• Sumatriptan tablets contain sumatriptan (as the succinate), a selective 5-hydroxytryptamine 1 receptor subtype agonist. (nih.gov)
  • Synthesis and in vitro characterisation of N -[5-(4,5-dihydro-1 H -imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α 1A receptor agonist. (rndsystems.com)
  • A-61603, a potent α 1 -adrenergic receptor agonist, selective for the α 1A receptor subtype. (rndsystems.com)
  • The α1B mediates cardiac hypertrophy induced by non-selective α1-AR agonists like phenylephrine. (unc.edu)
  • We recently showed that an oral selective α1A agonist drug, dabuzalgron, preserves ATP content and mitochondrial function in mouse HF models. (unc.edu)
  • Scholars@Duke publication: Fetal terbutaline exposure causes selective postnatal increases in cerebellar alpha-adrenergic receptor binding. (duke.edu)
  • Despite the absence of body or brain growth impairment, selective increases were seen postnatally in cerebellar alpha 1- and alpha 2-receptor subtypes, whereas the same receptor populations were decreased by small amounts in cerebral cortex and midbrain + brainstem. (duke.edu)
  • A dosage regimen of lysergic acid diethylamide (LSD) that reliably produces behavioral tolerance in rats was evaluated for effects on neurotransmitter receptor binding in rat brain using a variety of radioligands selective for amine receptor subtypes. (erowid.org)
  • alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. (nih.gov)
  • 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds. (nih.gov)
  • Highly selective antagonists that do not affect the H1 receptors and may be administered contemporary to H1-receptor antagonists. (medscape.com)
  • Previously, descriptions of pharmacological effects associated with 'non-selective' β-adrenergic receptor agonists used to manage pulmonary diseases such as asthma or COPD necessarily include unwanted side effects often due to β 1 adrenergic receptor activation. (pharmacology2000.com)
  • Other medications, which are relatively selective for β 2 -adrenergic receptors, retain the benefits in management of asthma and COPD, while limiting adverse effects mediated by β 1 -adrenergic receptor activation. (pharmacology2000.com)
  • At higher doses β 2 -selective adrenergic agonists are still able to activate β 1 -receptors, again emphasizing the role of drug concentration in drug specificity. (pharmacology2000.com)
  • The premise of β 2 -agonist-mediated receptor activation (applying also to 'non-selective' β-receptor agonists) is based on both smooth muscle relaxation and reduced airway resistance. (pharmacology2000.com)
  • is a commonly used selective β 2 -adrenergic receptor agonist that may be administered either orally or by inhalation. (pharmacology2000.com)
  • When comparing the non-selective adrenergic agonist isoproterenol to albuterol, at doses that produce comparable bronchodilation, albuterol will exhibit substantially less cardiac stimulation. (pharmacology2000.com)
  • Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. (pharmacycode.com)
  • Furthermore, it's partially adrenolytic, as it is less selective than yohimbine on the adrenergic system, partially antagonizing alpha-1- adrenoreceptors. (anabolicminds.com)
  • Isoprenaline is a catecholamine non-selective beta-adrenergic agonist typically used to treat bradycardia and heart block. (drugbank.com)
  • Isoprenaline is a non-selective beta adrenergic receptor agonist used in a number of indications for the heart, as well as bronchospasm in anesthesia. (drugbank.com)
  • Isoprenaline is a non-selective beta adrenergic receptor agonist. (drugbank.com)
  • A beta-2 selective adrenergic antagonist. (lookformedical.com)
  • Rezatomidine is a selective antagonist of α2-adrenergic receptor and can be used in studies about chronic pain, including neuropathic pain. (targetmol.com)
  • Agonists 4-NEMD 7-Me-marsanidine (also I1 agonist) Agmatine (also I agonist, NMDA, 5-HT3, nicotinic antagonist and NOS inhibitor) Apraclonidine Brimonidine Cannabigerol (also acts as a moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist). (wikipedia.org)
  • The stimulating effect of NE on the TRH secretion was abolished by icv antagonist of adrenergic alpha2-receptor, yohimbine (40 nmol/L). (nel.edu)
