Wakefulness-Promoting Agents: A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Serotonin 5-HT1 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.GABA Agonists: Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).GABA-A Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.GABA-B Receptor Agonists: Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Cannabinoid Receptor Agonists: Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.Serotonin 5-HT4 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Receptors, Adrenergic, alpha: One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.alpha 1-Antitrypsin: Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Nicotinic Agonists: Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine: A selective D1 dopamine receptor agonist used primarily as a research tool.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Hypoxia-Inducible Factor 1, alpha Subunit: Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Quinpirole: A dopamine D2/D3 receptor agonist.Baclofen: A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Excitatory Amino Acid Agonists: Drugs that bind to and activate excitatory amino acid receptors.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Benzazepines: Compounds with BENZENE fused to AZEPINES.8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.Piperidines: A family of hexahydropyridines.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.alpha7 Nicotinic Acetylcholine Receptor: A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.Receptors, Adrenergic, alpha-1: A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)PyrrolidinesReceptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Receptors, Nicotinic: One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.Naphthalenes: Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.Mice, Inbred C57BLCalcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Cholinergic Agonists: Drugs that bind to and activate cholinergic receptors.
(1/319) Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors.

The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors.  (+info)

(2/319) Role of potassium channels in the antinociception induced by agonists of alpha2-adrenoceptors.

1. The effect of the administration of pertussis toxin (PTX) as well as modulators of different subtypes of K+ channels on the antinociception induced by clonidine and guanabenz was evaluated in the mouse hot plate test. 2. Pretreatment with pertussis toxin (0.25 microg per mouse i.c.v.) 7 days before the hot-plate test, prevented the antinociception induced by both clonidine (0.08-0.2 mg kg(-1), s.c.) and guanabenz (0.1-0.5 mg kg(-1), s.c.). 3. The administration of the K(ATP) channel openers minoxidil (10 microg per mouse, i.c.v.), pinacidil (25 microg per mouse, i.c.v.) and diazoxide (100 mg kg(-1), p.o.) potentiated the antinociception produced by clonidine and guanabenz whereas the K(ATP) channel blocker gliquidone (6 microg per mouse, i.c.v.) prevented the alpha2 adrenoceptor agonist-induced analgesia. 4. Pretreatment with an antisense oligonucleotide (aODN) to mKv1.1, a voltage-gated K+ channel, at the dose of 2.0 nmol per single i.c.v. injection, prevented the antinociception induced by both clonidine and guanabenz in comparison with degenerate oligonucleotide (dODN)-treated mice. 5. The administration of the Ca2+-gated K+ channel blocker apamin (0.5-2.0 ng per mouse, i.c.v.) never modified clonidine and guanabenz analgesia. 6. At the highest effective doses, none of the drugs used modified animals' gross behaviour nor impaired motor coordination, as revealed by the rota-rod test. 7. The present data demonstrate that both K(ATP) and mKv1.1 K+ channels represent an important step in the transduction mechanism underlying central antinociception induced by activation of alpha2 adrenoceptors.  (+info)

(3/319) Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation.

The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory.  (+info)

(4/319) Cardiopulmonary effects of the alpha2-adrenoceptor agonists medetomidine and ST-91 in anesthetized sheep.

To test the hypothesis that pulmonary alterations are more important than hemodynamic changes in alpha2-agonist-induced hypoxemia in ruminants, the cardiopulmonary effects of incremental doses of (4-[1-(2,3-dimethylphenyl)ethyl]-1H-imadazole) hydrochloride (medetomidine; 0.5, 1.0, 2.0, and 4 micrograms/kg) and 2-(2, 6-diethylphenylamino)-2-imidazol (ST-91; 1.5, 3.0, 6.0, and 12 micrograms/kg) were compared in five halothane-anesthetized, ventilated sheep using a placebo-controlled randomized crossover design. Pulmonary resistance (RL), dynamic compliance, and tidal volume changes in transpulmonary pressure (DeltaPpl) were determined by pneumotachography, whereas cardiac index (CI), mean pulmonary artery pressure (Ppa), and pulmonary artery wedge pressure (Ppaw) were determined using thermodilution and a Swan-Ganz catheter. The most important finding was the fall in partial pressure of oxygen in arterial blood (PaO2) after administration of medetomidine at a dose (0.5 micrograms/kg) 20 times less than the sedative dose. The PaO2 levels decreased to 214 mm Hg as compared with 510 mm Hg in the placebo-treated group. This decrease in PaO2 was associated with a decrease in dynamic compliance and an increase in RL, DeltaPpl, and the intrapulmonary shunt fraction without changes in heart rate, CI, mean arterial pressure, pulmonary vascular resistance, Ppa, or Ppaw. On the other hand, ST-91 only produced significant changes in PaO2 at the highest dose. After this dose of ST-91, the decrease in PaO2 was accompanied by a 50% decrease in CI and an increase in mean arterial pressure, Ppa, Ppaw, and the intrapulmonary shunt fraction without significant alterations of RL and DeltaPpl. The study suggests that the mechanism(s) by which medetomidine and ST-91 produce lower PaO2 are different and that drug-induced alterations in the pulmonary system are mainly responsible for the oxygen-lowering effect of medetomidine.  (+info)

