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.
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.
Transcriptional regulation of alpha1-adrenoceptor gene in the rat liver during different phases of sepsis. (1/1305)Changes in alpha1-adrenoceptor (alpha1AR) gene expression in the rat liver during different phases of sepsis were studied. Sepsis was induced by cecal ligation and puncture (CLP). Septic rats exhibit two metabolically distinct phases: an initial hyperglycemic phase (9 h after CLP, early sepsis) followed by a hypoglycemic phase (18 h after CLP; late sepsis). The [3H]prazosin binding studies show that the density of alpha1AR was increased by 30% during the early phase while it was decreased by 24% during the late phase of sepsis. Western blot analyses reveal that alpha1AR protein level was elevated by 48% during early sepsis but was decreased by 55% during late sepsis. Northern blot analyses depict that the steady-state level of alpha1bAR mRNA was enhanced by 21% during the early phase but was declined by 29% during the late phase of sepsis. Nuclear run-off assays show that the transcription rate of alpha1bAR gene transcript was increased by 76% during early sepsis while it was decreased by 29% during late sepsis. The actinomycin D pulse-chase studies indicate that the half-life of alpha1bAR mRNA remained unaffected during the early and the late phases of sepsis. These findings demonstrate that during the early phase of sepsis, the increase in the rate of transcription of alpha1bAR gene paralleled with the elevations in the alpha1bAR mRNA abundance and alpha1AR protein level, while during the late phase of sepsis, the decrease in the rate of transcription of alpha1bAR gene coincided with the declines in the alpha1bAR mRNA abundance and the alpha1AR protein level in the rat liver. These observations indicate that the altered expression of alpha1AR genes in the rat liver during the progression of sepsis was regulated transcriptionally. (+info)
Expression of alpha2-adrenergic receptors in rat primary afferent neurones after peripheral nerve injury or inflammation. (2/1305)1. Immunocytochemistry with polyclonal antibodies directed against specific fragments of intracellular loops of alpha2A- and alpha2C-adrenergic receptors (alpha2A-AR, alpha2C-AR) was used to explore the possibility that expression of these receptors in dorsal root ganglion (DRG) neurones of rat alters as a result of peripheral nerve injury or localized inflammation. 2. Small numbers of neurones with positive alpha2A-AR immunoreactivity (alpha2A-AR-IR) were detected in DRG from normal animals or contralateral to nerve lesions. In contrast, after complete or partial sciatic nerve transection the numbers of ipsilateral L4 and L5 DRG somata expressing alpha2A-AR-IR sharply increased (>5-fold). There was no discernible change in the number of DRG neurones exhibiting alpha2A-AR-IR innervating a region in association with localized chemically induced inflammation. 3. After nerve injury, double labelling with Fluoro-Gold, a marker of retrograde transport from transected fibres, or by immunoreactivity for c-jun protein, an indicator of injury and regeneration, suggested that many of the neurones expressing alpha2A-AR-IR were uninjured by the sciatic lesions. 4. In general the largest proportionate increase in numbers of neurones labelled by alpha2A-AR-IR after nerve lesions appeared in the medium-large diameter range (31-40 microm), a group principally composed of cell bodies of low threshold mechanoreceptors. The number of small diameter DRG neurones labelled by alpha2A-AR-IR, a category likely to include somata of nociceptors, also increased but proportionately less. 5. Relatively few DRG neurones exhibited alpha2C-AR-IR; this population did not appear to change after either nerve lesions or inflammation. 6. These observations are considered in relation to effects of nerve injury on excitation of primary afferent neurones by sympathetic activity or adrenergic agents, sympathetically related neuropathy and reports of sprouting of sympathetic fibres in DRG. (+info)
alpha-adrenergic stimulation mediates glucose uptake through phosphatidylinositol 3-kinase in rat heart. (3/1305)We examined whether insulin and catecholamines share common pathways for their stimulating effects on glucose uptake. We perfused isolated working rat hearts with Krebs-Henseleit buffer containing [2-3H]glucose (5 mmol/L, 0.05 microCi/mL) and sodium oleate (0.4 mmol/L). In the absence or presence of the phosphatidylinositol 3-kinase (PI3-K) inhibitor wortmannin (3 micromol/L), we added insulin (1 mU/mL), epinephrine (1 micromol/L), phenylephrine (100 micromol/L) plus propranolol (10 micromol/L, selective alpha-adrenergic stimulation), or isoproterenol (1 micromol/L) plus phentolamine (10 micromol/L, selective beta-adrenergic stimulation) to the perfusate. Cardiac power was found to be stable in all groups (between 8.07+/-0.68 and 10.7+/-0. 88 mW) and increased (25% to 47%) with addition of epinephrine, but not with selective alpha- and beta-adrenergic stimulation. Insulin and epinephrine, as well as selective alpha- and beta-receptor stimulation, increased glucose uptake (the following values are in micromol/[min. g dry weight]: basal, 1.19+/-0.13; insulin, 3.89+/-0.36; epinephrine, 3.46+/-0.27; alpha-stimulation, 4.08+/-0.40; and beta-stimulation, 3.72+/-0.34). Wortmannin completely inhibited insulin-stimulated and selective alpha-stimulated glucose uptake, but it did not affect the epinephrine-stimulated or selective beta-stimulated glucose uptake. Sequential addition of insulin and epinephrine or insulin and alpha-selective stimulation showed additive effects on glucose uptake in both cases. Wortmannin further blocked the effects of insulin on glycogen synthesis. We conclude that alpha-adrenergic stimulation mediates glucose uptake in rat heart through a PI3-K-dependent pathway. However, the additive effects of alpha-adrenergic stimulation and insulin suggest 2 different isoforms of PI3-K, compartmentation of PI3-K, potentiation, or inhibition by wortmannin of another intermediate of the alpha-adrenergic signaling cascade. The stimulating effects of both the alpha- and the beta-adrenergic pathways on glucose uptake are independent of changes in cardiac performance. (+info)
Sympathetic nervous system activity and alpha-adrenergic responsiveness in older hypertensive humans. (4/1305)We have previously demonstrated in normotensive humans an age-associated increase in sympathetic nervous system (SNS) activity combined with appropriate downregulation of alpha-adrenergic responsiveness. Impaired downregulation of alpha-adrenergic responsiveness, despite a comparable level of SNS activity, could contribute to higher blood pressure in older hypertensive humans. We measured arterial plasma norepinephrine (NE) levels and the extravascular NE release rate (NE2) derived from [3H]NE kinetics (to assess systemic SNS activity), and platelet and forearm arterial adrenergic responsiveness in 20 normotensive (N) and in 24 hypertensive (H), otherwise healthy, older subjects (60-75 yr). Although plasma NE levels were similar (N 357 +/- 27 vs. H 322 +/- 22 pg/ml; P = 0.37), NE2 tended to be greater in the hypertensive group (H 2.23 +/- 0.21 vs. N 1.64 +/- 0.20 microgram. min-1. m-2; P = 0. 11), and the NE metabolic clearance rate was greater (H 1,100 +/- 30 vs. N 900 +/- 50 ml/m2; P = 0.004). In the hypertensive group, there was a greater alpha-agonist-mediated inhibition of platelet membrane adenylyl cyclase activity and a NE- but not ANG II-mediated decrease in forearm blood flow. Compared with normotensive subjects, in older hypertensive subjects 1) NE metabolic clearance rate is increased, 2) systemic SNS activity tends to be increased, and 3) arterial and platelet alpha-adrenergic responsiveness is enhanced. These results suggest that heightened SNS activity coupled with enhanced alpha-adrenergic responsiveness may contribute to elevated blood pressure in older hypertensive humans. (+info)
Hemodynamic basis for the acute cardiac effects of troglitazone in isolated perfused rat hearts. (5/1305)Troglitazone is a thiazolidinedione used for the treatment of NIDDM and potentially for other insulin-resistant disease states. Troglitazone has recently been shown to increase cardiac output and stroke volume in human subjects. These actions are thought to be mediated by the reduction of peripheral resistance, but a potential direct effect on cardiac function has not been studied. Therefore, we investigated the direct cardiac hemodynamic effects of troglitazone in isolated perfused rat hearts. Five groups of hearts were studied. Hearts were tested under isovolumetric contraction with a constant coronary flow, and troglitazone (0.2, 0.5, and 1.0 micromol) was administered by bolus injection. Peak isovolumetric left ventricular pressure (LVPmax), peak rate of rise of LVP (dP/dt(max)), and peak rate of fall of LVP (dP/dt(min)) were significantly increased 1 min after troglitazone administration in a dose-dependent manner, while the heart rate (HR) and coronary perfusion pressure (CPP) were significantly decreased (P < 0.05). HR was then fixed by pacing and/or CPP was fixed with nitroprusside to eliminate any effect of the two variables on the action of troglitazone. With constant HR and/or constant CPP, the effect of troglitazone on LVPmax, dP/dt(max), and dP/dt(min) was still unchanged. In addition, the positive inotropic, positive lusitropic, and negative chronotropic actions of troglitazone were not influenced even when hearts were pretreated with prazosin, propranolol, or nifedipine. In conclusion, troglitazone has direct positive inotropic, positive lusitropic, negative chronotropic, and coronary artery dilating effects. The inotropic and chronotropic actions of troglitazone are not mediated via adrenergic receptors or calcium channels. These findings have important clinical implications for diabetic patients with congestive heart failure. (+info)
Non-specific action of methoxamine on Ito, and the cloned channels hKv 1.5 and Kv 4.2. (6/1305)The alpha1-adrenoceptor agonist methoxamine acted independently of receptor activation to reduce Ito and the sustained outward current in rat ventricular myocytes, and hKv 1.5 and Kv 4.2 cloned K+ channel currents. Two hundred microM methoxamine reduced Ito by 36% in the presence of 2 microM prazosin, and by 37 and 38% after preincubation of myocytes with either N-ethylmaleimide or phenoxybenzamine (n=6). The EC50 values at +60 mV for direct reduction of Ito, hKv 1.5, and Kv 4.2 by methoxamine were 239, 276, and 363 microM, respectively, with Hill coefficients of 0.87-1.5. Methoxamine accelerated Ito and Kv 4.2 current inactivation in a concentration- and voltage-dependent manner. Apparent rate constants for methoxamine binding and unbinding gave Kd values in agreement with EC50 values measured from dose-response relations. The voltage-dependence of block supported charged methoxamine binding to a putative intracellular site that sensed approximately 20% of the transmembrane electrical field. In the presence of methoxamine, deactivating Kv 4.2 tail currents displayed a distinct rising phase, and were slowed relative to control, such that tail current crossover was observed. These observations support a dominant mechanism of open channel block, although closed channel block could not be ruled out. Single-channel data from hKv 1.5 patches revealed increased closed times with blank sweeps and decreased burst duration in the presence of drug, and a reduction of mean channel open time from 1.8 ms in control to 0.4 ms in 500 microM methoxamine. For this channel, therefore, both open and closed channel block appeared to be important mechanisms for the action of methoxamine. (+info)