  • Cirazoline is a full agonist at the α 1A adrenergic receptor , a partial agonist at both the α 1B and α 1D adrenergic receptors, [1] and a nonselective antagonist to the α 2 adrenergic receptor . (wikipedia.org)
  • These 3 categories of alpha-2-antagonist each possess a unique goal-specific attribute, but before we delve into specifics, let's look at how effective these compounds are for fat loss. (anabolicminds.com)
  • If there's one supplement to consume orally for stubborn fat loss, it's an alpha 2 antagonist. (anabolicminds.com)
  • A widely used non-cardioselective beta-adrenergic antagonist. (lookformedical.com)
  • Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist. (targetmol.com)
  • Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. (rndsystems.com)
  • epinephrine and isoproterenol might be expected to be effective bronchodilators because of their activity at 2 receptors. (pharmacology2000.com)
  • Isoproterenol with limited activity at alpha recetors has little effect. (pharmacology2000.com)
  • The α2-adrenergic receptor binds both norepinephrine released by sympathetic postganglionic fibers and epinephrine (adrenaline) released by the adrenal medulla, binding norepinephrine with slightly higher affinity. (wikipedia.org)
  • Derivatives of 2,5-DMA exhibited preferential high affinity at 5-HT2 serotonin receptors when compared to their relative affinities at 5-HT1 serotonin receptors. (erowid.org)
  • A pharmacological profile of the methylenedioxy-substituted amphetamine derivatives indicates that MDMA and MDA exhibited highest affinity for serotonin uptake sites, 5-HT2 serotonin, alpha 2-adrenergic and M-1 muscarinic receptors. (erowid.org)
  • Other behavioral, cardiovascular, and toxic effects of MDMA and related derivatives may be mediated by actions at other central and/or peripheral recognition sites, including muscarinic cholinergic receptors and alpha 2-adrenergic receptors, for which these compounds exhibit relatively high affinity. (erowid.org)
  • Pharmacological activity is mediated by the R-form, which exhibits about 100 times more affinity for the β-receptor compared to the S-form. (pharmacology2000.com)
  • In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro , and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. (pharmacycode.com)
  • Yohimbine possess extreme affinity for the alpha-2-adrenoreceptor, but due to receptor homology with various 5-HT receptors, yohimbine HCl is highly anxiogenic and is clinically used to model panic disorder. (anabolicminds.com)
  • The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
  • Studies in normal human subjects have shown that Prazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. (pharmacycode.com)
  • After 21 days of yohimbine supplementation, placebo remained unchanged but the yohimbine group lost about 2% bodyfat, taking them all the way to 7% BF. (anabolicminds.com)
  • 3 weeks of Yohimbine supplementation caused a 2% reduction in bodyfat from an already shredded baseline of 9% BF, all the while preserving muscle mass and strength/endurance. (anabolicminds.com)
  • And then we have the various yohimbe alkaloids like 11-OH yohimbine, that are alpha-2-antagonists (not to be confused with a broad-spectrum extract of alkaloids). (anabolicminds.com)
  • 2. The recommended dose for yohimbine is 0.2mg/kg BW in isolation. (anabolicminds.com)
  • Although GABA activates synaptic (αβγ) GABA A receptors with high efficacy, partial agonist activation of αβγ isoforms and GABA activation of the primary extrasynaptic (αβδ) GABA A receptors are limited to low-efficacy activity, characterized by minimal desensitization and brief openings. (jneurosci.org)
  • Although the physiological relevance of endogenous partial agonists remains poorly understood, the possibility of reversible augmentation of partial agonist efficacy by endogenous modulators raises the interesting possibility of plasticity at the level of agonist-dependent gating. (jneurosci.org)
  • Interrelationship between alpha- and beta-adrenergic agonists and histamine in canine airways. (uchicago.edu)