(5/319) The alpha2A-adrenergic receptor discriminates between Gi heterotrimers of different betagamma subunit composition in Sf9 insect cell membranes.

In view of the expanding roles of the betagamma subunits of the G proteins in signaling, the possibility was raised that the rich diversity of betagamma subunit combinations might contribute to the specificity of signaling at the level of the receptor. To test this possibility, Sf9 cell membranes expressing the recombinant alpha2A-adrenergic receptor were used to assess the contribution of the betagamma subunit composition. Reconstituted coupling between the receptor and heterotrimeric Gi protein was assayed by high affinity, guanine nucleotide-sensitive binding of the alpha2-adrenergic agonist, [3H]UK-14,304. Supporting this hypothesis, the present study showed clear differences in the abilities of the various betagamma dimers, including those containing the beta3 subtype and the newly described gamma4, gamma10, and gamma11 subtypes, to promote interaction of the same alphai subunit with the alpha2A-adrenergic receptor.  (+info)

(6/319) Effect of strenuous, acute exercise on alpha2-adrenergic agonist-potentiated platelet activation.

Vigorous exercise transiently increases the risk of primary cardiac arrest. Strenuous, acute exercise can also increase the release of plasma epinephrine. Previous investigations have indicated that epinephrine can potentiate platelet activation by activating platelet alpha2-adrenoceptors. This study investigated how strenuous, acute exercise affects alpha2-adrenergic agonist-potentiated platelet activation by closely examining 15 sedentary men who exercised strenuously on a bicycle ergometer. Before and immediately after exercise, platelet adhesiveness on fibrinogen-coated surfaces, [Ca2+]i in platelets, the number and affinity of alpha2-adrenergic sites on the platelet surface, and plasma catecholamine levels were determined. The results of this study can be summarized as follows: (1) The affinity of alpha2-adrenergic receptors on platelets decreases while the maximal binding number significantly increases after strenuous exercise, thereby correlating with the rise in plasma catecholamine levels. (2) Basal, clonidine-treated, ADP-treated, and clonidine plus ADP-treated adhesiveness and [Ca2+]i in platelets increased after strenuous exercise. (3) Strenuous exercise is associated with higher percentages of ADP- and clonidine plus ADP-enhanced platelet adhesiveness and [Ca2+]i than at rest. (4) The synergistic effects of clonidine on ADP-enhanced platelet adhesiveness and [Ca2+]i after strenuous exercise are much greater than those at rest. Therefore, we conclude that strenuous, acute exercise enhances platelet activation, possibly by altering the performance of platelet alpha2-adrenergic receptors, facilitating the ability of ADP-activated fibrinogen receptors, and enhancing fibrinogen binding to platelet fibrinogen receptors.  (+info)

(7/319) Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors.

