agonists B-HT 920 and UK 14304 but did not affect responses to the full α1-adrenergic agonist phenylephrine. These experiments suggest that cooling augments α2-adrenergic responsiveness without affecting α1-adrenergic responsiveness. However, the contractions evoked by the partial α1-adrenergic ...
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Aktivierte G-Protein gekoppelte Rezeptoren aktivieren heterotrimere GProteine, in dem sie den Austausch von GDP zu GTP am G-Protein katalysieren. Theoretische Untersuchungen mittels eines vereinfachten kinetischen Modells des Gi/o-Protein Zyklus legen nahe, dass nicht nur GDP-,sondern auch GTP-gebundene Gi/o-Proteine mit aktivierten α2A-adrenergen Rezeptoren (α2A-AR) interagieren können. Demgemäß sollten aktivierte Gi/o-Proteine mit aktivierten α2A-AR vermehrt interagieren, wenn mehr α2A-AR aktiviert werden als für eine maximale G-Protein Aktivierung nötig sind. Dies sollte zu einer paradoxen Deaktivierung von Gi/o-Proteinen und deren Effektorproteinen, z.B. dem G-Protein gekoppelten, einwärtsgleichrichtenden Kaliumkanal (GIRK-Kanal) führen. Mittels FRET lässt sich in lebenden und in permeabilisierten Zellen unter Kontrolle der intrazellulären Nukleotide die Aktivierung von α2A-AR, die Interaktion von Gi/o-Proteinen mit α2A-AR und die Aktivierung von Gi/o-Proteinen bestimmen. Die ...
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Phenylephrine or Neo-Synephrine is an α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure. Phenylephrine has recently been marketed as a substitute for pseudoephedrine but there are recent claims that oral phenylephrine may be no more effective as a decongestant than a placebo.
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Removal of endothelial cells on rings of rat aorta increased the sensitivity to the selective alpha-1 adrenoceptor agonist phenylephrine, to the nonselective alpha adrenoceptor agonist norepinephrine and to the selective alpha-2 adrenoceptor agonist clonidine. In the case of the first two, which are strong agonists for the alpha-1 adrenoceptor-mediating contraction, removal of endothelium increased sensitivity 4- and 6-fold at the EC30 level, but produced little or no increase in maximum. In the case of clonidine, a partial agonist for the alpha-1 adrenoceptor, which gave only about 15% of the maximum given by phenylephrine on endothelium-containing rings, removal of the endothelium not only shifted the curve to the left but also increased the maximum to about 50% of that given by phenylephrine. The depression of sensitivity to these agonists in rings with endothelium appeared to be due to the vasodepressor action of endothelium-derived relaxing factor (EDRF), as hemoglobin, a specific blocking ...
Phenylephrine test is one of the main factors determining the possibility of performing superior tarsal muscle resection. However, the influence of various factors on its result remains unexplored.Aim. To evaluate the effect of patient age, degree of ptosis, and levator muscle function on the result of the phenylephrine test.Patients and methods. 45 patients were examined (64 eyelids). The following examinations were performed for all patients: assessment of the degree of ptosis, levator muscle function and the phenylephrine test.Results. Age and the degree of ptosis do not affect the results of the phenylephrine test. Reduced levator muscle function leads to a decrease of the phenylephrine test results.Conclusion. The phenylephrine test remains an important criteria for patient selection for the planning superior tarsal muscle resection. Levator muscle function does affect the phenylephrine test result.
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alpha-2 adrenergic receptor agonist Decreases blood pressure and sympathetic nerve traffic. Clonidine,[12] Methyldopa[12] ... Alpha-2 adrenergic antagonist Increase blood pressure Yohimbine[111] Prognosis[edit]. POTS has a favorable prognosis when ... Especially elevations of adrenergic α1 receptor is associated with symptoms severity in patients with POTS.[55] ... Chen L, Du JB, Jin HF, Zhang QY, Li WZ, Wang L, Wang YL (September 2008). "[Effect of selective alpha1 receptor agonist in the ...
... alpha-2 and beta-2 adrenergic receptors,. The main endogenous agonist of these cell receptors is norepinephrine (NE). The ... See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... However, in clinical practice drugs applied intravenously that are agonists of alpha-2 receptors such as clonidine lead to ... adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ...
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... clonidine is an adrenergic agonist at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ... Alpha2-adrenergic receptor agonists, such as clonidine and guanfacine, act at noradrenergic autoreceptors to inhibit the firing ...
... exhibits agonist activity in vitro at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells ... It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ... It exhibits binding affinity against rat 5-hydroxytryptamine 2C receptors using [3H]mesulergine as a radioligand. As of October ... and 5-HT2A receptors in rats. It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat ...
Especially elevations of adrenergic α1 receptor is associated with symptoms severity in patients with POTS. If POTS is caused ... 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 ... April 1999). "Abnormal norepinephrine clearance and adrenergic receptor sensitivity in idiopathic orthostatic intolerance". ...
... is an adrenergic agonist used as a topical vasoconstrictor and hemostatic. Formerly, it was also used to prolong the ... It is the ketone form of epinephrine (adrenaline). Contrary to epinephrine, adrenalone mainly acts on alpha-1 adrenergic ... receptors, but has little affinity for beta receptors. The drug is largely obsolete, being superseded by other hemostatics such ... which is partly a consequence of the vasoconstriction caused by the drug via alpha-1 adrenergic receptors. In an (unspecified) ...
Day HE, Campeau S, Watson SJ, Akil H (July 1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA ... Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors, including α1A-, α1B-, and α1D- ... and syncope are associated with the body's poor ability to control blood pressure without active alpha-adrenergic receptors. ... "Functional α1-adrenergic receptors on leukocytes of patients with polyarticular juvenile rheumatoid arthritis". Journal of ...
... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - ... interferon receptor - interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - ...
Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP- ... Repinotan has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor ... Repinotan acts as a selective high-affinity full receptor agonist at the 5-HT1A receptor subtype. It increases the activity of ...
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 ...
Giovannitti JA, Thoms SM, Crawford JJ (2015). "Alpha-2 adrenergic receptor agonists: a review of current clinical applications ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... This is because adrenergic stimulation by agonists results in normal calcium channel regulation. If these adrenergic receptors ... Adrenergic receptor Alpha blocker Antagonist Beta blocker List of adrenergic drugs Propanolol Sympathetic nervous system ...
Giovannitti JA, Thoms SM, Crawford JJ (2015-03-01). "Alpha-2 adrenergic receptor agonists: a review of current clinical ... specifically at the 5-HT1A and 5-HT1B G-protein coupled receptors. Additionally, the effect of MDMA on alpha-2 receptors is ... Neurochemically, MDMA activates 5-hydroxytryptamine, or 5-HT serotonin receptors, ... 62 (1): 31-9. doi:10.2344/0003-3006-62.1.31. PMC 4389556. PMID 25849473. Lee N. "Weekly Dose: ecstasy, the party drug that ...
2001). "Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin". J. Biol. Chem. 276 (18): 15003-8. ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic ... "Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor". Roberts LR, Fish PV, Ian Storer R, Whitlock GA (April 2009). "6,7-Dihydro ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... Identification of a conserved aspartate residue involved in agonist binding and receptor activation". The Journal of Biological ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...
"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 veterinary anaesthesia where they affect sedation, ...
"Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ...
... 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 ...
... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... alpha-2A-, receptor". Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors ...
Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ... Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ...
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men". The American Journal of ...
... ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic receptors. ... SN-22, partial agonist at all three 5-HT2 subtypes. Peripherally selective agonistsEdit. One effect of 5-HT2A receptor ... G-protein coupled receptor activity. • virus receptor activity. • signal transducer activity. • drug binding. • G-protein alpha ... The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G ...
Labetalol - an alpha- and beta-adrenergic blocker, given as an intravenous bolus or infusion. Bolus followed by infusion. ... converting enzyme inhibitor or angiotensin II receptor blocker, which can interfere with renal autoregulation and produce acute ... Electroencephalographic examination detects the absence of alpha waves, signifying impaired consciousness. In people with ... 2 (6 Pt 1): 486-92. doi:10.1093/ajh/2.6.486. PMID 2757806. Tamaki K, Sadoshima S, Baumbach GL, Iadecola C, Reis DJ, Heistad DD ...
local anesthetics) Activators: Agonist: 4-chloro-m-cresol and suramin are direct agonists, i.e., direct activators. Xanthines ... Non-mammalian vertebrates typically express two RyR isoforms, referred to as RyR-alpha and RyR-beta. Many invertebrates, ... Ryanodine receptors are similar to the inositol trisphosphate (IP3) receptor, and stimulated to transport Ca2+ into the cytosol ... It has been shown that calcium release from a number of ryanodine receptors in a ryanodine receptor cluster results in a ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... Khan ZP, Ferguson CN, Jones RM (1999). "alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role". ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ...
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ...
... is a potent sedative drug which acts as a selective alpha-2 adrenergic agonist. It is closely related to dexmedetomidine ... and alpha 2-adrenergic receptors". Journal of Medicinal Chemistry. 37 (15): 2328-33. doi:10.1021/jm00041a011. PMID 7914537. ... Like other alpha-2 agonists, it produces sedative and muscle relaxant effects but without producing respiratory depression. It ... September 1997). "Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of ...
Agonists (−)-Dibromophakellin Antagonists Imiloxan Yohimbine Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000274286 - ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ...
... s must not be used in the treatment of selective alpha-adrenergic agonist overdose. The blockade of only beta ... Newer, third-generation beta blockers can cause vasodilation through blockade of alpha-adrenergic receptors.[69] ... are capable of exerting low-level agonist activity at the β-adrenergic receptor while simultaneously acting as a receptor site ... β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 ...
Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor-agonist ... Partial agonistsEdit. Partial agonists are defined as drugs that, at a given receptor, might differ in the amplitude of the ... Agonists and antagonists "compete" for the same binding site on the receptor. Once bound, an antagonist will block agonist ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine due to lack of alpha-2 receptor negative feedback and decreased fat accumulation due to epinephrine/ ...
腎上腺素受體激動藥 (α(英語:Alpha-adrenergic agonist) ... Glutamate receptor agonist(英語:Excitatory amino acid agonist) (AMPA(英語:Ampakine)) ... Acetylcholine receptor agonist(英語:Parasympathomimetic_drug) (Muscarinic(英語:Muscarinic agonist) ... Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor
Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ... although there is evidence that it may have some alpha-1 [7] and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... 1-59541-101-1. .. *^ a b Nichols AJ, Ruffolo RR, Brooks DP (June 1990). "The pharmacology of fenoldopam". Am. J. Hypertens. 3 ( ...
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-HT ... α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and dopamine D2, and as a partial agonist at 5-HT1A.[31][33][34][35] Yohimbine ... Yohimbine is an alpha-2 adrenergic antagonist, and has been used in a variety of research projects. It is a veterinary drug ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... Clortermine (Voranil) was developed by Ciba in the 1960s[1] and is an anorectic drug of the amphetamine class.[2] It is the 2- ... InChI=1S/C10H14ClN/c1-10(2,12)7-8-5-3-4-6-9(8)11/h3-6H,7,12H2,1-2H3 Y ...
... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". ... receptor". Naunyn-Schmiedeberg's Archives of Pharmacology. 357 (1): 17-24. PMID 9459568. doi:10.1007/PL00005133.. ...
σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... α2-Adrenergic. *Clonidine. *Detomidine. *Dexmedetomidine. * ...
Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH. gamolenic acid, gonadotropin release inhibitor ... antifungal, alkalinizing agents, quinolones, antibiotics, cholinergics, anticholinergics, antispasmodics, 5-alpha reductase ... inhaled and systemic corticosteroids, Beta2-adrenergic agonists, anticholinergics, Mast cell stabilizers. Leukotriene ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... It is most efficacious as a releaser of norepinephrine, with an ec50 of 109/41.4/5246nM for DA/NE/5HT, respectively .[1] It has ... N,alpha-Diethylphenylethylamine. *N-Ethylbuphedrone. *N-Ethylhexedrone. *N,N-Dimethylphenethylamine. *Naphthylamphetamine. * ...
Drugs such as bromocriptine interact with the dopaminergic receptor sites as agonists with selectivity for D2 receptors, making ... alpha-Ergosine *IUPAC name: Ergotaman-3',6',18-trione, 12'-hydroxy-2'-methyl-5'-(2-methylpropyl)-, (5'-alpha)- ... Drugs such as bromocriptine act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... Similarly, ergoline alkaloids have been shown to exhibit both 5-HT agonist and antagonist behaviors for multiple receptors, ...
5-Alpha-reductase inhibitor. *Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... Conversely not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs that ... PPAR agonist), mode of action (reducing blood triglycerides), and are used to prevent and to treat the same disease ( ...
Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine.[37] Radioactivity is ... Thyroid hormone receptor modulators. Receptor. (ligands). THR. *Agonists: Dextrothyroxine. *DIMIT. *DITPA. *Eprotirome (KB-2115 ... 80 (1): 220-223. doi:10.1210/jc.80.1.220. PMID 7829615.. *^ a b c d e f g Greer, Monte A.; Goodman, Gay; Pleus, Richard C.; ... doi:10.1007/s00259-008-0883-1. PMID 18670773. S2CID 81465.. *^ Nuclear medicine in thyroid cancer management: a practical ...
For nocturnal symptoms, intranasal corticosteroids can be combined with nightly oxymetazoline, an adrenergic alpha-agonist, or ... Nasal steroids, antihistamines such as diphenhydramine, cromolyn sodium, leukotriene receptor antagonists such as montelukast, ... Other measures that may be used second line include: decongestants, cromolyn, leukotriene receptor antagonists, and ... 10 (1): 1-7. doi:10.1097/ACI.0b013e328334f5fb. PMID 20010094.. *^ a b c d Rondón, C; Fernandez, J; Canto, G; Blanca, M (2010). ...
... 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 ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ... This results in activation of α2 adrenergic receptors,[21] as discussed previously. ...
2,5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... InChI=1S/C11H17NO2/c1-8(12)7-9-5-4-6-10(13-2)11(9)14-3/h4-6,8H,7,12H2,1-3H3 Y ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... on adrenergic receptors.[83] It is most usually marketed as the hydrochloride or sulfate salt. ... adrenergic receptors), producing sympathomimetic effects. Some drugs, such as MDMA and derivatives may decrease regulatory ...
Guanfacine - Sympatholytic, α2-adrenergic receptor agonist.. *Prazosin - Sympatholytic, alpha blocker.. Comorbidity[edit]. GAD ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ... 10 (1): 125-62.. *^ a b c d e f Hoyer, Jürgen; van der Heiden, Colin; Portman, Michael E. (February 2011). "Psychotherapy for ... 19 (1): 211-4. doi:10.1017/S003329170001117X. PMID 2727208.. *^ a b c Etkin, Amit; Prater, Katherine E.; Schatzberg, Alan F.; ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... It is structurally similar to MDA, but without the methyl group at the alpha position. ... DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ... However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase ...
Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine). *Beta blockers (e.g., propranolol) ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... 240.387 g·mol−1 Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). ... InChI=1/C15H28O2/c1-10(2)8-15(16)17-14-9-12(5)6-7-13(14)11(3)4/h10-14H,6-9H2,1-5H3/t12-,13+,14-/m1/s1 ...
Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine is a nonselective agonist of all adrenergic ... Racemic adrenaline works by stimulation of the alpha adrenergic receptors in the airway, with resultant mucosal ... Epinephrine's binding to these receptors triggers a number of metabolic changes. Binding to α-adrenergic receptors inhibits ... Its actions vary by tissue type and tissue expression of adrenergic receptors. For example, high levels of epinephrine causes ...
Alpha-2 adrenergic receptor) (A, B, C) · β1 · β2 · β3 ... CJ-033,466(英语:CJ-033,466) - partial agonist. 拮抗劑[编辑]. * ... 腺苷酸(英语:Adenosine receptor) (A1, A2A, A2B, A3) · P2Y(英语:P2Y receptor) (1(英语:P2RY1), 2(英语:P2RY2), 4(英语:P2RY4), 5(英语:LPAR6), 6(英语: ... 乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺(英语:Dopamine receptor) (D1, D2, D3, D4, D5) · 组织胺(英语:Histamine receptor) (H1, H2, H3, H4) · 褪黑素( ... 卷曲受体 (1(英语:FZD1), 2(英语:FZD2), 3(英语:FZD3), 4(英语:FZD4), 5(英语:FZD5), 6(英语:FZD6), 7(英语:FZD7), 8
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 ... doi:10.1038/s41419-019-2015-1. PMC 6791888. PMID 31611560.. *^ a b c d e f g h i j k l m n o p q r s t u v w x y Dellinger RP, ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ...
Serotonin receptor agonists. *Serotonin-norepinephrine-dopamine releasing agents. *Substituted amphetamines. Hidden categories ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Adrenergic release blockers: Bethanidine. *Bretylium. * ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ...
It is an alpha-2 adrenergic agonist that causes sedation and does have some analgesic properties. It has minimal effect on ... Midazolam[5] is a benzodiazepine that acts by stimulating inhibitory GABA receptors. Effects are seen within 2-5 minutes, and ... Propofol[5] is a non-barbiturate derivative that is thought to act by stimulating inhibitory GABA receptors and blocking ... It is phencyclidine that acts by partially blocking the NMDA receptors in the brain. Effects occur within 30 seconds, and last ...
... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... Further support for the monoamine hypothesis came from monoamine depletion studies: Alpha-methyl-p-tyrosine (AMPT) is a ... Data from clinical studies have shown that DA agonists, such as bromocriptine, pramipexole and ropinirole, exhibit ... These include receptor desensitization, alterations in intracellular transduction cascades and gene expression, the induction ...
... alpha}2-Adrenergic Receptor Subtypes Archived 2011-03-05 at the Wayback Machine J. Pharmacol. Exp. Ther. 322: pp. 214-221 (July ... as alpha-agonists such as ephedrine constrict the internal urethral sphincter, mimicking the effects of sympathetic nervous ... of the adrenergic receptor system by increasing the activity of norepinephrine at the postsynaptic α and β receptors.[26] The ... on adrenergic receptors.[26][27] It is most usually marketed as the hydrochloride or sulfate salt. ...
Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with ... a GABA-B receptor agonist and antispasmodic medication, has been found to reduce cravings but without a significant benefit ... a GABA-A receptor agonist and "Z-hypnotic" medication, has shown some efficacy in treating insomnia due to cannabis withdrawal ... a serotonin 1A receptor (5-HT1A) agonist, has shown limited efficacy for treating anxiety in people with cannabis use disorder ...
Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts.. A Tosaki, N S Behjet, D T Engelman ... Alpha-1 adrenergic receptor agonist-induced preconditioning in isolated working rat hearts. ...
alpha-2 adrenergic receptor agonist Decreases blood pressure and sympathetic nerve traffic. Clonidine,[12] Methyldopa[12] ... Alpha-2 adrenergic antagonist Increase blood pressure Yohimbine[111] Prognosis[edit]. POTS has a favorable prognosis when ... Especially elevations of adrenergic α1 receptor is associated with symptoms severity in patients with POTS.[55] ... Chen L, Du JB, Jin HF, Zhang QY, Li WZ, Wang L, Wang YL (September 2008). "[Effect of selective alpha1 receptor agonist in the ...