  • These agents act by competitive inhibition of histamine at the H1 receptor. (medscape.com)
  • Additional therapeutic benefits associated with β-adrenergic receptor agonists likely include reduced pulmonary mast cell leukotriene and histamine release, reduced microvascular permeability, phospholipase A 2 inhibition and increased mucociliary activity. (pharmacology2000.com)
  • it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin r. (targetmol.com)
  • Pharmacological characterization of alpha(2)adrenoceptors mediating this process. (nel.edu)
  • Pharmacological characterization of alpha adrenergic receptors in the young and old female rabbit urethra. (aspetjournals.org)
  • The pharmacological characteristics of alpha-1 and alpha-2 adrenergic receptors in young (6 month) and old (4.5-5 year) female rabbit urethra were studied using isolated muscle bath techniques. (aspetjournals.org)
  • Olodaterol is a novel, long-acting β2-adrenergic agonist (EC50s: 97.7 nM for the human β2-adrenoceptor) that exerts its pharmacological effect by binding and act. (targetmol.com)
  • To understand better the cellular mechanisms of NE and its adrenergic receptors in the LA, we used antibodies directed against dopamine beta-hydroxylase (DβH), the synthetic enzyme for NE, or against two different isoforms of the beta-adrenergic receptors (βARs), one that predominately recognizes neurons (βAR 248) and the other astrocytes (βAR 404), to characterize the microenvironments of DβH and βAR. (frontiersin.org)
  • Rotigotine Hydrochloride, a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. (targetmol.com)
  • The vascular 5-HT 1 receptor subtype that sumatriptan activates is present on cranial arteries in both dog and primate, on the human basilar artery, and in the vasculature of human dura mater and mediates vasoconstriction. (nih.gov)
  • In addition to causing vasoconstriction, experimental data from animal studies show that sumatriptan also activates 5-HT 1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels. (nih.gov)
  • These drugs bind to α1 receptors and activate them, leading to vasoconstriction and increased blood pressure. (proprofs.com)
  • α receptor activation causes vasoconstriction. (pharmacology2000.com)
  • It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. (lookformedical.com)
  • In the current study, pregnant rats were given 10 mg/kg of terbutaline on gestational days 17, 18 and 19 and adrenergic receptor binding capabilities examined in brain regions of the offspring. (duke.edu)
  • Agonists (activators) of the α2-adrenergic receptor are frequently used in anaesthesia where they affect sedation, muscle relaxation and analgesia through effects on the central nervous system (CNS). (wikipedia.org)
  • Pretreatment with chlorethylclonidine, which selectively alkylates the alpha-1B subtype, did not affect the Emax value of phenylephrine-induced contractions, but significantly shifted the curve to the right. (aspetjournals.org)
  • Epinephrine, Norepinephrine, and Phenylephrine select α1 receptors agonistically. (proprofs.com)
  • In addition, science higher blood pressure also results into the devastation of coronary arteries, kidneys, brain and eyes.2 and 3 Target identification events have confirmed the cardinal role in regulation of a variety of physiological events, markedly within the cardiovascular system. (peptidecost.com)
  • Physiological antagonism caused by adrenergic stimulation of canine tracheal muscle. (uchicago.edu)
  • Since 2 receptors are activated at lower, physiological concentrations, vasodilation results. (pharmacology2000.com)
  • "Lysergic acid diethylamide (LSD) administration selectively downregulates serotonin2 receptors in rat brain" Neuropsychopharmacology . (erowid.org)
  • Drugs that selectively bind to and activate beta-adrenergic receptors. (lookformedical.com)
  • The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. (wikipedia.org)
  • Drugs such as adrenoceptor agonists, muscarinic agonists, nitrates, and calcium channel blockers all affect smooth muscle. (britannica.com)
  • A 61603 hydrobromide is a potent α -adrenoceptor agonist that is at least 35-fold more potent at α 1A than at α 1B or α 1D sites. (rndsystems.com)