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters.  (+info)

(8/319) Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice.

alpha2-Adrenergic receptor (AR)-selective compounds produce antihypertensive and antinociceptive effects. Moxonidine alleviates hypertension in multiple species, including humans. This study demonstrates that intrathecally administered moxonidine produces antinociception in mice. Antinociception was detected via the (52.5 degrees C) tail-flick and Substance P (SP) nociceptive tests. Moxonidine was intrathecally administered to ICR, mixed C57BL/6 x 129/Sv [wild type (WT)], or C57BL/6 x 129/Sv mice with dysfunctional alpha2aARs (D79N-alpha2a). The alpha2AR-selective antagonist SK&F 86466 and the mixed I1/alpha2AR-selective antagonist efaroxan were tested for inhibition of moxonidine-induced antinociception. Moxonidine prolonged tail-flick latencies in ICR (ED50 = 0.5 nmol; 0. 3-0.7), WT (0.17 nmol; 0.09-0.32), and D79N-alpha2a (0.32 nmol; 0. 074-1.6) mice. Moxonidine inhibited SP-elicited behavior in ICR (0. 04 nmol; 0.03-0.07), WT (0.4 nmol; 0.3-0.5), and D79N-alpha2a (1.1 nmol; 0.7-1.7) mice. Clonidine produced antinociception in WT but not D79N-alpha2a mice. SK&F 86466 and efaroxan both antagonized moxonidine-induced inhibition of SP-elicited behavior in all mouse lines. SK&F 86466 antagonism of moxonidine-induced antinociception implicates the participation of alpha2ARs. The comparable moxonidine potency between D79N-alpha2a and WT mice suggests that receptors other than alpha2a mediate moxonidine-induced antinociception. Conversely, absence of clonidine efficacy in D79N-alpha2a mice implies that alpha2aAR activation enables clonidine-induced antinociception. When clinically administered, moxonidine induces fewer side effects relative to clonidine; moxonidine-induced antinociception appears to involve a different alpha2AR subtype than clonidine-induced antinociception. Therefore, moxonidine may prove to be an effective treatment for pain with an improved side effect profile.  (+info)