Human dynamic closed-loop accommodation augmented by sympathetic inhibition. (7/1305)PURPOSE: A ciliary alpha-adrenoceptor accommodative effect has been proposed, caused by a small population of alpha1-inhibitory receptors in excised human ciliary muscle. This study was intended to investigate the effect on the closed-loop dynamic accommodative process of modulating alpha1-adrenoceptor activity by topical instillation of the alpha1-adrenergic agonist, phenylephrine hydrochloride. METHODS: A group of 10 visually normal subjects viewed a photopic (30 candela/m2) high-contrast Maltese cross, which was modulated sinusoidally (0.05-0.6Hz) and stepwise over a 2-D range (2-4 D). Monocular temporal accommodation responses were measured using a continuously recording dynamic tracking infrared optometer under two trial conditions: after instillation of saline control solution and 50 minutes subsequent to the instillation of 0.27 microl 0.4% benoxinate hydrochloride and 0.27 microl 2.5% phenylephrine hydrochloride. Pupil size and accommodative amplitude were measured at 90-second intervals for 50 minutes after drug instillation. All accommodative measurements were recorded through a fixed 4-mm pupil. RESULTS: A significant reduction in accommodative amplitude (11%; P < 0.05) was recorded, whereas pupil size showed a significant increase (33%; P < 0.05). No significant change in step-response dynamics was observed. However, phenylephrine hydrochloride caused a significant increase in accommodative gain in the low and midtemporal frequency ranges compared with the effect of a saline control treatment. No significant variation in phase lag was observed. CONCLUSIONS: For the first time in humans, this study shows that augmentation of the alpha1-inhibitory sympathetic contribution results in increased accommodative gain at low and midtemporal frequencies, which is consistent with findings in animal studies. (+info)
Receptor subtype mediating the adrenergic sensitivity of pain behavior and ectopic discharges in neuropathic Lewis rats. (8/1305)Receptor subtype mediating the adrenergic sensitivity of pain behavior and ectopic discharges in neuropathic Lewis rats. We attempted to identify the subtype of alpha-adrenergic receptor (alpha-AR) that is responsible for the sympathetic (adrenergic) dependency of neuropathic pain in the segmental spinal injury (SSI) model in the Lewis strain of rat. This model was chosen because our previous study showed that pain behaviors in this condition are particularly sensitive to systemic injection of phentolamine (PTL), a general alpha-AR blocker. We examined the effects of specific alpha1- and alpha2-AR blockers on 1) behavioral signs of mechanical allodynia, 2) ectopic discharges recorded in the in vivo condition, and 3) ectopic discharges recorded in an in vitro setup. One week after tight ligation of the L5 and L6 spinal nerves, mechanical thresholds of the paw for foot withdrawals were drastically lowered; we interpreted this change as a sign of mechanical allodynia. Signs of mechanical allodynia were significantly relieved by a systemic injection of PTL (a mixed alpha1- and alpha2-AR antagonist) or terazosin (TRZ, an alpha1-AR antagonist) but not by various alpha2-AR antagonists (idazoxan, rauwolscine, or yohimbine), suggesting that the alpha1-AR is in part the mediator of the signs of mechanical allodynia. Ongoing ectopic discharges were recorded from injured afferents in fascicles of the L5 dorsal root of the neuropathic rat with an in vivo recording setup. Ongoing discharge rate was significantly reduced after intraperitoneal injection of PTL or TRZ but not by idazoxan. In addition, by using an in vitro recording setup, spontaneous activity was recorded from teased dorsal root fibers in a segment in which the spinal nerve was previously ligated. Application of epinephrine to the perfusion bath enhanced ongoing discharges. This evoked activity was blocked by pretreatment with TRZ but not with idazoxan. This study demonstrated that both behavioral signs of mechanical allodynia and ectopic discharges of injured afferents in the Lewis neuropathic rat are in part mediated by mechanisms involving alpha1-ARs. These results suggest that the sympathetic dependency of neuropathic pain in the Lewis strain of the rat is mediated by the alpha1 subtype of AR. (+info)
Alpha-adrenergic receptor synonyms, alpha-adrenergic receptor antonyms - FreeThesaurus.com
Synonyms for alpha-adrenergic receptor in Free Thesaurus. Antonyms for alpha-adrenergic receptor. 2 synonyms for alpha-adrenergic receptor: alpha receptor, alpha-adrenoceptor. What are synonyms for alpha-adrenergic receptor?
Selective modification of renal alpha 2-adrenergic receptors in Milan hypertensive rat strain. | Hypertension
Cerebral and renal alpha-adrenergic receptors play an important role in the control of blood pressure. We studied alpha-adrenergic receptors in the cerebral and renal cortex of Milan hypertensive strain (MHS) and normotensive strain (MNS) rats, a genetic model of spontaneous hypertension linked to a kidney abnormality. Binding of the selective alpha 1-adrenergic antagonist [3H]prazosin and the alpha 2-adrenergic antagonist [3H]rauwolscine was used for receptor studies in tissues of prehypertensive (24-day-old) and hypertensive (60-day-old) rats. In the cerebral cortex, no between-strain differences in alpha 1-adrenergic and alpha 2-adrenergic receptor density and affinity were observed in prehypertensive and hypertensive periods. The density of these receptors increased similarly with age in MHS and MNS rats. In the renal cortex, the differences between MHS and MNS rats concerned alpha 2-adrenergic receptors only. Compared with their age-matched normotensive controls, MHS rats showed 1) a lower ...
Epinephrine decreases glucose clearance in man: An α adrenergic effect independent of inhibition of insulin secretion<...
TY - JOUR. T1 - Epinephrine decreases glucose clearance in man. T2 - An α adrenergic effect independent of inhibition of insulin secretion. AU - Rizza, R.. AU - Miles, J.. AU - Verdonk, C.. PY - 1979/1/1. Y1 - 1979/1/1. UR - http://www.scopus.com/inward/record.url?scp=0018389251&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0018389251&partnerID=8YFLogxK. M3 - Article. AN - SCOPUS:0018389251. VL - 27. SP - 375A. JO - Journal of Investigative Medicine. JF - Journal of Investigative Medicine. SN - 1081-5589. IS - 2. ER - ...
cholinergic and adrenergic effects and side effects Flashcards - Cram.com
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An alpha 2-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet alpha 2-adrenergic receptor as a probe. The deduced amino acid sequence resembles the human platelet ...
Alpha adrenergic receptor | definition of Alpha adrenergic receptor by Medical dictionary
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Changes in endothelium-dependent vasodilatation and alpha-adrenergic responses in resistance vessels during the menstrual cycle...
TY - JOUR. T1 - Changes in endothelium-dependent vasodilatation and alpha-adrenergic responses in resistance vessels during the menstrual cycle in healthy women. AU - Chan, N. Norman. AU - MacAllister, Raymond J.. AU - Colhoun, Helen M.. AU - Vallance, Patrick. AU - Hingorani, Aroon D.. N1 - 10.1210/jc.86.6.2499 Article 0021-972X. PY - 2001. Y1 - 2001. N2 - During the menstrual cycle, changes in endothelium-dependent vasodilatation have been demonstrated in conduit vessels in vivo, but responses in resistance vessels have not been studied. The aim of this study was to examine endothelium-dependent vasodilatation, the effects of local nitric oxide synthesis, and alpha-adrenergic constriction in resistance vessels during the menstrual cycle in 15 healthy female volunteers (mean age, 28.07 ± 2.1 yr). Forearm blood flow in response to intrabrachial infusion of bradykinin (10, 30, and 100 pmol/min; endothelium-dependent vasodilator), glyceryl trinitrate (4, 8, and 16 nmol/min; ...
Na+-dependent, alpha-adrenergic mobilization of intracellular (mitochondrial) Ca2+ in brown adipocytes.
The existence and significance of a hormone-sensitive, rapidly mobilizable intracellular pool of Ca2+ in hamster brown-fat cells was investigated with 45Ca2+-labelling techniques. It was shown that such a pool existed and was probably located within the abundant mitochondria. It was rapidly mobilized by norepinephrine (median effective concentration 50 nM) through alpha-adrenergic mechanisms. The mobilization of Ca2+ from the intracellular stores (mitochondria) required the presence of extracellular Na+, but not of Ca2+, K+ or Mg2+. It is concluded that the experiments are in agreement with a hypothesis linking the mobilization of intracellular Ca2+ pools with an alpha-adrenergically-induced increase in plasma membrane Na+ permeability (observed as a membrane depolarization), and a subsequent activation of the mitochondrial Na+/Ca2+ exchange, leading to mobilization of mitochondrial Ca2+ and the mediation of alpha-adrenergic effects as a result of an elevated cytosolic Ca2+ level.. ...
To more fully characterize the alterations in myocardial adrenergic and cholinergic receptors induced by the diabetic state, we investigated the binding characteristics of (-) [3H] dihydroalprenolol to beta adrenergic receptors (bAR), [3H] prazosin to alpha adrenergic receptors (aAR), and [3H] quinuclidinyl-benzilate to muscarinic cholinergic receptors (MCR) in myocardial membranes derived from rats 8 wk after treatment with streptozotocin. We also studied an equal number of animals from three control groups: free-eating nondi-abetics, pair-weighted nondiabetics, and streptozoto-cin-treated animals treated daily with insulin.. Diabetic hearts demonstrated 27% fewer bAR (P , 0.01) and 31% fewer aAR (P , 0.01) than free-eating controls, without changes in MCR, and without changes in antagonist affinity, agonist affinity, or agonist slope factor (pseudo-Hill coefficient) for any class of receptors. Food restriction had no effect on receptor characteristics, and treatment of diabetic rats with ...