Adrenergic alpha-1 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Time Frame: Days 1 to 3/4 through patient diary, and followup at days 3/4 an 10/11. ]. ... Time Frame: Assessed during treatment (day 1 to 3/4) by patient diary and questioned by investigator at 1st followup visit. ]. ... Improval of fever by reduction of axillary temperature to less than 38,1°C. [ Time Frame: Assessed by investigator at baseline ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ... Baseline values were calculated as the mean from 4 consecutive 24-hour periods in which a symptom score was ≥1, prior to ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... is a potent vasopressor characterized by both α adrenergic agonistic activity in addition to a weak β adrenergic agonistic ...
Adrenergic alpha-1 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Angiotensin Receptor Antagonists. Molecular Mechanisms of Pharmacological Action. Cardiotonic Agents. Mydriatics. Autonomic ... current treatment with clonidine, beta blockers, angiotensin-converting-enzyme (ACE) inhibitors, or angiotensin II receptor ... Subjects hand will be submerged in cold water (~0-1°C) up to the wrist for 1 minute. ...
Adrenergic alpha-Agonists * Adrenergic beta-Agonists * Enzyme Inhibitors * Receptors, Adrenergic, alpha-1 ... we examined the effects of adrenoceptor agonists on firing properties and the intracellular mechanism for alpha(1)-adrenoceptor ... Phenylephrine (100microM), an alpha(1)-adrenoceptor agonist, also increased firing rate, which was inhibited by 100microM ... In agreement with previous reports, bath application of 100microM isoproterenol, a beta-adrenoceptor agonist, increased firing ...
We observed earlier that central alpha-2 adrenoceptor stimulation in mice greatly augments parasympathetic tone. To test the ... 0/Adrenergic alpha-Agonists; 0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Cardiotonic Agents; 0/Receptors, ... Receptors, Adrenergic, alpha-2 / agonists*, physiology. Stroke Volume / drug effects. Sympathetic Nervous System / drug effects ... Adrenergic alpha-Agonists / pharmacology*. Adrenergic beta-Antagonists / pharmacology. Adult. Antihypertensive Agents / ...
Adrenergic Agonist Agent, Ophthalmic. *Nonsteroidal Anti-inflammatory Drug (NSAID), Ophthalmic. *Ophthalmic Agent, Mydriatic ... Phenylephrine: Alpha1-adrenergic receptor agonist; it causes dilation of the pupil by contracting the radial muscle of the iris ... Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1- ... Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. ...
Traditional Chinese remedy for asthma that is a non-selective adrenergic agonist ... Muscarinic receptor that is mostly active in airway smooth muscle contraction and mucus hyper-secretion ... 3 effects of alpha adrenergic stimulation 1. smooth muscle contraction. 2. vasoconstriction. 3. slight bronchoconstriction ... 1. NO-mediated relaxation of smooth muscle, vasodilation. 2. MLCK-mediated contraction capillary endothelium, making ...
An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor ... Alpha-adrenergic agonists are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary ... Adrenergic+alpha-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH) ... Retrieved from "https://www.wikidoc.org/index.php?title=Alpha-adrenergic_agonist&oldid=668150" ...
administering said subject an alpha adrenergic receptor agonist in an amount effective to enhance coronary perfusion with said ... and other alpha adrenergic receptor agonists. Epinephrine is currently preferred. Vasoconstrictors may be administered by any ... wherein said alpha adrenergic receptor agonist is selected from the group consisting of epinephrine, norepinephrine, ... wherein said administering step is carried out by including said alpha adrenergic receptor agonist in said protective solution ...
0/Adrenergic alpha-Agonists; 0/Iodine Radioisotopes; 0/Receptors, Adrenergic, alpha; 108294-53-7/4-iodoclonidine; 146-48-5/ ... 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] ... Adrenergic alpha-Agonists / pharmacokinetics*. Blood Platelets / metabolism*. Cell Membrane / metabolism. Chromatography, Thin ... 8267204 - Methylprednisolone increases sensitivity to beta-adrenergic agonists within 48 hours in.... 6147954 - Adrenergic ...
"Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ...
... alpha-2 and beta-2 adrenergic receptors,. The main endogenous agonist of these cell receptors is norepinephrine (NE). The ... See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... However, in clinical practice drugs applied intravenously that are agonists of alpha-2 receptors such as clonidine lead to ... adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ...
What is Alpha adrenergic receptor? Meaning of Alpha adrenergic receptor medical term. What does Alpha adrenergic receptor mean? ... Looking for online definition of Alpha adrenergic receptor in the Medical Dictionary? Alpha adrenergic receptor explanation ... 5%, an alpha adrenergic receptor agonist with a beta adrenergic receptor inhibitor, for the reduction of elevated intraocular ... adrenergic receptor. (redirected from Alpha adrenergic receptor) adrenergic receptor. Etymology: L, ad + ren, kidney; Gk, ergon ...
Muscle fructose 1,6-bisphosphatase (FBPase), a well-known regulatory enzyme of glyconeogenic pathway has recently been found ... Adrenergic alpha-Agonists / metabolism * Adrenergic beta-Agonists / metabolism * Adrenergic beta-Antagonists / metabolism ... The import is also stimulated by isoproterenol (a nonselective beta-adrenergic receptors agonist) and inhibited by metoprolol ( ... strongly suggesting that nucleo-cytoplasmic shuttling of FBPase is under the control of beta1-adrenergic receptor-dependent Gs ...
... for the antagonist WB4101 and agonists phenylephrine and methoxamine suggests that cDNA RA42 encodes the alpha 1A receptor ... Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human ... using the hamster alpha 1B-adrenergic receptor as a probe. The deduced amino acid sequence of clone RA42 encodes a protein of ... Northern blot analysis of various rat tissues also shows the distribution expected of the alpha 1A receptor subtype with ...
Akorns Phenylephrine Hydrochloride Ophthalmic Solution, USP, is an alpha-1 adrenergic receptor agonist indicated to dilate the ...
I have POTS and documented alpha-1 adrenergic receptor autoantibodies. ---------------- Hi all, Im new here, from Los Angeles ... DR Could alpha-1 agonists help me regain functionality? ... muscarinic and adrenergic receptor antibodies are emerging in ... I just got my Celltrend results and also only have the alpha 1 andregenic antibodies. @Jesse or anyone else, did you find any ... Could alpha-1 agonists help me regain functionality? I have POTS and documented alpha-1 adrenergic receptor autoantibodies. ...
... receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 ... an alpha-2 adrenergic receptor agonist. The alpha-2 adrenergic receptor agonist may be an agonist or agent that selectively ... In addition to the alpha-2 adrenergic receptor agonist or alpha-2 adrenergic receptor agonists included in the intraocular ... the alpha-2 adrenergic receptor agonist can be brimonidine tartrate. The alpha-2 adrenergic receptor agonist can be dispersed ...
Agonist. General Function. Epinephrine binding. Specific Function. Alpha-2 adrenergic receptors mediate the catecholamine- ... Creagh O, Torres H, Rodriguez N, Gatica SR: Alpha-2B adrenergic receptor mediated hemodynamic profile of etomidate. P R Health ... The rank order of potency for agonists of this receptor is clonidine.... Gene Name. ADRA2B. Uniprot ID. P18089. Uniprot Name. ... Gamma-amino butyric acid type A receptor mutations at beta2N265 alter etomidate efficacy while preserving basal and agonist- ...
... functionally couple to sensory cell receptors such as taste GPCRs (TRs) and olfactory GPCRs (ORs) in an overly promiscuous ... In a particular embodiment, the G.alpha..sub.q protein variants can be expressed in mammalian cell lines or Xenopus oocytes, ... The invention provides a series of G.alpha..sub.q protein variants that ... adrenergic receptor, G.alpha..sub.olf-coupled mouse I7 olfactory receptor, G.alpha..sub.i-coupled m2 muscarinic receptor, and ...
Adrenergic alpha-2 Receptor Agonists (20) • Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. MeSH ... Adrenergic alpha-Agonists (52) • Drugs that selectively bind to and activate alpha adrenergic receptors. MeSH ... Adrenergic alpha-2 Receptor Antagonists (5) • Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS. MeSH ... Adrenergic alpha-Antagonists (65) • Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the ...
Norepinephrine is a potent alpha-adrenergic agonist with minimal beta-adrenergic agonist effects. It can increase blood ... Phenylephrine exerts a pure alpha-receptor agonist effect, which results in potent vasoconstriction, albeit at the expense of ... 11, 60] Norepinephrine has predominant alpha-receptor agonist effects and results in potent peripheral arterial ... At lower doses, it has a much greater effect on beta receptors; at higher doses, it has more alpha-receptor effects and ...
Norepinephrine is a potent alpha-adrenergic agonist with minimal beta-adrenergic agonist effects. It can successfully increase ... adrenergic receptor agonist that is primarily used in anesthesia to increase blood pressure. Although the data are limited, ... adrenergic effects induce an increase in cardiac contractility and heart rate. At doses of about 10 µg/kg/min, alpha-adrenergic ... Doses range from 0.2-1.35 µg/kg/min; doses as high as 3.3 µg/kg/min have been used because alpha-receptor down-regulation may ...
Alpha Adrenergic Central Agonist Amiodarone Amiodarone Pulmonary Toxicity Amrinone Angiotensin 2 Receptor Blocking Agent ... Preparations: Pressor Infusions - Alpha adrenergic agents (primarily) * Preparations: Pressor Infusions - Beta adrenergic ... Preparations: Pressor Infusions - Alpha adrenergic agents (primarily) * Preparations: Pressor Infusions - Beta adrenergic ... Preparations: Pressor Infusions - Alpha adrenergic agents (primarily) * Norepinephrine *Indications. *Preferred first-line ...