*  Alpha-1A adrenergic receptor
... a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype". J. Pharmacol. Exp. Ther. 274 (1): ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
*  Adenosine A2A receptor
This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices. The ... Makujina SR, Sabouni MH, Bhatia S, Douglas FL, Mustafa SJ (Oct 1992). "Vasodilatory effects of adenosine A2 receptor agonists ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
*  Methyldopa
... α-methylnorepinephrine is an agonist of presynaptic central nervous system α2 adrenergic receptors. Activation of these ... Methyldopa is in the alpha-2 adrenergic receptor agonist family of medication. It works by stimulating the brain to decrease ... with increased use of other safer and more tolerable agents such as alpha blockers, beta blockers, and calcium channel blockers ... This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. This effect ...
*  Attention deficit hyperactivity disorder
The DRD4 receptor is a G protein-coupled receptor that inhibits adenylyl cyclase. The DRD4-7R mutation results in a wide range ... Medications used include stimulants, atomoxetine, alpha-2 adrenergic receptor agonists, and sometimes antidepressants. In those ... The 7 repeat variant of dopamine receptor D4 (DRD4-7R) causes increased inhibitory effects induced by dopamine and is ... Conversely, methylphenidate, …showed poor efficacy at the TAAR1 receptor. In this respect it is worth noting that the ...
*  Adrenergic antagonist
This is because adrenergic stimulation by agonists, results in normal calcium channel regulation. If these adrenergic receptors ... The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. ...
*  Alpha-2 adrenergic receptor
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... also acts as a moderate affinity 5-HT1A receptor agonist, and low affinity CB1 receptor antagonist). Clonidine (also I1 agonist ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... Agonists (activators) of the α2-adrenergic receptor are frequently used in veterinary anaesthesia where they affect sedation, ...
*  Brimonidine/timolol
It is a combination of brimonidine (an α2 adrenergic agonist) and timolol (a β adrenergic blocker), in concentrations of 0.2% ... a non-selective beta-adrenergic receptor inhibitor. Elevated IOP is considered the only modifiable risk factor in the ... Combigan is composed of brimonidine, a selective alpha-2 adrenergic receptor agonist, and timolol, ... 21 (2): 14. 2008. PMID 18326089. Lee, AJ; McCluskey, P (2008). "Fixed combination of topical brimonidine 0.2% and timolol 0.5% ...
*  Olney's lesions
Drugs that work to suppress NAN include anticholinergics, benzodiazepines, barbiturates and agonists at the alpha-2 adrenergic ... In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are ... Jansen writes: Neuroscience portal NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J, Labruyere J, ... receptor in the brain, such as clonidine. Conversely, coadministration of NMDA-antagonists with alpha-2 adrenergic antagonists ...
*  Alpha-adrenergic agonist
... or alpha-adrenergic agonists) are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Alpha blocker Adrenergic agonist Beta-adrenergic agonist Declerck I, Himpens B, Droogmans G, Casteels R (September 1990). "The ... α Adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of ... MeSH list of agents 82000316 Adrenergic alpha-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH). ...
*  Guanabenz
... (pronounced GWAHN-a-benz, sold under the trade name Wytensin) is an alpha agonist of the alpha-2 adrenergic receptor ...
*  List of veterinary drugs
... α2-adrenergic agonist (used to temporarily sedate animals) yohimbine - used to reverse effects of xylazine, also called an " ... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists benazepril ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses carprofen - COX-2 ... Pure mu agonist/opioid analgesic used as a premedication moxifloxacin - Antibiotic used for the treatment of acute bacterial ...
*  TDIQ
It is thought these effects are mediated via a partial agonist action at Alpha-2 adrenergic receptors, and TDIQ has been ... 72 (1-2): 379-87. doi:10.1016/S0091-3057(01)00768-7. PMID 11900809. Young R (2007). "TDIQ (5,6,7,8-tetrahydro-1,3-dioxolo [4,5- ... 71 (1-2): 205-13. doi:10.1016/S0091-3057(01)00666-9. PMID 11812524. Glennon RA, Young R, Rangisetty JB (May 2002). "Further ... TDIQ (also known as 6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinoline or MDTHIQ) is a drug used in scientific research, which ...
*  Methamphetamine
... σ receptor antagonists ... prevent the development of behavioral sensitization to METH [17, 18]. ... σ Receptor agonists have ... Methamphetamine is also an agonist of the alpha-2 adrenergic receptors and sigma receptors with a greater affinity for σ1 than ... An extremely large overdose may produce symptoms such as adrenergic storm, methamphetamine psychosis, substantially reduced or ... NMDA receptors are voltage-dependent ligand-gated ion channels that requires simultaneous binding of glutamate and a co-agonist ...