3H]Dihydroergocryptine, a nonselective alpha adrenergic antagonist, the alpha-1 selective antagonist, [3H]prazosin and the alpha-2 selective antagonist, [3H]yohimbine, were used to study binding sites in rat renal membranes. To establish a correlation between binding and a biological function, the ability of alpha adrenergic agents to stimulate or inhibit vasoconstriction was quantified in vitro using an isolated perfused kidney preparation. Binding with each radioligand was rapid, saturable and specific. Moreover, the order of potencies of a variety of adrenergic agents, determined by competitive inhibition studies, suggested that the binding of each radioligand was to sites with alpha adrenergic specificity. The total number of binding sites in these rat renal membranes. determined with [3H]dihydroergocryptine (Bmax, 212 fmol/mg of protein; KD, 12.8 nM) was approximately equal to the sum of binding site concentrations determined with the alpha-1 and alpha-2 selective radioligands (Bmax, 57 and ...
Presynaptic modulation of the norepinephrine-induced β-adrenergic receptor desensitization phenomenon in vivo<...
TY - JOUR. T1 - Presynaptic modulation of the norepinephrine-induced β-adrenergic receptor desensitization phenomenon in vivo. AU - Nakamura, I.. AU - Yoshikawa, T.. AU - Anzai, T.. AU - Baba, A.. AU - Iwata, M.. AU - Wainai, Y.. AU - Suzuki, M.. AU - Ogawa, S.. PY - 2000/1/1. Y1 - 2000/1/1. N2 - Background: In vivo administration of norepinephrine fails to cause β-adrenergic receptor desensitization. However, short-term exposure of cultured cells to norepinephrine induces the phenomenon in vitro. We sought to identify the local regulatory mechanisms responsible for in vivo β-adrenergic receptor desensitization in congestive heart failure. Methods and Results: Control rabbits received norepinephrine (n = 7) or saline (n = 7) for 1 week, and rabbits with chemical denervation induced by 6-hydroxydopamine also received norepinephrine (n = 7) or saline (n = 7). Myocardial norepinephrine content decreased 80% in both groups of denervated rabbits. β1-Adrenergic receptor density in denervated ...
Receptors, Adrenergic, alpha-2 | Profiles RNS
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 ...
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Patent US20020197300 - Drug delivery system for anti-glaucomatous medication - Google Patents
The invention features polymeric hydrogel contact lenses containing an anti-glaucoma medication, such as a beta adrenergic receptor antagonist, e.g., timolol maleate, or an alpha adrenergic receptor agonist, e.g., brimonidine tartrate, and methods of fabrication and uses thereof. A medication is passively transferred into a contact lens by absorption from a dilute aqueous solution. Such treated lenses are contacted with the ocular fluid of an individual to treat glaucoma.
Buchweitz, Ellen and Weiss, Harvey R.: Effects of phenoxybenzamine or N-methyl chlorpromazine on regional cerebral blood flow: Comparison of central and peripheral alpha adrenergic receptor antagonism, vol. 223, no. 2, November, 1982, pp. 322-326.. Clarification: The chemical structure of the receptor antagonist N-methyl chlorpromazine iodide (incorrectly termed Aprobit, p. 323) used in this study was [3-(2-chloro-10-phenothiazinyl)propyl]trimethylammonium iodide. The compound is also known by the synonyms quarternary chlorpromazine iodide and chlorpromazine methiodide (SK&F 2680-J). The authors regret the inadvertent error in chemical structure printed in the Journal.. ...
Alpha-adrenergic | definition of alpha-adrenergic by Medical dictionary
Looking for online definition of alpha-adrenergic in the Medical Dictionary? alpha-adrenergic explanation free. What is alpha-adrenergic? Meaning of alpha-adrenergic medical term. What does alpha-adrenergic mean?
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Obesity often leads to hypertension. Previous work from my lab demonstrated that the adipocyte-derived hormone leptin reduces the ability of the aorta to contract in response to adrenergic stimulation, likely due to a decreased expression of the aorta alpha-adrenergic receptors. However, it is not known whether leptin decreases the expression of alpha-adrenergic receptors in such arteries like the mesenteric and renal arteries that play a key role in the control of blood pressure. To determine whether leptin decreases alpha-adrenergic receptor expression in renal and mesenteric arteries, I infused leptin (10ug/day) by implanting subcutaneous mini-pumps in five male C57bl/6 mice. Five mice did not receive leptin and served as controls. After seven days of treatment I euthanized nine mice as one mouse died. Renal and mesenteric arteries were taken from the mice and mRNa was extracted from the arteries. Reverse Transcription (RT) was completed in order to induce the transcription of mRNA into cDNA. ...
Regional Differences in β-Adrenergic Effects on Local Cerebral Blood Flow and Adrenergic Innervation | SpringerLink
Although it is now well documented (6, 8) that pial as well as intracerebral vessels are amply supplied with sympathetic adrenergic nerves which, as shown for pial arteries, fulfill ultra-structural...
Influence of adrenergic receptor stimulation on glucose metabolism during starvation in man: effects on circulating levels of...
Semantic Scholar extracted view of Influence of adrenergic receptor stimulation on glucose metabolism during starvation in man: effects on circulating levels of insulin growth hormone and free fatty acids. by Robert I Misbin et al.
Effects of exogenous and endogenous norepinephrine on the oxygen availability of intact muscular arteries.<...
TY - JOUR. T1 - Effects of exogenous and endogenous norepinephrine on the oxygen availability of intact muscular arteries.. AU - Moss, A. J.. AU - Minken, S. L.. AU - Samuelson, P.. AU - Angell, C.. PY - 1969/1/1. Y1 - 1969/1/1. UR - http://www.scopus.com/inward/record.url?scp=0014535404&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0014535404&partnerID=8YFLogxK. U2 - 10.1016/S0368-1319(69)80077-3. DO - 10.1016/S0368-1319(69)80077-3. M3 - Article. C2 - 5380898. AN - SCOPUS:0014535404. VL - 10. SP - 11. EP - 18. JO - Atherosclerosis. JF - Atherosclerosis. SN - 0021-9150. IS - 1. ER - ...
Myocardial alpha 1-adrenergic receptor stimulation. | Circulation
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Breaking the Mystery of Alpha Brainwaves
The brainwave entrainment technology has gained a lot of popularity these days. One of them that this technology is based on is the alpha brainwaves. These are the ...
We have used the subtype-selective radioligands [3H]prazosin (an alpha 1-adrenergic antagonist) and [3H]yohimbine (an alpha 2-adrenergic antagonist) to examine alpha-adrenergic receptors in rat renal cortical membranes. Under the conditions used in this study, [3H]prazosin bound only to alpha 1-adrenergic receptors, whereas [3H]yohimbine bound only to alpha 2-adrenergic receptors; the two radioligands were completely selective and did not bind to a common site. The ratio of alpha 2- to alpha 1-adrenergic receptors was about 3:1. Guanyl nucleotides decreased the affinity of epinephrine at both receptor subtypes, but this effect was greater at the alpha 2-receptor and, according to computer analysis, occurred through different mechanisms at the two receptor subtypes. NaCl decreased the affinity of epinephrine at both alpha-receptor subtypes; this effect was more Na+-selective at alpha 2- than at alpha 1-receptors. Guanyl nucleotides and NaCl were additive in decreasing the affinity of epinephrine ...
Εργοταμίνη τρυγική and breastfeeding. Are they compatible?
Ergot alkaloid and alpha adrenergic receptor antagonist with vasoconstrictor effect. Indicated in the treatment of acute migraine attack, usually together with caffeine. Oral administration every half hour if necessary, up to a maximum of 6 mg per day (Sandoz 2012, AEMPS 2009). Since the last update we have not found published data on its excretion in breastmilk. Its pharmacokinetic data (high molecular weight and high plasma protein binding) makes it unlikely it will transfer into breastmilk in significant amounts. Although gastrointestinal absorption is 62%, hepatic metabolism makes bioavailability less than 5% (AEMPS 2009), which impedes its transfer from breastmilk to infant plasma, except in premature infants and the immediate neonatal period when there may be greater intestinal permeability. Other ergot alkaloids, such as bromocriptine, inhibit prolactin secretion, but administration of 3mg daily of ergotamine during the first week postpartum did not affect the production of
Doxazosin mesylate CAS#: 77883-43-3
Doxazosin mesylate is a quinazoline compound that is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. Doxazosin mesylate is a new generation of quinazolone α1 receptor blocker developed by the Pfizer company (United States), It has a long half-life, exerting its effects of dilating the blood vessels, reducing the vascular resistance and lowering the blood pressure through blocking the a 1 receptor. It selectively blocks the a1 adrenergic receptor of the prostate smooth muscle matrix, capsule and bladder neck, alleviating the symptoms of patients of benign prostatic hyperplasia, while having good curing effect on the dysuria caused by simple prostatic hyperplasia.
Part 6: Advanced Cardiovascular Life Support | Circulation
Epinephrine hydrochloride produces beneficial effects in patients during cardiac arrest, primarily because of its α-adrenergic receptor-stimulating properties.1 The adrenergic effects of epinephrine increase myocardial and cerebral blood flow during CPR.2 The value and safety of the β-adrenergic effects of epinephrine are controversial because they may increase myocardial work and reduce subendocardial perfusion.3 Although epinephrine has been used universally in resuscitation, there is a paucity of evidence to show that it improves outcome in humans. For a number of years researchers and clinicians have also questioned the optimal dose of epinephrine. The standard dose of epinephrine (1.0 mg) is not based on body weight. Historically a standard dose of 1 mg epinephrine was used in surgical operating rooms for intracardiac injections.4 5 6 Surgeons observed that 1 to 3 mg of intracardiac epinephrine was effective in restarting the arrested heart.6 7 When these and other experts first ...
A hypothalamic alpha-adrenergic mechanism mediating the thermogenic response to electrical stimulation of the lower brainstem...
Electrical stimulation of the lower brain stem (ESLB) at sites presumed to be parts of the ascending noradrenergic system was carried out in unanaesthetized young guinea pigs. At neutral ambient...