Angiotensin 2 Receptor Blocking Agent * Alpha Adrenergic Central Agonist * Clonidine * Clonidine Overdose ... Preparations: Pressor Infusions - Alpha adrenergic agents (primarily). *Norepinephrine. *Indications. *Preferred first-line ... Preparations: Pressor Infusions - Beta adrenergic agents (primarily). *Dobutamine. *Receptor Activity. *Primarily Beta-1 ... Agents, Vasoconstrictor, Agents, Vasopressor, Agonists, Vasoactive, Vasoactive Agonists, Vasoconstrictor Agents, Vasopressor ...
Mg2+ extrusion following beta-adrenergic receptor stimulation, and role of cAMP 4.2 Is there a role for alpha-adrenergic ... T E Fagan, A Romani: Activation of a Na+- and a Ca2+-dependent Mg2+ extrusion mechanism by alpha- and beta-adrenergic agonists ... and beta2-adrenergic receptor stimulation. Circ Res 77, 973-983 (1995) 17. P B Molinoff: Alpha- and beta-adrenergic receptor ... Is there a role for alpha-adrenergic receptors in Mg2+ extrusion? The reports by Vormann and Gunther (12), Romani and Scarpa ( ...
Noradrenaline - agonist acting on all adrenergic receptors - alpha 1 an 2 and beta 1 an 2. But transmitters can also be ... Ach - agonist acts on all cholinergic receptors like nicotinic and muscarnic ... 2. Receptors that act and enzymes. 3. Receptors that regulate enzymes. 4. G protein coupled ... Determines how good a drug is at activating a receptor - drugs can partially activate receptors ...
  • Isolated rat hearts were perfused with .01, .1 or 1 mg/L of phenylephrine for 5 min followed by a 10-min washout period (preconditioning) before the induction of 30 min of normothermic global ischemia and 30 min of reperfusion. (aspetjournals.org)
  • Hearts preconditioned with increasing concentrations of phenylephrine (an alpha-1 adrenergic receptor agonist) produced a reduction in the incidence of reperfusion-induced ventricular fibrillation (VF) and ventricular tachycardia (VT). (aspetjournals.org)
  • Phenylephrine (100microM), an alpha(1)-adrenoceptor agonist, also increased firing rate, which was inhibited by 100microM prazosin, an alpha1-adrenoceptor antagonist. (nih.gov)
  • Following irrigation with diluted phenylephrine/ketorolac solution, plasma concentrations of phenylephrine were 1.2 to 1.4 ng/mL within 2 hours and plasma concentrations of ketorolac were 1 to 4.2 ng/mL within 8 hours. (drugs.com)
  • Prior to use, dilute 4 mL of phenylephrine 1%/ketorolac 0.3% solution in 500 mL of ophthalmic irrigation solution. (drugs.com)
  • Although complete selectivity between receptor agonism is rarely achieved, phenylephrine is an α 1 agonist, while clonidine and methyldopa are α 2 partial agonists [1] . (wikidoc.org)
  • 5. A method according to claim 1, wherein said alpha adrenergic receptor agonist is selected from the group consisting of epinephrine, norepinephrine, methoxamine, and phenylephrine. (freepatentsonline.com)
  • High affinity for the antagonist WB4101 and agonists phenylephrine and methoxamine suggests that cDNA RA42 encodes the alpha 1A receptor subtype. (nih.gov)
  • Akorn's Phenylephrine Hydrochloride Ophthalmic Solution, USP, is an alpha-1 adrenergic receptor agonist indicated to dilate the pupil. (cnbc.com)
  • Phenylephrine Hydrochloride Ophthalmic Solution, USP 2.5% and 10% is an alpha-1 adrenergic receptor agonist used for dilation of the pupil due to its vasoconstrictor and mydriatic action. (prweb.com)
  • Phenylephrine possesses predominantly α-adrenergic effects. (prweb.com)
  • A patient in the postanesthesia care unit (PACU) was prescribed 100 mcg of phenylephrine, an alpha-1 adrenergic receptor agonist, for acute hypotension. (lww.com)
  • 1 ) The drug was packaged in a 10 mL syringe labeled as "PHENYLephrine HCl 100 mcg/mL (1 mg/10 mL)" (see top photo at right). (lww.com)
  • Phenylephrine is an alpha-1 adrenergic receptor agonist used to treat hypotension,[L9416,L9410] dilate the pupil, and induce local vasoconstriction. (drugbank.ca)
  • Phenylephrine (PHE), a specific agonist of alpha 1-adrenergic receptors, provoked a significant rise of GH release. (kuleuven.be)
  • Fresenius Kabi Phenylephrine Hydrochloride Injection, USP is available as a 1 mL single dose vial and as 5 mL and 10 mL pharmacy bulk packages. (fresenius-kabi.com)
  • Phenylephrine Hydrochloride is an alpha-1 adrenergic receptor agonist indicated for increasing blood pressure in adults with clinically important hypotension resulting primarily from vasodilation, in such settings as septic shock or anesthesia. (fresenius-kabi.com)
  • Phenylephrine Hydrochloride Injection is an alpha-1 adrenergic receptor agonist indicated for treatment of clinically important hypotension resulting primarily from vasodilation in the setting of anesthesia. (fresenius-kabi.com)
  • phenylephrine decreases effects of iobenguane I 123 by receptor binding competition. (medscape.com)
  • The alpha 1- agonist phenylephrine (PE) (10-100 microM) evoked complex [Ca2+]i signals (22 of 26 slices, 90 of 90 cells in responding slices) composed of both a prolonged component (5.1 +/- 1.8 min), synchronized in neighboring cells, and multiple, mainly asynchronous [Ca2+]i spikes (25.0 +/- 11.6 sec). (jneurosci.org)
  • At 30°C the full agonists, adrenaline and phenylephrine, displaced 3 H-prazosin with a shallow inhibition curve. (springer.com)
  • Some agonists like adrenaline and phenylephrine seem to induce a temperature-dependent change in the conformation of the receptor which may represent a rapid form of desensitization. (springer.com)
  • Sagent Pharmaceuticals announced on March 11, 2021 that it is voluntarily recalling three lots of Phenylephrine Hydrochloride Injection, USP (10 mg/mL), an alpha-1 adrenergic receptor agonist for the treatment of low blood pressure resulting from the dilation of blood vessels, to the user level because of a customer complaint regarding potentially loose crimped vial overseals, which can result in a non-sterile product. (biopharminternational.com)
  • Each 1 ml ampoule contains 10 mg of the active ingredient phenylephrine hydrochloride. (mountainside-medical.com)
  • R)-(-)-Phenylephrine hydrochloride is a selective α 1 -adrenoceptor agonist with pK i s of 5.86, 4.87 and 4.70 for α 1D , α 1B and α 1A receptors respectively. (medchemexpress.com)
  • α 1 -adrenoceptor agonists such as phenylephrine increase the contractility of the heart. (medchemexpress.com)
  • Activation of mitogen-activated protein kinases (p38-MAPKs, SAPKs/JNKs and ERKs) by the G-protein-coupled receptor agonist phenylephrine in the perfused rat heart. (medchemexpress.com)
  • To demonstrate the effect of phenylephrine on alveolar fluid clearance, phenylephrine at different concentrations (10, 1, 0.1, 0.01, and 0.001 μM) is injected into the alveolar space of the HVT ventilated rats [5] . (medchemexpress.com)
  • Methods: The present prospective clinical study involved patients with involutional bilateral blepharoptosis who underwent two tests: 1) digital lifting of the more ptotic eyelid and observation of the effect on the contralateral eyelid and 2) instillation of two drops of 10% phenylephrine in the more ptotic eye and observation of the effect on the contralateral eyelid. (bvsalud.org)
  • Antagonists of alpha-1 receptors (doxazosin, prazosin) cause vasodilation (a decrease in vascular smooth muscle tone with increase of vessel diameter and decrease of the blood pressure). (wikipedia.org)
  • Certain medications, such as alpha-antagonists and ACE inhibitors, can exacerbate existing SUI. (uspharmacist.com)
  • Compared to other H2 receptor antagonists, famotidine displays high selectivity towards. (drugbank.ca)
  • The EPI-induced GH release could be totally blocked only by administration of both alpha- and beta-receptor antagonists. (kuleuven.be)
  • As a consequence, the binding of agonists, but not that of antagonists, is modulated by guanyl nucleotides. (aspetjournals.org)
  • This structure, followed by other co-crystals of β 2 AR ( Hanson and others 2008b ) and β 1 AR ( Warne and others 2008 ) with the antagonists (-)-timolol (PDB code 3D4S) and (-)-cyanopindolol (PDB code 2VT4) respectively, represents a leap forward in the understanding of the inactive state of adrenergic GPCRs. (pubmedcentralcanada.ca)
  • Antagonistic effects 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. (fresenius-kabi.com)
  • METHODS: Digital imaging and the Ca(2+)-reporting dye fura-2 were used to study the effects of agonists and their antagonists of Cai2+ in sheep lens primary cell cultures. (arvojournals.org)
  • More specifically, the epinephrine response was mediated by the alpha 1A adrenergic receptor subtype based on the greater potencies exhibited by the alpha 1A subtype selective competitive antagonists WB 4101 and 5-methylurapidil compared to the alpha 1B and alpha 1D selective antagonists spiperone and BMY 7378, respectively. (arvojournals.org)
  • But there are also adrenergic receptors in the brain, in the vasculature, in the liver, in the prostate (alpha 1 a adrenergic antagonists are in fact used to treat prostate hyperplasia). (scientificamerican.com)
  • For several partial agonists and antagonists (cirazoline, methoxamine, indanidine (Sgd 101-75), oxymetazoline and phentolamine) no such distinct temperature- and GTP-shifts could be demonstrated suggesting a different kind of interaction with al-binding sites. (springer.com)
  • Carlos G. Musso and Jose Alfie, "Resistant Hypertension in the Elderly-Second Line Treatments: Aldosterone Antagonists, Central Alpha-Agonist Agents, Alpha-Adrenergic Receptor Blockers, Direct Vasodilators, and Exogenous Nitric Oxide Donors", Cardiovascular & Hematological Agents in Medicinal Chemistry (2014) 12: 170. (eurekaselect.com)
  • Groups of anesthetized mice were pretreated with saline, the alpha(2)-agonist clonidine (1 mg/kg), and the alpha(2)-antagonists RX821002 (1 mg/kg) and yohimbine (1 mg/kg). (sigmaaldrich.com)
  • Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