  • Interaction of α1-adrenoceptor subtypes with different G proteins induces opposite effects on cardiac L-type Ca2+ channel. (rndsystems.com)
  • Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. (nih.gov)
  • The adrenoceptor subtype in mediating nicotine-induced vasodilation in isolated porcine basilar arterial rings denuded of endothelium was therefore examined pharmacologically and immunohistochemically. (lookformedical.com)
  • Results from using an in vitro tissue bath technique indicated that propranolol and preferential beta(2)-adrenoceptor antagonists (ICI-118,551 and butoxamine), in a concentration-dependent manner, blocked the relaxation induced by nicotine (100 microM) without affecting the relaxation elicited by transmural nerve stimulation (TNS, 8 Hz). (lookformedical.com)
  • Results of double-labeling studies indicated that beta(2)-adrenoceptor immunoreactivities and NADPH diaphorase reactivities were colocalized in the same nerve fibers in basilar and middle cerebral arteries. (lookformedical.com)
  • Guanabenz hydrochloride is an orally active α2-adrenoceptor agonist with hypotensive effects. (targetmol.com)
  • Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist. (targetmol.com)
  • ST-91 is an agonist of α2-adrenoceptor with a mixed α-adrenergic receptor type/subtype selection profile. (targetmol.com)
  • Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central and peripheral nervous systems. (wikipedia.org)
  • Specific antagonists and agonists of alpha(2)-adrenoceptors were employed for the characterization of alpha(2)-adrenoceptors involved in the autoregulation of depolarization-evoked release of norepinephrine in the pig pineal. (nel.edu)
  • By binding to α2 receptors in the CNS, clonidine can modulate the release of norepinephrine, resulting in a decrease in sympathetic outflow and ultimately leading to a decrease in heart rate. (proprofs.com)
  • The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β2 agonists and α2 agonists, which are used to treat high blood pressure and asthma, for example. (targetmol.com)
  • 1 , 4 Dissociation of the alpha subunit activates adenylate cyclase, converting ATP to cyclic AMP. (drugbank.com)
  • In the alveoli, agonism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the end result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase. (drugbank.com)
  • Heart failure (HF) is characterized by markedly elevated levels of catecholamines that bind to adrenergic receptors (ARs) in the heart. (unc.edu)
  • Because it crosses the blood-brain barrier so that the the alpha receptors it binds are ones in the CNS instead of on the effector organ. (proprofs.com)
  • This means that the alpha receptors it binds to are located in the central nervous system (CNS) rather than on the effector organ, which in this case is the heart. (proprofs.com)
  • Alternatively, one can admit that CEC is able to inhibit alpha-2 autoreceptors, which causes an increase of the transmitter release, and to activate a nonadrenergic inhibitory receptor thus causing a reduction of the transmitter release. (unesp.br)
  • The present data indicate that activated alpha 2-adrenergic and muscarinic receptors inhibit dihydropyridine-sensitive Ca2+ channels via pertussis toxin-sensitive G proteins without the involvement of a cAMP-dependent intermediate step. (mdc-berlin.de)
  • This means that they block or inhibit the activity of the α1 receptors. (proprofs.com)
  • The signal may stimulate or inhibit the receiving cell, depending on the neurotransmitter and receptor involved. (msdmanuals.com)
  • These two branches control heart rate by stimulating different G protein-coupled receptors (GPCRs), which in turn activate ion channels that modify the electrical properties of cardiac pacemaker cells ( DiFrancesco, 1993 ). (elifesciences.org)
  • 2 Agonism of beta-1 and beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to exchange GMP for GTP, activating them, and allowing the alpha subunit to dissociate from the beta and gamma subunits. (drugbank.com)
  • Clonidine uniquely stimulates α 2 receptors, yet affects the heart rate which is normally affected by beta receptors. (proprofs.com)