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Ergot alkaloid and alpha adrenergic receptor antagonist with vasoconstrictor effect which is less effective than ergotamine. Indicated in the treatment of acute migraine attack, usually together with caffeine. It is also used in orthostatic hypotension and prophylaxis of venous thromboembolism. Subcutaneous, intramuscular, intranasal or oral administration every half hour if necessary, up to a maximum of 2-3 mg per day. Since the last update we have not found published data on its excretion in breastmilk. Its moderately high molecular weight and high plasma protein binding and large volume of distribution (AEMPS 2014, FDA 2008) make it unlikely it will transfer into breastmilk in significant amounts. Its very low oral bioavailability (AEMPS 2014, FDA 2008) impedes its transfer from breastmilk to infant plasma, except in premature infants and the immediate neonatal period when there may be greater intestinal permeability. Like other ergot alkaloids, it can inhibit prolactin secretion
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BACKGROUND AND PURPOSE: In mouse tail arteries, selective alpha(2)-adrenoceptor antagonism with rauwolscine caused powerful dilation during constriction to the alpha(1)-adrenoceptor agonist phenylephrine. This study therefore assessed phenylephrines selectivity at vascular alpha-adrenoceptors and the mechanism(s) underlying dilation to rauwolscine. EXPERIMENTAL APPROACH: Mouse isolated tail arter
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Dan E. Berkowitz, David T. Price, Elizabeth A. Bello, Stella O. Page, Debra A. Schwinn; Localization of Messenger RNA for Three Distinct α2-Adrenergic Receptor Subtypes in Human Tissues: Evidence for Species Heterogeneity and Implications for Human Pharmacology. Anesthesiology 1994;81(5):1235-1244. Download citation file:. ...
In eleven dogs made hypotensive by means of rapid exsanguination over a period of forty to seventy minutes, mean glucagon rose to a peak of 516 ± (S.E.) 150 pg/ml. and mean glucose to a peak of 341 ± 27 mg. per 100 ml. The hyperglucagonemia induced by exsanguination was substantially reduced, although not abolished, by propranolol infusion, but was not diminished by phentolamine, suggesting that it was largely a β-adrenergic effect. Its possible contribution to survival during shock is considered.. ...
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes...
On the basis of extensive radioligand data and more limited functional data, three pharmacological subtypes of alpha 2-adrenergic receptors have been identified. More recently, three human genes or cDNAs for alpha 2-adrenergic receptors have been identified by molecular cloning. The relationship, however, among the pharmacologically defined subtypes and those identified by molecular cloning has not been clear. In order to resolve this issue, we have compared the pharmacological characteristics of the receptors identified by molecular cloning and expressed in COS-7 cells with the characteristics of the pharmacologically defined receptors in their respective prototypic tissue or cell line. The affinities (Ki values) of 12 subtype-selective alpha 2-adrenergic antagonists were determined for the alpha 2 receptor in the six preparations, by radioligand binding. Correlation analyses of the pKi values indicate that the alpha 2A subtype, as defined in the HT29 cell line, the alpha 2B receptor of the ...
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Cocaine increases production of the potent vasoconstrictor endothelin, and simultaneously decreases production of nitrous oxide, a powerful vasodilator. As a result of alpha-adrenergic stimulation, co... more
Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions
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Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait JH, Johnson MS, Larhammar D, Scheinin M (2004). „Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in zebrafish. Molecular Biology and Evolution. 21 (1): 14-28. PMID 12949138. doi:10.1093/molbev/msg224 ...
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van Brummelen P, Jie K, van Zwieten PA (1986). "Alpha-adrenergic receptors in human blood vessels". British Journal of Clinical ... In contrast to a hypertensive crisis, pheochromocytoma-associated MODS may not respond to traditional alpha-receptor agents and ... When catecholamines activate the alpha receptor, the vessel constricts (gets smaller), which results in hypertension. However, ... The newest PET modality involves somatostatin receptor type two receptor imaging with 68Ga-DOTA analogues. Over the last decade ...
Norepinephrine works by binding and activating alpha adrenergic receptors. Norepinephrine was discovered in 1946 and was ... Norepinephrine acts more on alpha receptors than the beta receptors. Norepinephrine is the INN while noradrenaline is the BAN. ... Norepinephrine acts on beta-1 adrenergic receptors, causing increase in heart rate and cardiac output. However, the elevation ... It stimulates α1 and α2 adrenergic receptors to cause blood vessel contraction, thus increases peripheral vascular resistance ...
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Alpha-2 adrenergic receptor agonistsEdit. Central alpha agonists lower blood pressure by stimulating alpha-receptors in the ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... These alpha 2 receptors are known as autoreceptors which provide a negative feedback in neurotransmission (in this case, the ... Endothelium receptor blockersEdit. Bosentan belongs to a new class of drug and works by blocking the receptors of the hormone ...
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"Renal alpha-1 and alpha-2 adrenergic receptors: Biochemical and pharmacological correlations". The Journal of Pharmacology and ... Elliott, J. (1997). "Alpha-adrenoceptors in equine digital veins: Evidence for the presence of both alpha1 and alpha2-receptors ... Sagrada, A; Fargeas, M J; Bueno, L (1987). "Involvement of alpha-1 and alpha-2 adrenoceptors in the postlaparotomy intestinal ... Woodman, OL; Vatner, SF (1987). "Coronary vasoconstriction mediated by alpha 1- and alpha 2-adrenoceptors in conscious dogs". ...
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Alpha α2 adrenergic receptors: Perhaps greater positive, negative, affective and cognitive symptom control. Histamine H1 ... Alpha α1 adrenergic receptors: This action accounts for its orthostatic hypotensive effects and perhaps some of the sedating ... Hecht EM, Landy DC (February 2012). "Alpha-2 receptor antagonist add-on therapy in the treatment of schizophrenia; a meta- ... Serotonin receptors: Its action at these receptors may be responsible for its lower extrapyramidal side effect liability (via ...
McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ... Osawa S, Dhanasekaran N, Woon CW, Johnson GL (Nov 1990). "G alpha i-G alpha s chimeras define the function of alpha chain ... "Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa". The Journal of Clinical ... GNAI2 has been shown to interact with: EYA2, GPSM2, Interleukin 8 receptor, alpha, MDFI, RGS5, and RIC8A. GRCh38: Ensembl ...
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Giovannitti JA, Thoms SM, Crawford JJ (2015-03-01). "Alpha-2 adrenergic receptor agonists: a review of current clinical ... specifically at the 5-HT1A and 5-HT1B G-protein coupled receptors. Additionally, the effect of MDMA on alpha-2 receptors is ... Neurochemically, MDMA activates 5-hydroxytryptamine, or 5-HT serotonin receptors, ...
ReceptorEdit. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). It belongs to the ... Azzolina A, Bongiovanni A, Lampiasi N (Dec 2003). "Substance P induces TNF-alpha and IL-6 production through NF kappa B in ... administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). ... "Absence of the SP/SP receptor circuitry in the substance P-precursor knockout mice or SP receptor, neurokinin (NK)1 knockout ...
Alfa-2 adrenergički receptor
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ... Elliott J (1997). "Alpha-adrenoceptors in equine digital veins: evidence for the presence of both α1 and α2-receptors mediating ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... norepinephrine due to lack of alpha-2 receptor negative feedback and decreased fat accumulation due to epinephrine/ ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ...
腎上腺素 - 維基百科，自由的百科全書
腎上腺素受體激動藥 (α（英語：Alpha-adrenergic agonist） ... Glutamate receptor antagonist（英語：Excitatory amino acid antagonist） (NMDA（英語：NMDA receptor antagonist）) ... Cannabinoid receptor antagonist（英語：Cannabinoid receptor antagonist）. *Endocannabinoid enhancer（英語：Endocannabinoid enhancer） ( ... 腎上腺素受體拮抗劑 (α（英語：Alpha blocker） (1
Integral membrane protein
G protein coupled receptors (e.g., Beta-adrenergic receptor). *Seipin. See alsoEdit. *Membrane protein ... The part of the protein that is embedded in the hydrophobic regions of the bilayer are alpha helical and composed of ... Insulin receptor. *Some types of cell adhesion proteins or cell adhesion molecules (CAMs) such as integrins, cadherins, NCAMs, ... This procedure has been extensively used for ligand-G protein-coupled receptors (GPCR) and their complexes. ...
... although there is evidence that it may have some alpha-1  and alpha-2 adrenoceptor antagonist activity. D1 receptor ... Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ...
February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT ... and dopamine D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B ... Yohimbine is an alpha-2 adrenergic antagonist, and has been used in a variety of research projects. It is a veterinary drug ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ...
Rauvolscin - Википедија, слободна енциклопедија
... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. ... receptor". Naunyn-Schmiedeberg's Archives of Pharmacology. 357 (1): 17-24. PMID 9459568. doi:10.1007/PL00005133.. ... Perry BD, U'Prichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): ... agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". ...
Cyclin-dependent kinase 4
Beta adrenergic receptor kinase (EC 188.8.131.52). *Beta adrenergic receptor kinase. *Beta adrenergic receptor kinase-2 ... Receptor protein serine/threonine kinase (EC 184.108.40.206). *Bone morphogenetic protein receptors *BMPR1 ... regulation of insulin receptor signaling pathway. • regulation of lipid biosynthetic process. • regulation of lipid catabolic ... Ribociclib are US FDA approved CDK4 and CDK6 inhibitors for the treatment of estrogen receptor positive/ HER2 negative advanced ...
σ receptors, IC50=145μM. Pharmacokinetics. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... σ1 receptor and D3 receptor agonist. It produces antidepressant-like effects in rats. However, captodiamine is unique ... enhances hypothalamic BDNF expression in vivo by synergistic 5-HT2c receptor antagonism and sigma-1 receptor agonism". J. ...