  • To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptor in the central and peripheral nervous systems. (wikipedia.org)
  • The neurotransmitter norepinephrine has higher affinity for the α1 receptor than does the hormone epinephrine/adrenaline. (wikipedia.org)
  • In particular, norepinephrine decreases glutamatergic excitatory postsynaptic potentials by the activation of α1-adrenergic receptors. (wikipedia.org)
  • Norepinephrine also stimulates serotonin release by binding α1-adrenergic receptors located on serotonergic neurons in the raphe. (wikipedia.org)
  • The main endogenous agonist of these cell receptors is norepinephrine (NE). (wikipedia.org)
  • Myocardial β-ARs are studied extensively, and blocking β-ARs in heart failure (HF), when the AR agonist norepinephrine (NE) is elevated, is now a cornerstone of therapy. (pubmedcentralcanada.ca)
  • Agonistic effects with monoamine oxidase inhibitors (MAOI), β-adrenergic blocking agents, α-2-adrenergic agonists, steroids, tricyclic antidepressants, norepinephrine transport inhibitors, ergot alkaloids, centrally-acting sympatholytic agents and atropine sulfate. (fresenius-kabi.com)
  • Adrenergic receptors are receptors which bind the neurotransmitters epinephrine and norepinephrine. (scientificamerican.com)
  • The addition of optimal concentrations of oxotremorine-M, norepinephrine, endothelin-1, and ATP enhanced the release of inositol phosphates by 2-9-fold after activation of muscarinic, alpha 1-adrenergic, endothelin, and P2 nucleotide receptors, respectively. (aspetjournals.org)
  • This potentiation of inositol lipid hydrolysis resulted from an increased activity of the muscarinic receptor after the addition or norepinephrine and persisted after alpha 1-adrenergic receptor blockade. (aspetjournals.org)
  • In our study we have determined that UK-14304 (UK) and norepinephrine (NE), both alpha 2-adrenergic agonists, can augment LPS-stimulated TNF from elicited macrophages (MO). (jimmunol.org)
  • Adrenergic Fibers: Nerve fibers that synthesize and release norepinephrine. (cram.com)
  • Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α 1 -adrenergic receptor in the central and peripheral nervous systems . (gutenberg.org)
  • Adrenergic receptors (ARs) are members of the 7-transmembrane domain G-protein-coupled receptor superfamily that bind the endogenous catecholamines epinephrine and norepinephrine. (acris-antibodies.com)
  • The norepinephrine provided by the LC acts at the medial septal area (MSA) and the medial preoptic area (MPOA) to activate waking-active neurons ( via alpha-1 adrenergic receptors) and inhibit sleep-active neurons ( via alpha-2 adrenergic receptors). (frontiersin.org)
  • This receptor binds epinephrine and norepinephrine with approximately equal affinity. (uniprot.org)
  • At adrenergic neurons they play important role as auto inhibitory feedback mechanisms controlling norepinephrine release. (egpat.com)
  • Our results show that alpha-1 adrenergic stimulation (preconditioning) can prevent postischemic abnormalities in intracellular ions, reperfusion arrhythmias, and contractile function without the inhibition of O2 delivery. (aspetjournals.org)
  • We observed earlier that central alpha-2 adrenoceptor stimulation in mice greatly augments parasympathetic tone. (biomedsearch.com)
  • We conclude that alpha-2 adrenoceptor stimulation has a differential effect on baroreflex HR and vasomotor regulation. (biomedsearch.com)
  • alpha-2 Adrenoceptor stimulation greatly augments baroreflex-mediated bradycardia, most likely by parasympathetic activation. (biomedsearch.com)
  • a site in a sympathetic effector cell that reacts to adrenergic stimulation. (thefreedictionary.com)
  • In general, stimulation of alpha receptors is excitatory of the function of the host organ or tissue, and stimulation of the beta receptors is inhibitory. (thefreedictionary.com)
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
  • Alpha1-adrenergic stimulation of phosphatidylinositol-phosphatidic acid turnover in rat parotid cells. (aspetjournals.org)
  • These results indicate that the beta-blocker pindolol has vasodilatory properties owing to stimulation of vascular beta 2-adrenergic receptors and that this effect may be of therapeutic relevance. (ahajournals.org)
  • Stimulation of P2U purinergic or alpha 1A adrenergic receptors mobilizes Ca2+ in lens cells. (arvojournals.org)
  • These results support a primary role of NE release and alpha 1-adrenoceptor stimulation in neuron-astrocyte communication in the mature CNS. (jneurosci.org)
  • Chronic Alpha-1A adrenergic receptor stimulation increases lifespan and reduces the overall incidence of cancer in mice" Saturday, Nov 12, 2011, 55.10. (scientificamerican.com)
  • A somewhat more specialized view for the role of NE came to light when it was shown that NE and LC activation can modulate the response properties of sensory neurons following stimulation in a dose-dependent manner [1, 2, 57]. (thefreelibrary.com)
  • Stimulation of alpha-adrenergic receptor augments the production of macrophage-derived tumor necrosis factor. (jimmunol.org)
  • These data indicate (i) that the regions of the alpha 1AR that determine coupling to phosphatidylinositol metabolism are similar to those previously shown to be involved in coupling of beta 2AR to adenylate cyclase stimulation and (ii) that point mutations of a G-protein-coupled receptor can cause remarkable increases in sensitivity of biological response. (duke.edu)
  • Although β 2 AR stimulation in DC induces protein kinase A-dependent cAMP-responsive element-binding protein phosphorylation, the effect of changing the profile of cytokines produced upon LPS challenge occurs in a protein kinase A-independent manner and, rather, is associated with inhibition of the NF-κB and AP-1 signaling pathways. (jimmunol.org)
  • In terms of pharmacologic effects, clonidine works by stimulation of alpha-2 adrenergic receptors in the brain. (thefreedictionary.com)
  • 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
  • An in vitro and in vivo comparison of dopamine agonists. (aspetjournals.org)
  • PEA appears to exert a stimulatory effect in the brain through its effect on the beta-adrenergic and dopamine receptors, similar to antidepressants (7). (anabolicminds.com)
  • 3: The method of claim 1, wherein the agents comprise at least two of a Gi-coupled dopamine D2 receptor agonist, a Gs-coupled .beta.1 adrenergic receptor antagonist, or a Gq-coupled .alpha.1 adrenergic receptor blocker. (patents.com)
  • a dopamine receptor agonist sodium oxybate (Jazz), and a neuromuscular blocking agent botulinum toxin A (Allergan). (massagemag.com)
  • α2-adrenergic drugs modulate the binding of [18F]fallypride to dopamine D2/3 receptors in striatum of living mouse. (sigmaaldrich.com)
  • To test for alpha(2) adrenergic modulation of dopamine D(2/3) receptor availability in striatum of living mice using the high-affinity ligand [(18)F]fallypride and microPET. (sigmaaldrich.com)
  • α1-adrenergic receptor subtypes increase inhibition in the olfactory system, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors. (wikipedia.org)
  • There are three families of adrenergic receptors, alpha 1 , alpha 2 and beta, and each family contains three distinct subtypes. (thefreedictionary.com)
  • This study provides definitive evidence for the existence of three alpha 1-adrenergic receptor subtypes. (nih.gov)
  • Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. (aspetjournals.org)
  • 1 KO of the two main myocardial α1-AR subtypes, the α1A and α1B, impairs normal post-natal cardiac growth, and causes severe dilated cardiomyopathy and death after pressure overload. (pubmedcentralcanada.ca)
  • The alpha-AR -induced mydriasis in mice is mediated mainly by the alphaA-AR, with a smaller contribution of the alphaB-AR, matching the relative abundance of these subtypes at the mRNA level. (antikoerper-online.de)
  • It consists of three highly homologous subtypes, including α 1A - , α 1B - , and α 1D -adrenergic . (gutenberg.org)
  • Nine receptor subtypes have been identified thus far including three alpha-1 AR subtypes (1A/D, 1B, and 1C), three alpha-2 ARs (2A, 2B, and 2C), and three beta AR subtypes (1, 2, and 3). (acris-antibodies.com)
  • Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. (medchemexpress.com)
  • However, in clinical practice drugs applied intravenously that are agonists of alpha-2 receptors such as clonidine lead to powerful vasodilation, which causes a decrease in blood pressure by presynaptic activation of the receptors in the sympathetic ganglia. (wikipedia.org)
  • alpha 2 Agonist binding (p-amino-clonidine) declined in both hypothalamus and brain stem, and the fall was greater in hypertensive than in normotensive rats. (ahajournals.org)
  • The effectiveness of PHE but not clonidine, together with the high potency of the alpha 1-blocker prazosin suggest that the alpha-adrenergic receptor is predominantly of the alpha 1-subtype. (kuleuven.be)
  • The alpha 2-agonist clonidine (10- 100 microM) did not increase [Ca2+]i (n = 4 slices). (jneurosci.org)
  • Many investigators have used dexmedetomidine and clonidine (another alpha-2 agonist) to control agitation and delirium ( 7 - 15 ). (frontiersin.org)
  • In the present study, we examined the effects of adrenoceptor agonists on firing properties and the intracellular mechanism for alpha(1)-adrenoceptor-dependent modulation of firing in pyramidal neurons of rat cerebral cortex. (nih.gov)
  • In agreement with previous reports, bath application of 100microM isoproterenol, a beta-adrenoceptor agonist, increased firing frequency in response to a long intracellular depolarizing current injection. (nih.gov)
  • Beta receptors are divided into beta1, beta2, beta3, which are linked to Gs, and adenylate cyclase, increasing cAMP, which in turn drives cAMP-dependent protein kinase that mediates intracellular events. (thefreedictionary.com)