*  Yohimbine
It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a partial agonist ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine blocks the pre- and post-synaptic α2 receptors. Blockade of post-synaptic α2 receptors causes only minor corpus ...
*  Alpha-2A adrenergic receptor
... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... ADRA2A adrenergic, alpha-2A-, receptor". "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union ...
*  Alpha-1 adrenergic receptor
"Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... Adrenergic receptor Graham, Robert (May 1, 1996). "α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling ...
*  Beta-2 adrenergic receptor
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 ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...
*  Repinotan
... has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP- ... 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 ...
*  Major depressive disorder
... responses of depressive symptoms to dopamine receptor agonists, decreased dopamine receptor D1 binding in the striatum, and ... Third, decreased size of the locus coeruleus, decreased activity of tyrosine hydroxylase, increased density of alpha-2 ... adrenergic receptor, and evidence from rat models suggest decreased adrenergic neurotransmission in depression. Furthermore, ... Secondly, the correlation between depression risk and polymorphisms in the 5-HTTLPR gene, which codes for serotonin receptors, ...
*  Primary polydipsia
Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... 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 ...
*  RDS-127
It acts as a D2-like receptor agonist and also has some serotonin and adrenergic agonist effects, as well as some ... Rezaki YE, Ilhan M (1991). "Evaluation of alpha-adrenoceptor agonistic activity of RDS-127 (2-di-n-propylamino-4,7- ... "The antimuscarinic activity of a dopamine receptor agonist (RDS-127) differentiates M2-muscarinic receptors of heart, ileum and ... Sahin I, Tuncer M, Ilhan M (March 1990). "Dopamine receptor agonists, N,N-dipropyl-2-aminotetralin (TL-68) and 2-di-n- ...
*  Index of biochemistry articles
... alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - alpha-MSH - Ames test - amide - amine - amino - amino ... beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta-thromboglobulin - ...
*  Alpha-2B adrenergic receptor
Agonists (−)-Dibromophakellin Antagonists Imiloxan Yohimbine Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000274286 - ... 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- ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...
*  Alpha-2 blocker
α2-blockers are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly ... Increases the noradrenaline release due to blockade of alpha-2 receptors. Historically, yohimbine was used as an aphrodisiac, ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ...
*  Beta-3 adrenergic receptor
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 ... The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men". The American Journal of ...
*  Cannabigerol
CBG has been found to act as a high affinity α2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and ... "Evidence that the plant cannabinoid cannabigerol is a highly potent alpha(2)-adrenoceptor agonist and moderately potent 5HT ... It also binds to the CB2 receptor as an antagonist. CBG does not trigger THC-like activity in mice, rats, gerbils and non-human ... that the plant cannabinoid cannabigerol is a highly potent α2-adrenoceptor agonist and moderately potent 5HT1A receptor ...
*  Vascular smooth muscle
The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... receptors. Under NE binding α 1 {\displaystyle \alpha _{1}} receptors cause vasoconstriction (i.e. contraction of the vascular ... Antagonists of α 1 {\displaystyle \alpha _{1}} receptors (doxazosin, prazosin) cause vasodilation (i.e. decrease in vascular ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ...
p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor.  p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor.
0/Adrenergic alpha-Agonists; 0/Iodine Radioisotopes; 0/Receptors, Adrenergic, alpha; 108294-53-7/4-iodoclonidine; 146-48-5/ ... 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 ... Thus, PIC behaves as a partial agonist in a human platelet aggregation assay. [125I]PIC binds to the alpha 2B-AR in NG-10815 ...
more infohttp://www.biomedsearch.com/nih/p-125Iiodoclonidine-partial-agonist-at/1974694.html
EP 2329849 A1 - Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or...  EP 2329849 A1 - Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or...
Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or Preventing An ...
more infohttps://www.lens.org/lens/patent/EP_2329849_A1/family