General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... antifungal, alkalinizing agents, quinolones, antibiotics, cholinergics, anticholinergics, antispasmodics, 5-alpha reductase ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... N,alpha-Diethylphenylethylamine. *N-Ethylbuphedrone. *N-Ethylhexedrone. *N,N-Dimethylphenethylamine. *Naphthylamphetamine. * ...
alpha-Ergosine *IUPAC name: Ergotaman-3',6',18-trione, 12'-hydroxy-2'-methyl-5'-(2-methylpropyl)-, (5'-alpha)- ... Drugs such as bromocriptine interact with the dopaminergic receptor sites as agonists with selectivity for D2 receptors, making ... alpha-Ergocryptine. CH(CH3)2. CH2CH(CH3)2. Leucine ... Adrenergic receptor modulators. α1. *Agonists: 6-FNE. * ... These substances are neuroleptic and are either an antagonist of dopamine at the postsynaptic level at the D2 receptor site or ...
5-Alpha-reductase inhibitor. *Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ...
Meta-[I-131]iodobenzylguanidine is a radio-labeled analog of the adrenergic blocking agent guanethidine. Radioactivity is ... alpha emitters. *223Ra (Radium chloride). beta emitters. *32P. *89Sr ... See also: Receptor/signaling modulators. Retrieved from "https://en.wikipedia.org/w/index.php?title=Iodine-131&oldid=1011894954 ...
For nocturnal symptoms, intranasal corticosteroids can be combined with nightly oxymetazoline, an adrenergic alpha-agonist, or ... Nasal steroids, antihistamines such as diphenhydramine, cromolyn sodium, leukotriene receptor antagonists such as montelukast, ... Other measures that may be used second line include: decongestants, cromolyn, leukotriene receptor antagonists, and ... and leukotriene receptor antagonists such as montelukast. Medications are, however, not sufficient or are associated with ...
... an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... Vasopressin receptor antagonists, such as conivaptan Acetazolamide, a carbonic anhydrase inhibitor Lithium was previously used ...
Serotonin-norepinephrine reuptake inhibitor
Assays have shown that selective NRIs have insignificant penchant for mACh, α1 and α2 adrenergic, or H1 receptors. ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... In addition, the TCAs interact with adrenergic receptors. This interaction seems to be critical for increased availability of ... Norepinephrine interacts with postsynaptic α and β adrenergic receptor subtypes and presynaptic α2 autoreceptors. The α2 ...
2,5-DMA is the alpha-methyl homologue of 2C-H and could be called "DOH" under the DO naming scheme. ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ...
Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and ... on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. ... adrenergic receptors), producing sympathomimetic effects. Some drugs, such as MDMA and derivatives may decrease regulatory ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors, however the implications for humans ...
Generalized anxiety disorder
Guanfacine - Sympatholytic, α2-adrenergic receptor agonist.. *Prazosin - Sympatholytic, alpha blocker.. Comorbidity. GAD ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... It is structurally similar to MDA, but without the methyl group at the alpha position. ...
... causing excessive stimulation of adrenergic receptors, which results in peripheral vasoconstriction and cardiac stimulation. ... 17 alpha-hydroxylase deficiency causes an inability to produce cortisol. Instead, extremely high levels of the precursor ... Schäfer SG, Kaan EC, Christen MO, Löw-Kröger A, Mest HJ, Molderings GJ (July 1995). "Why imidazoline receptor modulator in the ... Drugs: In particular, alcohol, nasal decongestants with adrenergic effects, NSAIDs, MAOIs, adrenoceptor stimulants, and ...
See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ...
Racemic adrenaline works by stimulation of the alpha adrenergic receptors in the airway, with resultant mucosal ... Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine is a nonselective agonist of all adrenergic ... Epinephrine's binding to these receptors triggers a number of metabolic changes. Binding to α-adrenergic receptors inhibits ... Its actions vary by tissue type and tissue expression of adrenergic receptors. For example, high levels of epinephrine causes ...
5-HT4受體 - 维基百科，自由的百科全书
α1（英语：Alpha-1 adrenergic receptor） (A, B, D) · α2（英语：Alpha-2 adrenergic receptor） (A, B, C) · β1 · β2 · β3 ... 腺苷酸（英语：Adenosine receptor） (A1, A2A, A2B, A3) · P2Y（英语：P2Y receptor） (1（英语：P2RY1）, 2（英语：P2RY2）, 4（英语：P2RY4）, 5（英语：LPAR6）, 6（英语： ... 乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺（英语：Dopamine receptor） (D1, D2, D3, D4, D5) · 组织胺（英语：Histamine receptor） (H1, H2, H3, H4) · 褪黑素（ ... 英语：Melatonin receptor） (1A, 1B, 1C) · 痕量胺相关受体 (1（英语：TAAR1）, 2（英语：TAAR2）, 3（英语：TAAR3）,
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Recombinant activated protein C (drotrecogin alpha) was originally introduced for severe sepsis (as identified by a high APACHE ... the toll-like receptors, the C-type lectin receptors, the NOD-like receptors, and the RIG-I-like receptors. Invariably, the ... This forced receptor interaction induces the production of pro-inflammatory chemical signals (cytokines) by T-cells. ...
See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ...
Alpha-2B adrenergic receptor - Wikipedia
"Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...
Alpha-1D adrenergic receptor - Wikipedia
The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... Receptor. There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 ...
Alpha-1A adrenergic receptor - Wikipedia
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 ... a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype". J. Pharmacol. Exp. Ther. 274 (1): ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
Myocardial alpha 1-adrenergic receptor stimulation. | Circulation
alpha-1 adrenergic receptor Protein Superfamily Detail
Alpha-2B adrenergic receptor - Wikipedia
The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... ReceptorEdit. α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical ... adrenergic receptor activity. • protein binding. • alpha2-adrenergic receptor activity. Cellular component. • integral ...
Familial Dysautonomia Medication: Benzodiazepines, H2 receptor antagonists, Alpha-adrenergic agonists, Corticosteroids
Alpha-adrenergic agonists. Class Summary. These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory ... A central alpha-adrenergic agonist that suppresses peripheral release of norepinephrine, resulting in lower blood pressure; ... H2 receptor antagonists. Class Summary. These agents are reversible competitive blockers of histamine at the H2 receptors, ... A pure peripheral alpha-adrenergic agonist, which causes peripheral vasoconstriction and raises blood pressure without ...
Insulin Downregulates Alpha-2 Adrenergic Receptors in Cultured Glial Cells | SpringerLink
Richards E.M., Raizada M.K., Sumners C. (1987) Insulin Downregulates Alpha-2 Adrenergic Receptors in Cultured Glial Cells. In: ... Using [3H]-yohimbine as a ligand for α2-adrenergic receptors, we have demonstrated that insulin is able to decrease [3H]- ... These results suggest that insulin, by modulating α2adrenergic receptor levels, is able to regulate the amount of NE present in ... Neuronal and glial cells in culture contain a2-adrenergic receptors, in preparation.Google Scholar ...
alpha 1 Adrenergic Receptor peptide (ab41797) | Abcam
Buy our alpha 1 Adrenergic Receptor peptide. Ab41797 is a blocking peptide for ab3462 and has been validated in Neut, BL. Abcam ... alpha 1 Adrenergic Receptor peptide. See all alpha 1 Adrenergic Receptor proteins and peptides. ... This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium. ... Belongs to the G-protein coupled receptor 1 family. Adrenergic receptor subfamily. ADRA1D sub-subfamily. ...
Alpha-2A adrenergic receptor - DrugBank
Alpha-2B adrenergic receptor - DrugBank
Alpha-2BAR. Gene Name. ADRA2B. Organism. Human. Amino acid sequence. ,lcl,BSEQ0010396,Alpha-2B adrenergic receptor ... Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins ... lcl,BSEQ0010397,Alpha-2B adrenergic receptor (ADRA2B) ATGGACCACCAGGACCCCTACTCCGTGCAGGCCACAGCGGCCATAGCGGCGGCCATCACC ... blood coagulation / activation of MAPK activity by adrenergic receptor signaling pathway / activation of protein kinase B ...
Anti-alpha 1b Adrenergic Receptor antibody (ab15851) | Abcam
Chicken polyclonal alpha 1b Adrenergic Receptor antibody validated for WB and tested in Human. Referenced in 1 publication. ... Anti-alpha 1b Adrenergic Receptor antibody. See all alpha 1b Adrenergic Receptor primary antibodies. ... This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium ... Ten commercial antibodies for alpha-1-adrenergic receptor subtypes are nonspecific.. Naunyn Schmiedebergs Arch Pharmacol 379: ...
ADRA2A - Alpha-2A adrenergic receptor - Homo sapiens (Human) - ADRA2A gene & protein
The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > ... Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins ... alpha-1B adrenergic receptor binding Source: BHF-UCL. *alpha-2C adrenergic receptor binding Source: BHF-UCLInferred from ... alpha-1B adrenergic receptor binding Source: BHF-UCL. *alpha2-adrenergic receptor activity Source: BHF-UCL ,p>Inferred from ...
ADRA2C - Adrenergic, alpha-2C-, receptor - Homo sapiens (Human) - ADRA2C gene & protein
Adrenergic, alpha-2C-, receptorImported. ,p>Information which has been imported from another database using automatic ... tr,Q4W594,Q4W594_HUMAN Adrenergic, alpha-2C-, receptor OS=Homo sapiens OX=9606 GN=ADRA2C PE=2 SV=1 ... G-protein coupled receptorUniRule annotation. ,p>Information which has been generated by the UniProtKB automatic annotation ... Belongs to the G-protein coupled receptor 1 family.UniRule annotation. Automatic assertion according to rulesi ...
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. - PubMed - NCBI
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in ... rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. ...
Postsynaptic localization of alpha 2-adrenergic receptors in rat submandibular gland | Journal of Neuroscience
3) Surgical denervation resulted in the appearance of high levels of alpha 2-adrenergic receptors. (4) The changes in alpha 2 ... Postsynaptic localization of alpha 2-adrenergic receptors in rat submandibular gland Message Subject (Your Name) has forwarded ... Postsynaptic localization of alpha 2-adrenergic receptors in rat submandibular gland. DB Bylund and JR Martinez ... alpha 2-Adrenergic receptors (as determined by [3H]clonidine binding) appear in rat submandibular gland membranes following ...