  • Heterotrimeric G proteins, consisting of alpha, beta and gamma subunits, couple ligand-bound seven transmembrane domain receptors (GPCRs or G-protein coupled receptors) to the regulation of effector proteins and production of intracellular secondmessengers such as cAMP, cGMP, and Ca.sup.2+. (patentgenius.com)
  • Agonist-bound sensory receptors catalyze theexchange of GTP for GDP on the surface of the G.alpha.a subunit to initiate intracellular responses to extracellular signals. (patentgenius.com)
  • What should the ligand be in order to bind to an intracellular receptor? (brainscape.com)
  • What do intracellular receptors often regulate? (brainscape.com)
  • G-protein-coupled adrenergic receptors activate phospholipase C, resulting in release of intracellular calcium, ultimately leading to smooth muscle vasoconstriction. (reviewofophthalmology.com)
  • The agonist-mediated Cai2+ increase was dependent on intracellular Ca2+ stores and was inhibited by the phospholipase C inhibitor U73122. (arvojournals.org)
  • ATP or epinephrine could desensitize the cells to either agonist because of both the depletion of intracellular Ca2+ stores and the downregulation of a common intermediate in the signal transduction pathway. (arvojournals.org)
  • CONCLUSIONS: Ca2+ is mobilized from intracellular stores in the sheep lens by ATP and epinephrine acting through P2U purinergic and the alpha 1A adrenergic receptors, respectively. (arvojournals.org)
  • alpha 1-mediated [Ca2+]i transients were observed after removal of extracellular [Ca2+]o (n = 8 of 9 slices), indicating PE-induced Ca2+ release from intracellular stores. (jneurosci.org)
  • Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. (acris-antibodies.com)
  • Analysis of the ligand binding properties of RA42 expressed in COS-7 cells with a variety of adrenergic ligands demonstrates a unique alpha 1-adrenergic receptor pharmacology. (nih.gov)
  • (Department of Pharmacology and Toxicology, University of Lausanne, Switzerland) Working with Professor Kaethi Geering and Dr Stephanie Bibert to identify the candidate cysteine residue on the beta 1 subunit of Na+-K+ pump subunit that mediates its oxidative regulation. (edu.au)
  • This presynaptic effect is predominant and completely overrides the vasoconstrictive effect of the alpha-2 receptors in the vascular smooth muscle. (wikipedia.org)
  • The down regulation of alpha 2-adrenergic receptors and the up regulation of alpha 1-adrenergic receptors are compatible with increased alpha 2-adrenergic agonist presynaptic inhibition of catecholamine release with resultant postsynaptic alpha 1-adrenergic receptor supersensitivity. (ahajournals.org)
  • Gabapentin And Magnesium Cleocin Gel, [, Meana JJ, Barturen F, Garro MA, Garcia-Sevilla JA, Fontan A, Zarranz JJ: Decreased density of presynaptic alpha 2-adrenoceptors in postmortem brains of patients with Alzheimer's disease. (swan.ac.uk)
  • At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. (wikipedia.org)
  • Northern blot analysis of various rat tissues also shows the distribution expected of the alpha 1A receptor subtype with abundant expression in vas deferens followed by hippocampus, cerebral cortex, aorta, brainstem, heart and spleen. (nih.gov)
  • The second alpha 1-adrenergic receptor cloned represents the rat homolog of the hamster alpha 1B subtype. (nih.gov)
  • Subtype alpha-1 adrenergic receptors consist of Alpha-1A adrenergic receptor , Alpha-1B adrenergic receptor and Alpha-1D adrenergic receptor . (bio-rad.com)
  • Further, receptor models incorporating a flexible TM-V backbone allow reliable prediction of binding affinities for a set of diverse ligands, suggesting potential utility of this approach to design of effective and subtype-specific agonists for adrenergic receptors. (pubmedcentralcanada.ca)
  • Like the nicotinic receptor, the muscarinic receptor is a subtype of acetylcholine (Ach) receptor which is activated by the neurotransmitter Acetylcholine (Ach. (anabolicminds.com)
  • In the mouse bleomycin model of right ventricular failure, the alpha1A -adrenergic receptor subtype agonist A61603 prevents right ventricular failure. (antikoerper-online.de)
  • Dexmedetomidine is a potent alpha-2 adrenergic agonist that binds to the alpha-2 adrenergic receptor subtype A at the LC, resulting in almost complete inhibition of the LC, which has a sedative effect ( 5 , 6 ). (frontiersin.org)
  • The import is also stimulated by isoproterenol (a nonselective beta-adrenergic receptors agonist) and inhibited by metoprolol (a selective beta1 antagonist), strongly suggesting that nucleo-cytoplasmic shuttling of FBPase is under the control of beta1-adrenergic receptor-dependent Gs protein signaling cascade. (nih.gov)
  • 4. The method of claim 1 , wherein the at least one alpha-adrenergic receptor agonist is an agonist selective for an alpha 1-adrenergic receptor. (google.co.uk)
  • 19 Recently, we found that modest augmentation of cardiac α1A signaling with a subpressor dose of an α1A-selective agonist can prevent doxorubicin-induced cardiomyopathy in mice. (pubmedcentralcanada.ca)
  • SYMJEPI contains epinephrine, a non-selective alpha and beta-adrenergic receptor agonist, indicated in the emergency treatment of allergic reactions (Type I) including anaphylaxis. (nih.gov)
  • The epinephrine response was mediated by alpha 1 adrenergic receptors based on the greater potency of the alpha 1 adrenergic selective antagonist prazosin compared to that of the alpha 2 adrenergic selective antagonist yohimbine. (arvojournals.org)
  • Propranolol, a non-selective beta-adrenergic antagonist with good penetration of the blood-brain barrier, has not been investigated for this purpose. (frontiersin.org)
  • Propranolol is a non-selective beta-adrenergic antagonist that has good penetration of the blood-brain barrier ( 21 ). (frontiersin.org)
  • In the present paper we show that, in HL-1 cardiomyocyte cell line, the activity of adenylyl cyclase and cAMP-dependent protein kinase A is essential to nuclear import of FBPase. (nih.gov)
  • Beta receptors are coupled to Gs proteins, which in turn are linked to adenylyl cyclase. (acris-antibodies.com)
  • α 2 adrenergic receptors are again G-protein coupled receptors coupled with inactivation of adenylyl cyclase. (egpat.com)
  • In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. (wikipedia.org)
  • In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more resistant to inhibition, and attenuation of α1-adrenergic-receptor-mediated vasoconstriction only occurs during heavy exercise. (wikipedia.org)
  • Resting muscle will not have its α1-adrenergic receptors blocked, and hence the overall effect will be α1-adrenergic-mediated vasoconstriction. (wikipedia.org)
  • Under NE binding alpha-1 receptors cause vasoconstriction ( contraction of the vascular smooth muscle cells decreasing the diameter of the vessels). (wikipedia.org)
  • Agonists of alpha-2 receptors in the vascular smooth muscle lead to vasoconstriction. (wikipedia.org)
  • Alpha receptor effects Vasoconstriction, reduced GI tract motility. (thefreedictionary.com)
  • No significant influence of pindolol was found on the vasoconstriction induced by the alpha 1-adrenergic receptor agonist methoxamine, the alpha 2-adrenergic receptor agonist BHT-933, or angiotensin II. (ahajournals.org)
  • The imidazoles can be α 2 -AR agonists (e.g., brimonidine), or mixed α 1 -AR/α 2 -AR agonists (e.g., naphazoline), and act post-synaptically on sympathetic nerves to cause vasoconstriction. (reviewofophthalmology.com)
  • Adrenergic-mediated vasoconstriction is associated with unwanted pharmacological and clinical phenomena, such as tachyphylaxis, tolerance, rebound vasodilation, toxicity and the potential for abuse. (reviewofophthalmology.com)
  • Xylometazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion. (hmdb.ca)
  • alpha 1-Adrenergic receptor binding (prazosin) was increased, again more in hypertensive than in normotensive rats. (ahajournals.org)
  • The stimulatory effect of EPI and PHE was lowered, respectively blocked, by low concentrations of the potent alpha 1-adrenergic antagonist prazosin. (kuleuven.be)
  • PE responses were completely blocked by the alpha 1-antagonist prazosin (200 nM, n = 4 slices), but not by the alpha 2- antagonist yohimbine (n = 3 slices). (jneurosci.org)
  • Binding of agonists to al-adrenoceptors labelled by 3 H-prazosin was investigated in membranes of rat myocardium and compared to the inotropic response elicited by α 1 -adrenoceptor activation on isolated right ventricles. (springer.com)
  • The therapies with the most evidence to support their use are Image Rehearsal Therapy (IRT) and the alpha-1-adrenergic receptor antagonist, prazosin. (allenpress.com)
  • We have now cloned two alpha 1-adrenergic receptors from a rat cerebral cortex cDNA library, using the hamster alpha 1B-adrenergic receptor as a probe. (nih.gov)
  • sub.q protein variants that functionally couple to sensory cell receptors such as taste GPCRs (TRs) and olfactory GPCRs (ORs) in an overly promiscuous manner. (patentgenius.com)
  • Although activation of beta-adrenoceptors increases firing frequency similarly to noradrenaline, it is still controversial whether alpha(1)-adrenoceptor activation influences repetitive firing. (nih.gov)
  • [1] The neurotransmitter noradrenaline has higher affinity for the α1 receptor than does adrenaline (which is a hormone). (gutenberg.org)
  • Alpha-2 adrenergic transmission and human baroreflex regulation. (biomedsearch.com)
  • Regulation of autonomic receptors in rat submandibular gland. (aspetjournals.org)
  • Apparent "down-regulation" of human platelet alpha 2-adrenergic receptors is due to retained agonist. (aspetjournals.org)
  • Regulation of adhesion of ICAM-1 by the cytoplasmic domain of LFA-1 integrin beta subunit. (semanticscholar.org)