  • Why can this drug affect the heart rate by affecting alpha instead of beta receptors? (proprofs.com)
  • It is also located on the vascular smooth muscle cells of certain blood vessels, such as those found in skin arterioles or on veins, where it sits alongside the more plentiful α1-adrenergic receptor. (wikipedia.org)
  • α receptor dominate in the cutaneous vascular beds. (pharmacology2000.com)
  • Both α and β adrenergic receptor are present in skeletal muscle vascular beds. (pharmacology2000.com)
  • The methylenedioxy amphetamine derivatives exhibited an inverse stereospecificity with respect to serotonin uptake sites versus postsynaptic 5-HT receptors with the S(+) isomer being more potent at the presynaptic recognition site, while the R(-) isomer was more potent at the postsynaptic recognition sites. (erowid.org)
  • These observations suggest that LSD and other indole hallucinogens may act as 5-HT2 agonists at postsynaptic 5-HT2 receptors. (erowid.org)
  • 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. (lookformedical.com)
  • The alpha-2 receptor is an autoreceptor, meaning it is located NOT on the postsynaptic neuron chiefly, but on the pre-synaptic neuron. (anabolicminds.com)
  • In such cases, the dendrites (a neuron's receiving branches) on the postsynaptic neurons release neurotransmitters that affect receptors on the presynaptic neurons. (msdmanuals.com)
  • Prazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. (pharmacycode.com)
  • Unlike 2,5-DMA derivatives, MDMA and MDA demonstrated little selectivity for 5-HT2 versus 5-HT1 subtypes of receptors. (erowid.org)
  • The regional and subtype selectivity are compatible with primary deficits in the development of noradrenergic projections to the cerebellum identified in previous studies and provide further evidence that therapeutic use of beta-adrenergic agonists may produce neurobehavioral teratology. (duke.edu)
  • Many GABA A receptor modulators exhibit clear subunit selectivity ( Olsen and Macdonald, 2002 ). (jneurosci.org)
  • Likewise, beta-adrenergic antagonists (e.g. propranolol (Inderal)) can induce depression and fatigue. (hedweb.com)
  • The contractile mechanism of skeletal muscles entails the binding of acetylcholine to nicotinic receptors on the membranes of muscle fibres. (britannica.com)
  • Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver, 5 glucagon release from the pancreas, and activation of the renin-angiotensin-aldosterone system. (drugbank.com)
  • The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. (lookformedical.com)
  • The purpose of this study was to examine the analgesic action of peripheral muscarinic receptors by administering intra-articular neostigmine after operation in patients undergoing knee arthroscopy. (asahq.org)
  • [1] Recently for opioid and alpha 2 -adrenergic receptors, a peripheral analgesia was demonstrated. (asahq.org)
  • Some drugs for the treatment of asthma block the binding of leukotrienes to their receptor. (britannica.com)
  • Because this mechanism is relatively insensitive to drug action, the most important group of drugs that affect the neuromuscular junction act on (1) acetylcholine release, (2) acetylcholine receptors, or (3) the enzyme acetylcholinesterase (which normally inactivates acetylcholine to terminate muscle fibre contraction). (britannica.com)
  • Neuromuscular blocking drugs act on acetylcholine receptors and fall into two distinct groups: nondepolarizing (competitive) and depolarizing blocking agents. (britannica.com)
  • Competitive neuromuscular blocking drugs act as antagonists at acetylcholine receptors, reducing the effectiveness of acetylcholine in generating an end-plate potential . (britannica.com)
  • Which drugs select α 1 receptors and indicate whether agonistically or antagonistically. (proprofs.com)
  • Ephedrine and Pseudo-Ephedrine are referred to as mixed acting drugs because they exhibit both antagonistic and stimulatory effects on their receptor simultaneously. (proprofs.com)
  • This dual action of the drugs on the receptor is what classifies them as mixed acting drugs. (proprofs.com)