Produktübersicht alpha 1 Adrenergic Receptor ELISA
alpha 1 Adrenergic Receptor ELISA Kits vergleichen und bestellen. ... alpha 1 Adrenergic Receptor ELISA Kits für viele Reaktivitäten ... alpha-1C adrenergic receptor , adrenergic alpha 1c receptor , adrenergic receptor alpha 1c subtype , adrenergic receptor, alpha ... adrenergic, alpha-1A-, receptor variant 5 , adrenergic, alpha-1A-, receptor variant 8 , alpha-1A adrenergic receptor , alpha-1A ... alpha 1C-adrenergic receptor , alpha 1a-adrenoceptor , alpha-1A-adrenergic receptor , adrenergic receptor alpha-1A ...
Selective modification of renal alpha 2-adrenergic receptors in Milan hypertensive rat strain. | Hypertension
In the cerebral cortex, no between-strain differences in alpha 1-adrenergic and alpha 2-adrenergic receptor density and ... Cerebral and renal alpha-adrenergic receptors play an important role in the control of blood pressure. We studied alpha- ... Binding of the selective alpha 1-adrenergic antagonist [3H]prazosin and the alpha 2-adrenergic antagonist [3H]rauwolscine was ... Selective modification of renal alpha 2-adrenergic receptors in Milan hypertensive rat strain.. A Parini, L Diop, P Ferrari, G ...
beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system | Science
beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system ... beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system ... beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system ... beta-Adrenergic regulation of alpha 2-adrenergic receptors in the central nervous system ...
alpha 1b Adrenergic Receptor Proteins
Order alpha 1b Adrenergic Receptor Proteins from many different species. Find the right product on antibodies-online.com. ... alpha-1B-adrenergic receptor , Adrenergic alpha 1B- receptor , adrenergic receptor, alpha 1b , alpha 1B-adrenoceptor , alpha 1B ... alpha-1B adrenoceptor , adrenergic, alpha-1B-, receptor , alpha-1B adrenergic receptor-like , alpha-1B adrenergic receptor , ... alpha 1b Adrenergic Receptor (ADRA1B) Protein Überblick Protein Überblick Alpha-1-adrenergic receptors (alpha-1-ARs) are ...
Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats. |...
The down regulation of alpha 2-adrenergic receptors and the up regulation of alpha 1-adrenergic receptors are compatible with ... larger up regulation of alpha 1-adrenergic receptors, and greater down regulation of alpha 2-adrenergic receptors than did the ... Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats.. C R ... Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats. ...
Alpha-2B adrenergic receptor | definition of alpha-2B adrenergic receptor by Medical dictionary
... alpha-2B adrenergic receptor explanation free. What is alpha-2B adrenergic receptor? Meaning of alpha-2B adrenergic receptor ... Looking for online definition of alpha-2B adrenergic receptor in the Medical Dictionary? ... redirected from alpha-2B adrenergic receptor) ADRA2B. A gene on chromosome 2p13-q13 that encodes alpha-2B-adrenergic receptor, ... Alpha-2B adrenergic receptor , definition of alpha-2B adrenergic receptor by Medical dictionary https://medical-dictionary. ...
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/ ... 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] ... Adrenergic alpha-Agonists / pharmacokinetics*. Blood Platelets / metabolism*. Cell Membrane / metabolism. Chromatography, Thin ... 6147954 - Adrenergic nerves and the alpha 2-adrenoceptor system regulating melanosome aggregation.... 14557414 - Prevention of ...
Product Overview anti-alpha 1b Adrenergic Receptor Antibodies
Selected quality suppliers for anti-alpha 1b Adrenergic Receptor antibodies. ... Order monoclonal and polyclonal alpha 1b Adrenergic Receptor antibodies for many applications. ... alpha-1B-adrenergic receptor , Adrenergic alpha 1B- receptor , adrenergic receptor, alpha 1b , alpha 1B-adrenoceptor , alpha 1B ... alpha-1B adrenoceptor , adrenergic, alpha-1B-, receptor , alpha-1B adrenergic receptor-like , alpha-1B adrenergic receptor , ...
Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human...
The second alpha 1-adrenergic receptor cloned represents the rat homolog of the hamster alpha 1B subtype. Expression of mRNA ... We have now cloned two alpha 1-adrenergic receptors from a rat cerebral cortex cDNA library, using the hamster alpha 1B- ... Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human ... The primary structure though most closely resembles that of an alpha 1-adrenergic receptor, having approximately 73% amino acid ...
Platelet alpha 2-adrenergic receptors in hypercholesterolemia: relationship between binding studies and epinephrine-induced...
Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with plasma total and ... Conclusion: Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with ... Platelet alpha 2-adrenergic receptors in hypercholesterolemia: relationship between binding studies and epinephrine-induced ... A statistically significantly higher alpha 2-adrenergic receptor density was observed in a subgroup of 13 patients with ...
Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia. | Journal of Pharmacology and Experimental Therapeutics
Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia.. I Angel, R Niddam and S Z Langer ... Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia.. I Angel, R Niddam and S Z Langer ... Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia.. I Angel, R Niddam and S Z Langer ... Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia. Message Subject (Your Name) has forwarded a page to you ...
RCSB PDB - 1HOD: NMR STRUCTURE OF D130I MUTANT T3-I2, A 32 RESIDUE PEPTIDE FROM THE ALPHA 2A ADRENERGIC RECEPTOR...
NMR structure of the second intracellular loop of the alpha 2A adrenergic receptor: evidence for a novel cytoplasmic helix. ... alpha-2a adrenergic receptor pepride t3-i2 alpha-2a adrenergic receptor pepride t3-i2 alpha-2a adrenergic receptor pepride t3- ... NMR STRUCTURE OF D130I MUTANT T3-I2, A 32 RESIDUE PEPTIDE FROM THE ALPHA 2A ADRENERGIC RECEPTOR. ...
anti-alpha 2c Adrenergic Receptor antibody | GeneTex
... adrenergic, alpha-2C-, receptor) for IHC-P. Anti-alpha 2c Adrenergic Receptor pAb (GTX71833) is tested in Human samples. 100% ... adrenergic, alpha-2C-, receptor. Background. The Alpha 2c- Adrenergic Receptor controls the release of neurotransmitter from ... alpha 2c Adrenergic Receptor antibody See all alpha 2c Adrenergic Receptor products ... Storage Conditions: alpha 2c Adrenergic Receptor antibody. Storage Buffer. Phosphate buffered saline, pH 7.4 containing 0.01% ...
AntagonistAgonistAntibodyBeta-adrenergicAdrenoceptorPathwaysADRA1AAdrenoreceptorCatecholaminesNorepinephrineAffinityYohimbineMediatesPrazosinPharmacologyNeuronsStimulationEpinephrineRegulationSmooth muscle contractionPeptideSubtypes increase inhibitionADRA1BAlpha1BAntibodiesCharacterizationMolecularAdenylate cyclaseCoding sequenceCardiacPolyclonalBlockadeProteinLigandADRA2BMembranesContractionClonidineGene encodesGenesHumanMetabolismPresynaptic alpha 2 receptorsMediateBlockersPlatelet AggregationLocalizationALPHA1Subtype selectiveDrugsDensity
- 3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. (nih.gov)
- 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in bovine cerebral cortex. (nih.gov)
- Binding of the selective alpha 1-adrenergic antagonist [3H]prazosin and the alpha 2-adrenergic antagonist [3H]rauwolscine was used for receptor studies in tissues of prehypertensive (24-day-old) and hypertensive (60-day-old) rats. (ahajournals.org)
- Compared with their age-matched normotensive controls, MHS rats showed 1) a lower affinity for the antagonist (p less than 0.05) in the prehypertensive period, 2) absence of the normal age-related increase in receptor density, and 3) a lower density of [3H]rauwolscine binding sites (p less than 0.001) in the hypertensive period. (ahajournals.org)
- The effects are rapid and reversible, show a parallel time course, and are blocked by sotalol, a beta-adrenergic receptor antagonist. (sciencemag.org)
- This effect was blocked by co-injection of the alpha-2-receptor antagonist, yohimbine, demonstrating that the alpha-2-receptor is related to stimulation of feeding in layer-type chicks. (biomedsearch.com)
- 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] bromoxidine (UK14,304), which represented approximately 40% of the sites bound by the antagonist [3H]yohimbine. (biomedsearch.com)
- High affinity for the antagonist WB4101 and agonists phenylephrine and methoxamine suggests that cDNA RA42 encodes the alpha 1A receptor subtype. (nih.gov)
- Both the effect on glycemic level and the inhibition of insulin release by oxymetazoline were antagonized by the alpha-2 adrenoceptor antagonist idazoxan. (aspetjournals.org)
- The concentration-effect curve for UK and NE was shifted to the right by the alpha 2-antagonist yohimbine (10(-6) M), with new EC50 of 49.7 +/- 12.2 (p less than 0.001) nM and 10.3 +/- 22 nM. (jimmunol.org)
- The presence of a MO alpha-adrenergic receptor was established by demonstrating binding of the alpha 2-adrenergic antagonist 3H-yohimbine to membranes prepared from MO. (jimmunol.org)
- By using [3H]rauwolscine, a selective alpha 2-adrenergic receptor antagonist, we have identified for the first time alpha 2-adrenergic receptor sites in a mammalian pineal gland. (aspetjournals.org)
- The epinephrine response was mediated by alpha 1 adrenergic receptors based on the greater potency of the alpha 1 adrenergic selective antagonist prazosin compared to that of the alpha 2 adrenergic selective antagonist yohimbine. (arvojournals.org)
- adrenergic receptor antagonist, wherein the imidazoline .alpha. (patentgenius.com)
- These phorbol ester-treated cells also displayed a decrease in binding affinity of cellular alpha 1 receptors for agonists with no change in antagonist affinity. (duke.edu)
- Importance of Alpha - adrenergic Receptor Subtypes in Regulating of Airways Tonus at Patients with Bronchial Asthma In this work, effect of Tamsulosin hydrochloride as antagonist of alpha1A and alpha1B- adrenergic receptor and effect of Salbutamol as agonist of beta2- adrenergic receptor in patients with bronchial asthma and increased bronchial reactibility was studied.Parameters of the lung function are determined by Body plethysmography. (tripdatabase.com)
- Interestingly, β2- adrenergic receptor (β2-AR) antagonist ICI 118551 attenuated ischemia-induced BBB damage by regulating HIF-1α expression. (tripdatabase.com)
- The antagonist response profile for the paw-pinch test of the affected paw most closely approximated the α 2B receptor binding profile. (thejns.org)