  • A stimulatory role for cAMP in the regulation of receptor-activated phosphoinositide hydrolysis has been examined in human SK-N-MCIXC and SK-N-MCIIE neuroepithelioma cells. (aspetjournals.org)
  • Regulation of the postsynaptic alpha-adrenergic receptor in rat mesenteric artery. (meta.org)
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
  • Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • Pharmacological characterization of histamine receptors mediating the elevation of cyclic AMP. (aspetjournals.org)
  • Famotidine is a competitive histamine-2 (H2) receptor antagonist that works to inhibit gastric acid secretion. (drugbank.ca)
  • PIC had minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, but it potentiated platelet aggregation induced by ADP with an EC50 of 1.5 microM. (biomedsearch.com)
  • Characterization with agonist and antagonist radioligands and relationship to adenylate cyclase. (aspetjournals.org)
  • The CRF receptors belong to the 7-transmembrane domain receptor family that is coupled to adenylate cyclase via GTP-binding proteins (G proteins). (aspetjournals.org)
  • Contreras ML, Wolfe BB, Molinoff PB (1986a) Thermodynamic properties of agonist interactions with the beta-adrenergic receptor-coupled adenylate cyclase system. (springer.com)
  • Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (abcam.com)
  • Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (uniprot.org)
  • α1-AR gain-of-function in cardiac transgenic models generally supports the KO results, although phenotypes vary greatly with receptor level, promoter, and absence or presence of an activating mutation. (pubmedcentralcanada.ca)
  • On the other hand, constantly active alpha 1 b adrenergic receptor mice have rather opposite effects, with more cardiac issues, and an increase in neurodegeneration . (scientificamerican.com)
  • GTP transformed all binding sites into the low affinity form suggesting that at least some of the cardiac α 1 -adrenoceptors are coupled to N-proteins. (springer.com)
  • An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors . (wikidoc.org)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
  • We conclude 1) that, in SK-N-MCIXC cells, the addition of beta-adrenergic agonists selectively enhances muscarinic receptor-stimulated phosphoinositide hydrolysis through a cAMP-dependent process and 2) that the ability of exogenously added cAMP to enhance the activation of all four inositol lipid-linked receptors indicates that the effects of cAMP on inositol lipid hydrolysis are compartmentalized in these cells. (aspetjournals.org)
  • Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. (fpnotebook.com)
  • Guanfacine binds more selectively to the alpha 2A receptor. (psychdb.com)
  • 125I]PIC binds to the alpha 2B-AR in NG-10815 cell membranes with a Kd of 0.5 +/- 0.1 nM. (biomedsearch.com)
  • Etomidate binds at a distinct binding site associated with a Cl - ionopore at the GABA A receptor, increasing the duration of time for which the Cl - ionopore is open. (drugbank.ca)
  • Astressin binds with high affinity to the native cerebellar/brain stem receptor and relative potencies of selected CRF analogs determined with Ast* on the native receptor are similar to those obtained for the cloned CRF-R1. (aspetjournals.org)
  • The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. (wikipedia.org)
  • α1-Adrenergic receptors are members of the G protein-coupled receptor superfamily. (wikipedia.org)
  • The deduced amino acid sequence of clone RA42 encodes a protein of 560 amino acids whose putative topology is similar to that of the family of G-protein-coupled receptors. (nih.gov)
  • Functional Characterization of a Series of Mutant G Protein alpha q Subunits Displaying Promiscuous Receptopr Coupling Properties. (patentgenius.com)
  • G Protein Diversity: A Distinct Class of alpha Subunits isPresent in Vertibrates and Invertebrates. (patentgenius.com)
  • 1. A nucleic acid encoding a mutated Gq protein identical to the polypeptide contained in SEQ ID NO:1 or 37 except for the substitution of an aspartic acid residue for theglycine residue at position 66. (patentgenius.com)
  • 6. A nucleic acid encoding a mutated Gq protein which is identical to the polypeptide contained in SEQ ID NO:1 except for the replacement of the last 5 amino acid residues with the 5 amino acid residues of the carboxy terminus of Golf ortransducin. (patentgenius.com)
  • This invention relates to G.alpha.q protein variants and their use in the analysis and discovery of agonists and antagonsists of chemosensory receptors, such as G protein coupled receptors involved in sensing of tastants, olfactants, andpheromones. (patentgenius.com)
  • subunits also contribute to the specificity of receptor-G protein coupling (Xuet al. (patentgenius.com)
  • What happens when a G-protein receptor is couples to Phospholipase C? (brainscape.com)
  • Protein modeling to assess the pathogenicity of rare variants of SERPINA1 in patients suspected of having Alpha 1 Antitrypsin Deficiency. (alpha1.org)
  • Alpha-1B adrenergic receptor acts through G-protein beta/gamma of pertussis toxin-sensitive Alpha activating activity polypeptide O ( G-protein alpha-o ) [ 3 ], [ 5 ]. (bio-rad.com)
  • H-Ras then activates v-raf-1 murine leukemia viral oncogene homolog 1 ( c-Raf-1 ) / Mitogen-activated protein kinase kinases 1 and 2 ( MEK1(MAP2K1) and MEK2(MAP2K2) )/ Mitogen activated protein kinase 1 ( ERK2(MAPK1) ) [ 1 ], [ 10 ]. (bio-rad.com)
  • ERK2(MAPK1) activates Tuberous sclerosis 2 ( Tuberin ) [ 12 ]/ Ras homolog enriched in brain ( RHEB2 )/ FK506 binding protein 12-rapamycin associated protein 1 ( mTOR ) / Ribosomal protein S6 kinase 70kDa polypeptide 1 and 2 ( p70 S6 kinase1 and p70 S6 kinase2 )/ Eukaryotic elongation factor-2 kinase ( eEF2K )/ Eukaryotic translation elongation factor 2 ( eEF2 ). (bio-rad.com)
  • Receptors that are coupled to G proteins are characterized by agonist states of high and low affinity, which interconvert via GDP/GTP exchange on the G protein ( Conklin and Bourne, 1993 ). (aspetjournals.org)
  • The apparent affinity of an agonist depends on the degree of coupling of the receptor to the G protein, whereas the affinity of an antagonist is independent of such coupling. (aspetjournals.org)
  • They are members of the superfamily of G-protein coupled receptors, classified as α 1 -AR, α 2 -AR and β-AR, each with multiple and mixed sub-types. (reviewofophthalmology.com)
  • Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM, KD = 2.5 nM, Bmax = 160 fmol/mg protein) and competition studies indicated that [3H]rauwolscine labeled the alpha 2-receptor. (nih.gov)
  • Belongs to the G-protein coupled receptor 1 family. (abcam.com)
  • A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation. (patents.com)
  • Regions of the hamster alpha 1-adrenergic receptor (alpha 1 AR) that are important in GTP-binding protein (G protein)-mediated activation of phospholipase C were determined by studying the biological functions of mutant receptors constructed by recombinant DNA techniques. (duke.edu)
  • The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
  • Zusätzlich bieten wir Ihnen alpha 1 Adrenergic Receptor Antikörper (92) und alpha 1 Adrenergic Receptor Proteine (7) und viele weitere Produktgruppen zu diesem Protein an. (antikoerper-online.de)
  • A mutation of rs2322333, located in the intronic and 3' UTR (zeige UTS2R ELISA Kits ) part of the gene ADRA1A in chromosome 8, has a probability of being deleterious the abolition of ELAV-like protein 1 (ELAVL1 (zeige ELAVL1 ELISA Kits )) binding site rs2695260. (antikoerper-online.de)
  • The α 1 receptors at GI smooth muscle are again G-protein coupled receptors but not coupled with IP3/DAG instead coupled with opening of potassium channels leading to hyperpolarisation. (egpat.com)
  • The region of i loop 3 highlighted in blue is implicated in signalling from receptor to G protein. (els.net)
  • Marchese A, Chen C, Kim YM and Benovic JL (2003) The ins and outs of G‐protein‐coupled receptor trafficking. (els.net)
  • Tao J, Wang HY and Malbon CC (2003) Protein kinase A regulates AKAP250 (gravin) scaffold binding to the beta2‐adrenergic receptor. (els.net)
  • α1-receptors primarily mediate smooth muscle contraction, but have important functions elsewhere as well. (wikipedia.org)
  • During exercise, α1-adrenergic receptors in active muscles are attenuated in an exercise intensity-dependent manner, allowing the β2-adrenergic receptors which mediate vasodilation to dominate. (wikipedia.org)
  • The specific binding of Ast* to endogenous brain receptors is greater than that of Ucn*, resulting in more sites being detected by the antagonist than by the agonist. (aspetjournals.org)
  • Because it is a high-affinity, specific CRF antagonist, astressin is eminently suitable as a ligand for detection and characterization of both endogenous and cloned CRF receptors. (aspetjournals.org)
  • 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] bromoxidine (UK14,304), which represented approximately 40% of the sites bound by the antagonist [3H]yohimbine. (biomedsearch.com)
  • What is the affinity and efficacy of a full agonist? (brainscape.com)
  • The characteristics of a high-affinity antagonist radioligand are compared with those a high-affinity agonist in binding to the cloned corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2) and to the native receptors that exist in rat cerebellum and brain stem. (aspetjournals.org)
  • The 2.4 Å crystal structure of the β 2 -adrenergic receptor (β 2 AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. (pubmedcentralcanada.ca)
  • The data are compatible with the assumption that 32% of the binding sites were in a state of high affinity for the agonist adrenaline (K I 85 nmol/l) and 68% in a low affinity state (K I I738 nmol/l). (springer.com)