  • Short-acting β 2 -adrenergic agonists administered by inhalation represent drugs of choice for management of acute asthma presentations and for prevention of exercise-induced bronchospastic reactions. (pharmacology2000.com)
  • Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. (lookformedical.com)
  • Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lookformedical.com)
  • Smart Drugs 2. (hedweb.com)
  • The α2A-adrenergic agonist, guanfacine, is now used to treat prefrontal cortical cognitive disorders such as Attention Deficit Hyperactivity Disorder. (wikipedia.org)
  • Clonidine is able to affect the heart rate by stimulating α2 receptors instead of β receptors because it has the ability to cross the blood-brain barrier. (proprofs.com)
  • The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. (rndsystems.com)
  • The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS. (lookformedical.com)
  • [4] [5] However, in preliminary studies, through stimulation of α 2 adrenoceptors, working memory is comparatively improved. (wikipedia.org)
  • [1-5] Muscarinic receptors, located in the substantia gelatinosa of the spinal cord, are believed to be involved in this analgesic property, which is not due to stimulation of nicotinic or opioid receptors. (asahq.org)
  • As many of you may already know, alpha-2-antagonists are simply compounds that antagonize the alpha-2-adrenoreceptor. (anabolicminds.com)
  • Furthermore, because alpha-2 antagonism can increase insulin release, these compounds are best taken fasted. (anabolicminds.com)
  • Four pertussis toxin-sensitive G proteins were identified in membranes of PC-12 cells: two members of the Gi family, Gi1 and Gi2, and two members of the Go family, Go2 and another Go subtype (possibly Go1). (mdc-berlin.de)
  • The proteins synthesized by parotid acinar cells are stored in large secretory granules whose composition includes α-amylase, leucine-rich parotid secretory protein (PSP), and proline-rich proteins (PRPs), in addition to multiple minor components 2-3 related to digestive and protective functions. (bvsalud.org)
  • This means that while they bind to the receptor in an antagonistic manner, they also stimulate the receptor at the same time. (proprofs.com)
  • The activated receptor catalyzes removal of GDP from the G protein alpha subunit (Gα i ), which allows intracellular GTP to bind. (elifesciences.org)
  • Neurotransmitters that are released bind to receptors on another neuron. (msdmanuals.com)
  • Neurotransmitters diffuse across the synaptic cleft and bind briefly to specific receptors on the adjoining neuron or effector cell. (msdmanuals.com)
  • [3] Administration of cirazoline also seemed to present impairment in the spatial memory of monkeys through the activation of the same receptors that showed decreased food intake in rats. (wikipedia.org)
  • 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. (lookformedical.com)
  • 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. (lookformedical.com)
  • β receptor activation promotes vasodilatation. (pharmacology2000.com)
  • Salivary seromucous glands are regulated predominantly by parasympathetic activation of muscarinic receptors, resulting in exocrine secretion of mucins and macroglobulin responsible by lubrication and protection of oral mucosa 3-4 . (bvsalud.org)
  • Dr. Beak discovered that the orphan nuclear receptor, RORα, is expressed in the mouse and human heart and mediates cardiac hypertrophy in response to angiotensin II. (unc.edu)
  • Combination of long-acting β-adrenergic receptor agonists with anti-inflammatory agents represents a strongly endorsed therapeutic approach. (pharmacology2000.com)
  • In the brain, α2-adrenergic receptors can be localized either pre- or post-synaptically, and the majority of receptors appear to be post-synaptic. (wikipedia.org)
  • For example, the alpha-2A adrenergic receptor subtype is post-synaptic in the prefrontal cortex and these receptors strengthen cognitive and executive functions by inhibiting cAMP opening of potassium channels, thus enhancing prefrontal connections and neuronal firing. (wikipedia.org)
  • An Alpha-1A Adrenergic Receptor Agonist Prevents Acute dox. (rndsystems.com)