- The antagonist profile from the current study is most consistent with the theory that the α 2B -adrenergic receptor subtype mediates the analgesic effect of intrathecally administered tizanidine on CCI-associated neuropathic pain. (thejns.org)
- The binding properties of two alpha-adrenergic radioligands, [3H]epinephrine (an agonist) and [3H]dihydroergocryptine (an antagonist), were compared in two model systems--membranes derived from human platelets and membranes from rat liver. (meta.org)
- Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan) drug for VHL disease. (nature.com)
- This review analyzed the outcome of alpha adrenergic antagonist in children with ureteral calculi. (scielo.br)
- 23. A pharmaceutical composition comprising a somatostatin receptor antagonist and a pharmaceutically acceptable liver targeting substance. (freepatentsonline.com)
- 24. The pharmaceutical composition according to claim 23, wherein the somatostatin receptor antagonist is cyclosomatostatin. (freepatentsonline.com)
- In the mouse bleomycin model of right ventricular failure, the alpha1A -adrenergic receptor subtype agonist A61603 prevents right ventricular failure. (antikoerper-online.de)
- Incubation of rat cerebral cortical slices with the beta-adrenergic agonist isoproterenol causes an increase in alpha 2-adrenergic receptor binding in addition to a decrease in beta-adrenergic receptor binding. (sciencemag.org)
- alpha 2 Agonist binding (p-amino-clonidine) declined in both hypothalamus and brain stem, and the fall was greater in hypertensive than in normotensive rats. (ahajournals.org)
- The down regulation of alpha 2-adrenergic receptors and the up regulation of alpha 1-adrenergic receptors are compatible with increased alpha 2-adrenergic agonist presynaptic inhibition of catecholamine release with resultant postsynaptic alpha 1-adrenergic receptor supersensitivity. (ahajournals.org)
- Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. (biomedsearch.com)
- p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor. (biomedsearch.com)
- The alpha-2A preferential agonist oxymetazoline induced in the mouse a hyperglycemic response similar to that of the nonselective alpha-2 adrenoceptor agonist UK 14.304. (aspetjournals.org)
- Dexmedetomidine is an alpha-2 adrenergic receptor agonist (A2ARA) used for sedation and analgesia, and as an adjunct in anesthesia to reduce anesthetic requirements in procedures requiring total intravenous anesthesia (TIVA) (1,2,3). (thefreedictionary.com)
- Carlos G. Musso and Jose Alfie, "Resistant Hypertension in the Elderly-Second Line Treatments: Aldosterone Antagonists, Central Alpha-Agonist Agents, Alpha-Adrenergic Receptor Blockers, Direct Vasodilators, and Exogenous Nitric Oxide Donors", Cardiovascular & Hematological Agents in Medicinal Chemistry (2014) 12: 170. (eurekaselect.com)
- Effects of combined use of alpha-2 adrenergic agonist, clonidine (150mug/kg), were also examined. (nii.ac.jp)
- Modification of anestnetic actions by α_2 receptor agonist, clonidine,in the rat. (nii.ac.jp)
- Flucatisone is a corticosteroid and salmeterol is a selective long-acting beta-2 adrenergic receptor agonist. (thefreedictionary.com)
- Thus, in liver membranes the endogenous 'physiological' agonist may not label the physiologically relevant alpha 1 receptors in typical radioligand binding assays using low concentrations of [3H]epinephrine. (meta.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)
- The alpha 2 adrenergic receptor agonist may have a vitreal half-life greater than about three hours. (justia.com)
- Brimonidine, 5-bromo-6-(2-imidazolidinylideneamino)quinoxaline, is an alpha-2-selective adrenergic receptor agonist that is effective in the treatment of open-angle glaucoma by decreasing aqueous humor production and increasing uveoscleral outflow. (justia.com)
- Hasegawa, M & Townley, R 1982, ' Effect of fenoterol (beta-2 agonist) on human lymphocytes alpha adrenergic receptor density ', Journal of Allergy and Clinical Immunology , vol. 69, no. 1 II. (elsevier.com)
- You need info about Human Anti-alpha 1 adrenergic receptor IgG antibody (ADRA1-Ab-IgG) ELISA Kit or any other Gentaur produtct? (gentaurshop.com)
- Western Blot: alpha-2C Adrenergic R/ADRA2C Antibody (S330A-51) [NBP2-59377] - Analysis of Rat Brain Membrane showing detection of ~100 kDa Alpha 2C Adrenergic. (novusbio.com)
- Immunocytochemistry/ Immunofluorescence: alpha-2C Adrenergic R/ADRA2C Antibody (S330A-51) [NBP2-59377] - Tissue: Neuroblastoma cell line SK-N-BE. (novusbio.com)
- Immunohistochemistry-Paraffin: alpha-1B Adrenergic R/ADRA1B Antibody [NLS698] - Anti-ADRA1B antibody IHC of human Ovary, Carcinoma. (novusbio.com)
- Immunohistochemistry-Paraffin: alpha-1B Adrenergic R/ADRA1B Antibody [NLS698] - Analysis of anti-ADRA1B antibody with human breast, carcinoma. (novusbio.com)
- 4) The changes in alpha 2 receptors paralleled the changes in postsynaptic beta-adrenergic receptor binding (as determined by [3H]dihydroalprenolol). (jneurosci.org)
- It is interesting to note that the ligand binding activity is lost on treatment with most common detergents like Triton X-100 or sodium cholate, but not digitonin, and that [beta] adrenergic receptors as well as rhodopsin and muscarinic receptors were also found to be solubilized in their active forms only with digitonin (14) when these three proteins were not thought to belong to the same family. (thefreedictionary.com)
- 5) At that time, it was shown that aerobic exercisers had greater alpha-adrenergic receptor density and significantly lower beta-adrenergic receptor density than weight trainers. (freethesaurus.com)
- The number of beta-adrenergic receptors is reduced, usually with preservation of alpha-adrenergic receptors and circulating catecholamines, causing beta/alpha-adrenergic imbalance, diastolic hypertension, reduced total blood volume, and other manifestations (3). (freethesaurus.com)
- Exercise-induced pulmonary vasoconstriction during combined blockade of nitric oxide synthase and beta adrenergic receptors. (jci.org)
- We studied the effects of inhibition of nitric oxide (NO) (endothelium-derived relaxation factor) synthase in combination with alpha and beta adrenergic receptor blockade on pulmonary vascular tone during exercise. (jci.org)
- During exercise in sheep there appears to be a high degree of alpha and beta adrenergic-mediated tone in the pulmonary circulation. (jci.org)
- Characterization of a potentially reversible increase in beta-adrenergic receptors in isolated, neonatal rat cardiac myocytes with impaired energy metabolism. (semanticscholar.org)
- Rapid recovery of cardiac beta-adrenergic receptors after isoproterenol-induced 'down'-regulation. (semanticscholar.org)
- Characterization of beta-adrenergic receptors in rat brain and pituitary using a new high-affinity ligand, [125I]iodocyanopindolol. (semanticscholar.org)
- Relationship between beta-adrenergic receptor numbers and physiological responses during experimental canine myocardial ischemia. (semanticscholar.org)
- A biochemical study of receptor internalization during beta-adrenergic receptor desensitization in frog erythrocytes. (semanticscholar.org)
- Beta adrenergic and muscarinic cholinergic receptors in canine myocardium. (semanticscholar.org)
- Alpha- and beta-adrenergic receptor polymorphisms in hypertensive and normotensive offspring. (cdc.gov)
- The present study aimed to verify whether these differences are associated with a different genotype distribution of functionally relevant polymorphisms of the alpha- and beta-adrenergic receptor (AR) genes. (cdc.gov)
- The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. (wikipedia.org)
- Auf www.antikoerper-online.de finden Sie aktuell 44 Adrenoceptor alpha 1A (ADRA1A) ELISA Kits von 10 unterschiedlichen Herstellern. (antikoerper-online.de)
- Alpha-2 adrenoceptor stimulation induces in the mouse a hyperglycemic response which is accompanied by a concomitant inhibition of insulin secretion. (aspetjournals.org)
- To test the possibility that one of the postulated subtypes of alpha-2 adrenoceptors is preferentially implicated in this response, we compared the interaction of several drugs with known selectivity toward alpha-2A or alpha-2B adrenoceptor subtypes in our model. (aspetjournals.org)
- The alpha-2B preferential antagonists ARC-239, prazosin or chlorpromazine failed to block the modifications in both glycemic and insulin levels induced by alpha-2 adrenoceptor stimulation. (aspetjournals.org)
- Alpha 2c-Adrenoceptor has been reported extensively in the brain. (genetex.com)
- Also known as Alpha-1B adrenergic receptor (Alpha-1B adrenoreceptor) (Alpha-1B adrenoceptor). (mybiosource.com)
- Chez www.anticorps-enligne.fr sont 7 Adrenoceptor alpha 1A (ADRA1A) Protéines de 4 de différents fournisseurs disponibles. (anticorps-enligne.fr)
- Recent studies have suggested that brimonidine can promote survival of injured retinal ganglion nerve cells by activation of the alpha-2-adrenoceptor in the retina and/or optic nerve. (justia.com)
- The alpha-1b adrenoceptor is an Adrenergic Receptor that causes contraction of smooth muscle cells and thereby controls vascular tone, blood pressure, and accelerates the development of atherosclerosis. (novusbio.com)
- Decreased alpha-1b adrenoceptor is associated with benign prostatic hyperplasia (BPH). (novusbio.com)
- Adrenergic responsiveness is altered with aging and the age-related changes are limited to the β-adrenergic receptor density reduction and to the β-adrenoceptor-G-protein(s)-adenylyl cyclase system abnormalities, while the type and level of abnormalities change with species and tissues. (frontiersin.org)
- Likewise, the inhibition of norepinephrine reuptake (INR) in the axonic endings of the inhibitory noradrenergic descending pathways, increases the extracellular concentration of norepinephrine (NE) in the spinal cord, which can also produce anti-nociception by the activation of the [alpha]2 adrenergic receptors which can be of particular interest in chronic neuropathic pain. (thefreedictionary.com)
- Unfortunately, little information exists about the signaling pathways used by this important G protein-coupled receptor (GPCR). (pnas.org)
- Multiple second messenger pathways of alpha-adrenergic receptor subtypes expressed in eukaryotic cells. (freethesaurus.com)
- The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it. (wikipedia.org)