EP 2329849 A1 - Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or...  EP 2329849 A1 - Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or...
Combination Of Alpha-2 Adrenergic Receptor Agonist And Non-steroidal Anti-inflammatory Agent For Treating Or Preventing An ...
more infohttps://www.lens.org/lens/patent/EP_2329849_A1/collections
Access to Extended Release Guanfacine HCl for Subjects Who Participated in Studies SPD503-315 or SPD503-316 in Europe - Full...  Access to Extended Release Guanfacine HCl for Subjects Who Participated in Studies SPD503-315 or SPD503-316 in Europe - Full...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Subjects will be dosed orally once-daily in the AM at 1, 2, 3, 4, 5, 6, or 7 mg according to subjects weight and age ... This is an extension study that will allow participants access to Extended-release Guanfacine Hydrochloride (HCl) for up to 2 ... Final Assessment is the last valid assessment obtained after Baseline (Visit 2/Day 0) whilst on investigational product and ...
more infohttps://clinicaltrials.gov/show/NCT01500694
Clonidine to Treat Iatrogenic-induced Opioid Dependence in Infants - Full Text View - ClinicalTrials.gov  Clonidine to Treat Iatrogenic-induced Opioid Dependence in Infants - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... central alpha 2 agonist) to tapering doses of opioids was efficacious and safe in treating opioid dependence in infants who had ... Specific Aim 2. To determine the pharmacokinetics and pharmacodynamics of clonidine in this critically ill infant population. ... The hypothesis will be tested by addressing 2 specific aims that will determine: 1) the efficacy and safety of clonidine in ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01360450?term=infant+care&recr=Open&fund=0&rank=9
Safety and Efficacy of Brimonidine Intravitreal Implant in Patients With Geographic Atrophy Due to Age-related Macular...  Safety and Efficacy of Brimonidine Intravitreal Implant in Patients With Geographic Atrophy Due to Age-related Macular...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Stage 2: 400 µg brimonidine tartrate implant in the study eye and sham in the fellow eye on Day 1 and Month 6. ... Stage 2: 200 µg brimonidine tartrate implant in the study eye and sham in the fellow eye on Day 1 and Month 6. ... Stage 2 will begin after 1 month of safety has been evaluated for Stage 1. Stage 2 is a randomized, double-masked, dose- ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT00658619?term=BRIMONIDINE&
Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons.  Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons.
To test this hypothesis, we applied baclofen, a selective GABAB receptor agonist, also known to activate GIRK channels in many ... Adrenergic alpha-2 Receptor Agonists / pharmacology. Animals. Brain / pathology. Calcium / metabolism. Clonidine / pharmacology ... Regulation of adrenergic receptors could represent a homeostatic response to the continuous discharge by the hcrt/orx neurons ... 0/Adrenergic alpha-2 Receptor Agonists; 0/G Protein-Coupled Inwardly-Rectifying Potassium Channels; 0/Intracellular Signaling ...
more infohttp://www.biomedsearch.com/nih/Sleep-Deprivation-Regulates-2-Adrenergic/21347440.html
Antihypertensive  Antihypertensive
Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Endothelium receptor blockers[edit]. Bosentan belongs to a new class of drug and works by blocking endothelin receptors. It is ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ...
more infohttp://www.let.rug.nl/~gosse/termpedia2/termpedia.php?language=dutch_general&density=7&link_color=000000&termpedia_system=perl_db&url=http%3A%2F%2Fen.wikipedia.org%2Fwiki%2FAntihypertensive
Antihypertensive drug - Wikipedia  Antihypertensive drug - Wikipedia
Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Endothelium receptor blockersEdit. Bosentan belongs to a new class of drug and works by blocking the receptors of the hormone ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ...
more infohttps://en.m.wikipedia.org/wiki/Antihypertensive_drug
Intermittent Explosive Disorder disease: Malacards - Research Articles, Drugs, Genes, Clinical Trials  Intermittent Explosive Disorder disease: Malacards - Research Articles, Drugs, Genes, Clinical Trials
Adrenergic Agonists. Phase 4. 6. Adrenergic alpha-2 Receptor Agonists. Phase 4. ... Cholinergic Receptor Nicotinic Alpha 7 Subunit. 15.04. DISEASES inferred 14 GeneCards inferred via :. DISEASES inferred (show ... or (-)-N-Methyl-3-phenyl-3-((alpha,alpha,alpha-trifluoro-p-tolyl)oxy)propylamine ... N-Methyl-3-phenyl-3-((alpha,alpha,alpha-trifluoro-p-tolyl)oxy)propylamine ...
more infohttp://www.malacards.org/card/intermittent_explosive_disorder
Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital...  Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital...