  • At 0°C most of the binding sites (86%) were in a state of high affinity for agonists (K I for adrenaline: 91 nmol/l). (springer.com)
  • When temperature was changed during incubation with adrenaline, a rise of temperature (from 0°C to 30°C) converted high affinity sites into the low affinity form, whereas a decrease in temperature (from 30°C to 0°C) failed to induce the high affinity state for agonists. (springer.com)
  • Our binding experiments suggest that myocardial α 1 -adrenoceptors can exist in states of different affinity for agonists. (springer.com)
  • Since no appreciable receptor reserve was detected it is hypothesized that the high affinity state which can be measured at 0°C under equilibrium conditions may be relevant to the initiation of the functional response. (springer.com)
  • These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes. (nih.gov)
  • PURPOSE: To identify agonists that elevate cytosolic Ca2+ (Cai2+) in lens cells and to characterize their mechanism of action. (arvojournals.org)
  • p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor. (biomedsearch.com)
  • Thus, PIC behaves as a partial agonist in a human platelet aggregation assay. (biomedsearch.com)
  • Tilting of TM-Ve towards the receptor axis provides a more complete description of polar receptor/ligand interactions for full and partial agonists, by enabling optimal engagement of agonists with two experimentally identified anchor sites, formed by Asp113/Asn312 and Ser203/Ser204/Ser207 side chains. (pubmedcentralcanada.ca)
  • Systematic differences in capacity of partial, full and inverse agonists to induce TM-V helix tilt in the β 2 AR model suggest potential role of TM-V as a conformational "rheostat" involved in the whole spectrum of β 2 AR responses to small molecule signals. (pubmedcentralcanada.ca)
  • Data are presented that indicate that Iso represents a novel type of alpha1A -AR partial agonist with signaling bias toward MAPK/ERK (zeige MAPK1 ELISA Kits ) signaling cascade that is likely independent of coupling to Galphaq (zeige GNAQ ELISA Kits ). (antikoerper-online.de)
  • Occupancy of al-adrenoceptor binding sites with adrenaline at O°C but not at 30°C rather closely paralleled the concentration-response curve for the α 1 -mediated increase in ontractile force. (springer.com)
  • Auf www.antikoerper-online.de finden Sie aktuell 44 Adrenoceptor alpha 1A (ADRA1A) ELISA Kits von 10 unterschiedlichen Herstellern. (antikoerper-online.de)
  • 1) Alpha receptors, which evoke an excitatory response of smooth muscle cells to catecholamines. (thefreedictionary.com)
  • 2) Beta receptors, which dampen the response to catecholamines. (thefreedictionary.com)
  • We have studied the effect of long-term (72 hour) intravenous infusions of methyldopa to awake restrained spontaneously hypertensive rats and normotensive Wistar-Kyoto control animals to look for differences in hypotensive effect, differences in concentrations of natural and alpha-methylated catecholamines, and differences in alpha 1 and alpha 2-adrenergic receptor populations. (ahajournals.org)
  • Pharmacological and molecular cloning studies have demonstrated heterogeneity of alpha 1-adrenergic receptors. (nih.gov)
  • Pharmacological, structural, and molecular cloning data indicate significant heterogeneity within this receptor family. (acris-antibodies.com)
  • Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). (wikipedia.org)
  • Incorporation of G alpha z-Specific Sequence at the Carboxyl Terminus Increases the Promiscuity of Galpha16 toward Gi-coupled Receptors. (patentgenius.com)
  • 1 The unique structure of the bladder allows for an increase in urine volume without significant increases in bladder pressure. (uspharmacist.com)
  • Found throughout the body, Ach is crucial for autonomic activation of the central nervous system and by binding to the muscarinic receptor, arecoline increases cholinergic activity (more acetylcholine) (2). (anabolicminds.com)
  • The metabotropic agonist t-ACPD (30 or 50 microM) did not increase astrocytic [Ca2+]i in hippocampal slices (0 of 5), while kainate (200 microM or 1 mM) induced brief (1-2 min) [Ca2+]i increases only rarely (2 of 8 applications in 6 slices). (jneurosci.org)
  • Mice with constantly active alpha 1 a adrenergic receptors are less anxious than normal mice, show less depressive-like activity in mouse depression tests , and showed increases in new neuron birth in the hippocampus . (scientificamerican.com)
  • Beta-2 adrenergic receptor activation also appears to be important in the MSA and MPOA, resulting in dose-dependent increases in time spent awake ( 4 ). (frontiersin.org)
  • Indeed, LC neurons are known to degenerate in both of these conditions [27, 29, 42, 56], potentially limiting forebrain nor-adrenergic facilitation of sensory perception. (thefreelibrary.com)
  • Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. (drugs.com)
  • Agonism of beta-2 receptors causes vasodilation and low blood pressure (i.e. the effect is opposite of the one resulting from activation of alpha-1 and alpha-2 receptors in the vascular smooth muscle cells). (wikipedia.org)
  • You said through cell trend - did you get tested for muscarinic receptor antibodies as well? (dinet.org)
  • Arecoline exerts its effects through the muscarinic receptor system. (anabolicminds.com)
  • The enhancement of muscarinic receptor-stimulated inositol phosphate release could be quantitatively mimicked by inclusion of the beta-adrenergic agonist isoproterenol (EC50 approximately 0.1 microM), but not by alpha 1- or alpha 2-adrenergic agonists. (aspetjournals.org)
  • 125I]PIC bound rapidly and reversibly to platelet membranes, with a first-order association rate constant (kon) at room temperature of 8.0 +/- 2.7 x 10(6) M-1 sec-1 and a dissociation rate constant (koff) of 2.0 +/- 0.8 x 10(-3) sec-1. (biomedsearch.com)
  • Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. (meta.org)
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • G-proteins also activate Phospholipase C beta 1 ( PLC-beta1 ) [ 6 ]. (bio-rad.com)
  • Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
  • While detailed knowledge of ligand-receptor interactions would be instrumental in design of new and improved clinical candidates, the insight into spatial structure of GPCR has been limited to ab initio models ( Goddard and Abrol 2007 ) or models based on rhodopsin crystal structure ( Palczewski and others 2000 ). (pubmedcentralcanada.ca)
  • It also induces contraction of the urinary bladder, although this effect is minor compared to the relaxing effect of β2-adrenergic receptors. (wikipedia.org)
  • Other effects on smooth muscle are contraction in: Ureter Uterus (when pregnant): this is minor compared to the relaxing effects of the β2 receptor, agonists of which - notably albuterol/salbutamol - were formerly[citation needed] used to inhibit premature labor. (wikipedia.org)
  • These regional and strain differences in the metabolism of alpha-methyldopa suggest that the production of methylnorepinephrine in brain stem nuclei is most correlated with the hypotensive action of methyldopa. (ahajournals.org)
  • Buxton IL, Brunton LL (1986) α-Adrenergic receptors on rat ventricular myocytes: Characteristics and linkage to CAMP metabolism. (springer.com)
  • A chimeric receptor consisting of the beta 2-adrenergic receptor (beta 2AR) into which the putative third cytoplasmic loop of the alpha 1AR had been placed activated phosphatidylinositol metabolism as effectively as the native alpha 1AR, as did a truncated alpha 1AR lacking the last 47 residues in its cytoplasmic tail. (duke.edu)
  • The present data show that the natural beta-agonist epinephrine (EPI) stimulates GH release through an additional alpha-adrenergic mechanism. (kuleuven.be)
  • The alpha adrenergic receptor system, which responds to the neurotransmitter adrenaline, is an important signaling mechanism in the body and is believed to be involved in such diverse therapeutic indications as cardiovascular disease, benign prostatic hyperplasia (BPH), pain and glaucoma. (thefreedictionary.com)
  • Here we show that while the carazolol pocket captured in the β 2 AR crystal structure accommodates (-)-isoproterenol and other agonists without steric clashes, a finite movement of the flexible extracellular part of TM-V helix (TM-Ve) obtained by receptor optimization in the presence of docked ligand can further improve the calculated binding affinities for agonist compounds. (pubmedcentralcanada.ca)
  • Local sub-type concentrations, distributions and ligand binding affinities all define a given tissue's response to adrenergic agonists. (reviewofophthalmology.com)
  • 1987) Ligand binding to the beta‐adrenergic receptor involves its rhodopsin‐like core. (els.net)
  • Vascular Alpha-1 Adrenergic Sensitivity is Enhanced in Chronic Kidney Disease. (alpha1.org)
  • Regions of the alpha 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function. (duke.edu)
  • The adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. (wikipedia.org)
  • α 1 -ARs are excitatory post-synaptic receptors, constricting larger arterioles. (reviewofophthalmology.com)
  • Xylometazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. (hmdb.ca)
  • Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. (drugs.com)
  • Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. (drugs.com)
  • Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. (drugs.com)
  • Most effector proteins interact with the G.alpha. (patentgenius.com)
  • These adrenergic receptors activate different Guanine nucleotide binding proteins (G-proteins). (bio-rad.com)
  • Right now the authors hypothesize that differences in these two receptors may be in the way they interactive with downstream proteins, in particular p21, a cell cycle regulator . (scientificamerican.com)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)