  • Central adrenergic system may play a stimulating role through alpha2-receptor in the acute hypoxia-modulating TRH release from rat hypothalamus. (nel.edu)
  • Pretreatment of cells with pertussis toxin or intracellular infusion of the GDP analogue guanosine-5'-O-(2-thiodiphosphate) was without effects on the control Ca2+ channel current but abolished its hormonal inhibition. (mdc-berlin.de)
  • Acts primarily on somatostatin receptor subtypes II and V. Inhibits GH secretion and has many other endocrine and nonendocrine effects, including inhibition of glucagon, VIP, and GI peptides. (medscape.com)
  • beta-Adrenergic agonists used in therapy of premature labor and asthma cross the placenta and can affect development of the fetal nervous system. (duke.edu)
  • Most recently, research with ampakines , modulators of neurotrophin-regulating AMPA -type glutamate receptors, suggests that designer nootropics will soon deliver sharper intellectual performance even to healthy young adults. (hedweb.com)
  • The aim of the study was to ascertain whether rilmenidine, a second generation imidazoline-alpha-2-adrenoreceptor agonist, is able to increase analgesic effects of ibuprofen in the writhing test in mice. (nel.edu)
  • In addition, the neurotoxic, psychotomimetic, analgesic, temperature regulation, and mood-altering effects of MDMA and other methylenedioxy-substituted derivatives may be mediated, in part, through their actions at other serotonin recognition sites in brain, including serotonin uptake sites and 5-HT1A serotonin receptors. (erowid.org)
  • Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. (rndsystems.com)
  • It is even more intriguing to consider the potential plasticity of allosteric modulation given the observation of agonist-dependent functional properties of GABA A receptors. (jneurosci.org)
  • Cardiac alpha (α)1-ARs have received less attention, however data from cell and animal studies indicate that they protect against the development of HF. (unc.edu)
  • It has several general functions in common with the α1-adrenergic receptor, but also has specific effects of its own. (wikipedia.org)
  • There were significant correlations between the in vitro affinities of 2,5-DMA derivatives at 5-HT2 serotonin receptors and their human hallucinogenic potencies as well as with their potencies in behavioral generalization studies, suggesting the importance of 5-HT2 serotonin receptors in mediating the hallucinogenic effects of the various 2,5-DMA derivatives. (erowid.org)
  • The relatively weak hallucinogenic effects of the methylenedioxy-substituted amphetamine derivatives (when compared to the 2,5-DMA derivatives) may be mediated through actions at 5-HT2 serotonin receptors. (erowid.org)
  • Anti-sialogue (anticholinergic) - reduces salivary and GIT secretions (pre-operative prep) due to widespread location of autonomic receptors side effects are common which both the clinician and patient should be aware of. (emedsa.org.au)
  • The anti-tumour effects of α2-AR agonists were reverted by α2-AR antagonists, and were absent in Adra2a-knockout (encoding α2a-AR) mice, demonstrating on-target action exerted on host cells, not tumour cells. (bvsalud.org)
  • To exert their anti-tumour effects, α2-AR agonists required CD4+ T lymphocytes, CD8+ T lymphocytes and macrophages. (bvsalud.org)
  • Furthermore, 2,5-DMA derivatives exhibited agonist-like binding characteristics at 5-HT2 serotonin receptors with the R(-) isomer being the more potent isomer. (erowid.org)
  • The process is reversed by the alpha subunit, which hydrolyses GTP to GDP followed by reformation of the Gα i (GDP)βγ complex. (elifesciences.org)
  • The unusual sensitivity of αβδ receptor channels to neurosteroid modulation prompted investigation of whether this high sensitivity was dependent on the δ subunit or the low-efficacy channel function that it confers. (jneurosci.org)
  • We suggest that neurosteroids preferentially enhance low-efficacy GABA A receptor activity independent of subunit composition. (jneurosci.org)
  • The present study was undertaken to look for the effect of chloroethylclonidine (CEC) on prejunctional alpha-2 autoreceptors of the canine saphenous vein. (unesp.br)