... a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital-anesthetized rats ... Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to ... Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital- ... Pretreatment with the alpha 2-adrenoceptor antagonist rauwolscine (0.5 mg/kg, i.v.) blocked the bradycardia induced by ...
more infohttp://www.curehunter.com/public/pubmed9241327.do
Exam 3 Flashcards by Megan tunstill | Brainscape  Exam 3 Flashcards by Megan tunstill | Brainscape
B. Prevention of cardiac beta-1 adrenergic receptor activation. C. Blockade of aldosterone receptors. D.ALL OF THE ABOVE ... Combination anti-anginal therapy can include using beta-adrenergic receptor. antagonists with either nitrovasodilators or ... Propranolol (lnderal) is more selective for beta-1 adrenergic receptors than. is metoprolol (LoPressor). ... A. prevent ATI angiotensin receptors from being activated.. B. reduce the synthesis of angiotensin ll.. C. increase levels of ...
more infohttps://www.brainscape.com/flashcards/exam-3-2013142/packs/3595637
Adverse Cutaneous Drug Reactions to Cardiovascular Drugs | Esen Özkaya | Springer  Adverse Cutaneous Drug Reactions to Cardiovascular Drugs | Esen Özkaya | Springer
Beta Adrenergic Receptor Blockers (Class II Antiarrhythmics). Özkaya, Esen (et al.). Pages 111-121 ... Alpha-2 Adrenergic Receptor Agonists. Özkaya, Esen (et al.). Pages 93-97 ... Apart from the well-known angioedema/urticaria from ACE inhibitors, lichen planus / lichenoid reaction from beta adrenergic ...
more infohttps://www.springer.com/us/book/9781447165354?wt_mc=
Atelosteogenesis, Type Ii disease: Malacards - Research Articles, Drugs, Genes, Clinical Trials  Atelosteogenesis, Type Ii disease: Malacards - Research Articles, Drugs, Genes, Clinical Trials
Adrenergic alpha-Agonists. Phase 4. 8. Adrenergic alpha-2 Receptor Agonists. Phase 4. ... 2. SLC26A2 NM_000112.3(SLC26A2): c.1724delA (p.Lys575Serfs) deletion. Pathogenic. rs386833498 GRCh37. Chromosome 5, 149360880: ... Phase 2. GM-CSF. 3. Comparison of Gas Consumption From Two Different Anesthesia Machines. Completed. NCT02774031 Not Applicable ... 2. A novel mutation in the sulfate transporter gene SLC26A2 (DTDST) specific to the Finnish population causes de la Chapelle ...
more infohttps://www.malacards.org/card/atelosteogenesis_type_ii
CCAC - Canadian Council on Animal Care: Analgesia  CCAC - Canadian Council on Animal Care: Analgesia
The alpha2-adrenergic receptor agonists: the alpha2-adrenergic receptor agonists are available on prescription. Although there ... Alpha 2-Adrenergic Receptor Agonists. The alpha2-adrenergic receptor agonists have been used extensively in animals to ... The activity is either stimulation (agonist), partial stimulation (partial agonist) or blocking (antagonist) of the receptor. ... All of the commonly used opioid analgesics are µ receptor agonists or partial agonists. ...
more infohttps://www.ccac.ca/en/training/modules/animals-housed-in-vivaria-stream/analgesia.html
ChemIDplus - 33089-61-1 - QXAITBQSYVNQDR-ZIOPAAQOSA-N - Amitraz [USAN:USP:INN:BAN] - Similar structures search, synonyms,...  ChemIDplus - 33089-61-1 - QXAITBQSYVNQDR-ZIOPAAQOSA-N - Amitraz [USAN:USP:INN:BAN] - Similar structures search, synonyms,...
Adrenergic Agents. *. Adrenergic Agonists. *. Adrenergic alpha-2 Receptor Agonists. *. Adrenergic alpha-Agonists ... 2, Pg. 289, 1989.. rat. LDLo. intramuscular. 250mg/kg (250mg/kg). SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER ... 1S/C19H23N3/c1-14-6-8-18(16(3)10-14)20-12-22(5)13-21-19-9-7-15(2)11-17(19)4/h6-13H,1-5H3/b20-12+,21-13+. Download. ... Methanimidamide, N'-(2,4-dimethylphenyl)-N-(((2,4-dimethylphenyl)imino)methyl)-N-methyl- ...
more infohttps://chem.nlm.nih.gov/chemidplus/rn/33089-61-1
Articles worth reading! - 3 Fat Chicks on a Diet Weight Loss Community  Articles worth reading! - 3 Fat Chicks on a Diet Weight Loss Community
Usually articles on stubborn fat discuss breakthroughs in transdermal delivery systems, adrenergic agonists, alpha-2 receptors ... Plant forms (called alpha-linoleic acids or ALA) differ from the kinds you get in fatty fish (EPA and DHA). The plant forms ... Plants provide an omega-3, called ALA (alpha-linolenic acid). The body must convert it for use -- which some say means it takes ... Just 1 ounce of walnuts packs 2.5 grams of alpha-linoleic acid, an omega-3 fatty acid. This recipe comes from Fran McCullough's ...
more infohttps://www.3fatchicks.com/forum/weight-resistance-training/23901-articles-worth-reading.html
US Patent for Ocular therapy using alpha-2 adrenergic receptor compounds having enhanced anterior clearance rates Patent ...  US Patent for Ocular therapy using alpha-2 adrenergic receptor compounds having enhanced anterior clearance rates Patent ...
The alpha 2 adrenergic receptor agonist may have a vitreal half-life greater than about three hours. The present materials are ... The alpha 2 adrenergic receptor agonists can be provided in liquid-containing formulations and/or bioerodible and/or non- ... include a therapeutic component which includes an alpha 2 adrenergic receptor agonist that is cleared from the anterior segment ... In ocular therapies, alpha agonists (e.g., agonists of alpha adrenergic receptors) are used to reduce aqueous humor production ...
more infohttps://patents.justia.com/patent/7931909
Emergency Trauma Care: Current Topics And Controversies, Volume III (Trauma CME)  Emergency Trauma Care: Current Topics And Controversies, Volume III (Trauma CME)
Alpha-2 Adrenergic Receptor Agonists. * Gabapentinoids. * Nitrous Oxide. * Nonpharmacological Pain Management. * Time- and Cost ... Chapter 2: Utilizing Ultrasound in Trauma: As the number of applications of point-of-care ultrasound (POCUS) in the trauma ... Table 2. Orthopedic Injuries and Associated Potential Nerve Injuries. * Figure 1. Salter-Harris Classification of Fractures and ... Table 2. Ultrasound-Guided Regional Anesthesia in Trauma. * Table 3. Guidelines for Regional Anesthesia for Traumatic ...
more infohttps://www.ebmedicine.net/store.php?paction=showProduct&pid=551
  • This is an extension study that will allow participants access to Extended-release Guanfacine Hydrochloride (HCl) for up to 2 years. (clinicaltrials.gov)
  • Apart from the well-known angioedema/urticaria from ACE inhibitors, lichen planus / lichenoid reaction from beta adrenergic blockers and photosensitivity from thiazid diuretics, ACDR from CV drugs might be seen in a wide spectrum extending to rare but life-threatening conditions such as erythroderma, Stevens-Johnson syndrome, toxic epidermal necrolysis or drug hypersensitivity syndrome. (springer.com)
  • The aim of this study was to determine the relative contribution of central versus peripheral α 2 -adrenoceptors in mediating diuresis and natriuresis, as well as the role of α 2 -adrenoceptors in antagonizing the actions of AVP. (okstate.edu)
  • This inhibition results in reduced dopaminergic and adrenergic neurotransmission in the peripheral nervous system. (wikipedia.org)
  • Stage 2: 400 µg brimonidine tartrate implant in the study eye and sham in the fellow eye on Day 1 and Month 6. (clinicaltrials.gov)
  • What Brimonidine Tartrate/Timolol Eye Drops, Solution is and what it is used for 2. (drugs.com)
  • Brimonidine Tartrate/Timolol should not be used in children less than 2 years old and should not usually be used in children aged 2 to 17. (drugs.com)
  • 53 Atelosteogenesis type 2 is a genetic disorder that affects cartilage and bone development. (malacards.org)
  • It affects about 5-7% of children when diagnosed via the DSM-IV criteria and 1-2% when diagnosed via the ICD-10 criteria. (wikipedia.org)
  • An important gene associated with Intermittent Explosive Disorder is SLC6A4 (Solute Carrier Family 6 Member 4), and among its related pathways/superpathways are Peptide ligand-binding receptors and G alpha (s) signalling events . (malacards.org)
  • An important gene associated with Atelosteogenesis, Type Ii is SLC26A2 (Solute Carrier Family 26 Member 2). (malacards.org)
  • Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (springer.com)
  • Atelosteogenesis type 2 causes serious health problems and infants with this disorder are usually stillborn or die soon after birth from respiratory failure. (malacards.org)
  • The administration of propranolol was associated with significant reductions in fentanyl equivalents (65%, p = 0.009), midazolam equivalents (57%, p = 0.048), propofol (16%, p = 0.009), and haloperidol (44%, p = 0.024) on day 2 after starting propranolol compared with baseline. (frontiersin.org)
  • Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component which includes an alpha 2 adrenergic receptor agonist that is cleared from the anterior segment of an individual's eye to which the material is administered. (justia.com)
  • As we saw in the previous chapter, direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid bilayer. (springer.com)
  • 9-13 Movement of the hormone-occupied receptor is not required subsequent to dimerization, and consistent with this, activated receptors appear to be aggregated and essentially immobile at physiological temperature (see section E, chapter 4). (springer.com)
  • The signs and symptoms of atelosteogenesis type 2 include an opening in the roof of the mouth (a cleft palate), characteristic facial features, an inward- and upward-turning foot (clubfoot), and unusually positioned thumbs (hitchhiker thumbs). (malacards.org)
  • About 30-50% of people diagnosed in childhood continue to have symptoms into adulthood and between 2-5% of adults have the condition. (wikipedia.org)
  • Jans DA, Pavo I. A mechanistic role for polypeptide hormone receptor lateral mobility in signal transduction. (springer.com)
  • 25 Atelosteogenesis type 2 is a severe disorder of cartilage and bone development. (malacards.org)
  • 2) I think losing weight will solve other problems in my life. (3fatchicks.com)