- The alpha-1D adrenergic receptor (α 1D adrenoreceptor), also known as ADRA1D , is an alpha-1 adrenergic receptor , and also denotes the human gene encoding it. (wikipedia.org)
- We have studied the effect of long-term (72 hour) intravenous infusions of methyldopa to awake restrained spontaneously hypertensive rats and normotensive Wistar-Kyoto control animals to look for differences in hypotensive effect, differences in concentrations of natural and alpha-methylated catecholamines, and differences in alpha 1 and alpha 2-adrenergic receptor populations. (ahajournals.org)
- The role of beta and alpha adrenergic receptors in the lipolytic effect of catecholamines on dog adipocytes. (thefreedictionary.com)
- Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α 1 -adrenergic receptor in the central and peripheral nervous systems . (gutenberg.org)
- Adrenergic receptors activation by catecholamines is the most important regulatory mechanism of cardiovascular performance. (frontiersin.org)
- F. T. Boyd, Jr., D. W. Clarke, T. F. Muther, and M. K. Raizada, Insulin receptors and modulation of norepinephrine uptake by insulin in neuronal cells in culture, J. Biol. (springer.com)
- Norepinephrine is known to inhibit its own release from presynaptic nerve terminals through alpha 2-adrenergic receptors, which presumably have a presynaptic localization. (jneurosci.org)
- The beta-mediated regulation of alpha 2-receptor sensitivity at brain norepinephrine synapses may be a mechanism for the homeostatic control of central noradrenergic activity. (sciencemag.org)
- In our study we have determined that UK-14304 (UK) and norepinephrine (NE), both alpha 2-adrenergic agonists, can augment LPS-stimulated TNF from elicited macrophages (MO). (jimmunol.org)
- The functional status of these alpha-1 adrenergic receptors was also assessed by measuring the norepinephrine-induced accumulation of inositol phosphates in myometrial tissue. (aspetjournals.org)
- Incubation of these cells with tumor-promoting phorbol esters, which stimulate calcium- and phospholipid-dependent protein kinase, leads to a marked attenuation of the ability of alpha 1-receptor agonists such as norepinephrine to stimulate the turnover of inositol phospholipids. (duke.edu)
- The effect of phorbol esters on norepinephrine-stimulated inositol phospholipid turnover and alpha 1-receptor phosphorylation showed the same rapid time course with a t1/2 less than 2 min. (duke.edu)
- At adrenergic neurons they play important role as auto inhibitory feedback mechanisms controlling norepinephrine release. (egpat.com)
- Clonidine activates α receptors, which causes inhibition of norepinephrine release from synaptic vesicles. (picmonic.com)
- In particular, norepinephrine decreases glutamatergic excitatory postsynaptic potentials by the activation of α 1 -adrenergic receptors. (gutenberg.org)
- Adrenergic drugs have similar structures as the chemical messengers that your body produces during times of stress, such as epinephrine and norepinephrine. (healthline.com)
- Certain areas called adrenergic receptors receive the messages from epinephrine and norepinephrine that tell your body how to respond. (healthline.com)
- They can mimic epinephrine and norepinephrine and bind with the receptors, causing the fight or flight responses. (healthline.com)
- These drugs can also bind with the receptors to stimulate the release of epinephrine and norepinephrine. (healthline.com)
- These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in brain membranes. (nih.gov)
- In the cerebral cortex, no between-strain differences in alpha 1-adrenergic and alpha 2-adrenergic receptor density and affinity were observed in prehypertensive and hypertensive periods. (ahajournals.org)
- This study assessed whether platelet hyperreactivity to epinephrine in hypercholesterolemia is associated with higher alpha 2-adrenergic receptor density or affinity for epinephrine. (nih.gov)
- 0.03), but no difference was observed in receptor affinity for the ligand. (nih.gov)
- By using affinity chromatography on the affinity resin Affi-Gel-A55414, the alpha 1 receptors were purified approximately equal to 300-fold from control and phorbol ester-treated 32Pi-prelabeled cells. (duke.edu)
- Agonists induce the formation of a guanine nucleotide-sensitive high-affinity state of alpha 2 but not alpha 1 receptors. (meta.org)
- 3H]Dihydroergocryptine labels all the alpha receptors, whereas [3H]epinephrine at low concentrations labels predominantly the high-affinity form of the alpha 2 receptor in both platelet and liver. (meta.org)
-  The neurotransmitter noradrenaline has higher affinity for the α1 receptor than does adrenaline (which is a hormone). (gutenberg.org)
- Using [ 3 H]-yohimbine as a ligand for α 2 -adrenergic receptors, we have demonstrated that insulin is able to decrease [ 3 H]-yohimbine binding to glia in a time- and dose-dependent manner. (springer.com)
- The nonselective antagonists rauwolscine, yohimbine, WY 26703, phentolamine and corynanthine, as well as the receptor antagonists with alpha-2A selectivity like WB 4101, idazoxan and tolazoline, dose-dependently antagonized both the glycemic and the insulin responses to UK 14.304. (aspetjournals.org)
- Home / Test Division / Reference Database / 1990 to 1999 / 1990 / Platelet alpha-sub-2-adrenergic receptor binding to -3H-yohimbine and personality. (umn.edu)
- The results of the paw-pinch test on the affected side were compared with binding data cited in the existing literature for the three different α 2 -adrenergic receptor subtypes (α 2A , α 2B , and α 2C ) with yohimbine, prazosin, and WB4101. (thejns.org)
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium. (abcam.com)
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. (abcam.com)
- Î²2- Adrenergic Receptor-Mediated HIF-1Î± Upregulation Mediates Blood Brain Barrier Damage in Acute Cerebral Ischemia Disruption of the blood brain barrier (BBB) within the thrombolytic time window is an antecedent event to intracerebral hemorrhage in ischemic stroke. (tripdatabase.com)
- Intrathecally administered α 2 -adrenergic receptor subtype-specific antagonists were used to determine which α 2 -adrenergic receptor subtype mediates the analgesic effect of intrathecally administered tizanidine in a chronic constriction injury (CCI) rat model of neuropathic pain. (thejns.org)
- Activation of α 1 -adrenergic receptors produces anorexia and partially mediates the efficacy of appetite suppressants like phenylpropanolamine and amphetamine in the treatment of obesity . (gutenberg.org)
- alpha 1-Adrenergic receptor binding (prazosin) was increased, again more in hypertensive than in normotensive rats. (ahajournals.org)
- Alpha-1 adrenergic receptors were examined in both inner and outer layers of human pregnant myometrium using radioligand binding of [3H]prazosin. (aspetjournals.org)
- Adult male mongrel dogs were intravenously infused with 1) normal saline solution , 2) CaCl2 solution , 3) CaCl2 + calcium channel blocker ( verapamil ), 4) CaCl2 + selective alpha-1 adrenergic receptor blocker ( prazosin ), or 5) CaCl2 + verapamil + prazosin . (bvsalud.org)
- Analysis of the ligand binding properties of RA42 expressed in COS-7 cells with a variety of adrenergic ligands demonstrates a unique alpha 1-adrenergic receptor pharmacology. (nih.gov)
- In general, human alpha-1AR subtypes have similar pharmacology compared to their rat, hamster and bovine homologs, although a few minor species differences important for alpha-1AR classification are noted. (duke.edu)
- These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (wikipedia.org)
- A gene on chromosome 2p13-q13 that encodes alpha-2B-adrenergic receptor, a member of the G protein-coupled receptor superfamily, which plays a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the CNS, smooth muscle contraction and thermoregulation. (thefreedictionary.com)
- The Alpha 2c- Adrenergic Receptor controls the release of neurotransmitter from central adrenergic neurons and from sympathetic nerves in the heart. (genetex.com)
- This protein is a member of a subfamily of G protein-coupled receptors that regulate neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (nih.gov)
- Myocardial alpha 1-adrenergic receptor stimulation. (ahajournals.org)
- Stimulation of alpha-adrenergic receptor augments the production of macrophage-derived tumor necrosis factor. (jimmunol.org)
- In terms of pharmacologic effects, clonidine works by stimulation of alpha-2 adrenergic receptors in the brain. (thefreedictionary.com)
- Stimulation of P2U purinergic or alpha 1A adrenergic receptors mobilizes Ca2+ in lens cells. (arvojournals.org)
- DDT1 MF-2 cells, which are derived from hamster vas deferens smooth muscle, contain alpha 1-adrenergic receptors (54,800 +/- 2700 sites per cell) that are coupled to stimulation of inositol phospholipid metabolism. (duke.edu)
- alpha(1)-Adrenergic receptor activation caused phosphorylation of PLC-beta(1) but not PLC-beta(3), whereas stimulation by ATP induced phosphorylation of PLC-beta(3) but not PLC-beta(1. (garvan.org.au)
- The primary mechanism of action of alpha-2 agonists is stimulation of presynaptic alpha-2 receptors in the central nervous system. (picmonic.com)
- The majority of alpha-1 receptors are directed toward the function of epinephrine, a hormone that has to do with the fight-or-flight response. (wikipedia.org)
- In addition, the lack of any guanylylimidodiphosphate effect on the l-epinephrine competition curve observed in MHS rats suggests the uncoupling of these receptors from the guanosine 5'-triphosphate binding protein. (ahajournals.org)
- Platelet alpha 2-adrenergic receptor density is increased in hypercholesterolemia and directly correlates with plasma total and levels of LDL cholesterol, providing at least a partial explanation for the enhanced platelet response to epinephrine that is observed in hypercholesterolemia. (nih.gov)
- More specifically, the epinephrine response was mediated by the alpha 1A adrenergic receptor subtype based on the greater potencies exhibited by the alpha 1A subtype selective competitive antagonists WB 4101 and 5-methylurapidil compared to the alpha 1B and alpha 1D selective antagonists spiperone and BMY 7378, respectively. (arvojournals.org)
- CONCLUSIONS: Ca2+ is mobilized from intracellular stores in the sheep lens by ATP and epinephrine acting through P2U purinergic and the alpha 1A adrenergic receptors, respectively. (arvojournals.org)
- In the present study we have investigated this further by examining the actions of this peptide on the regulation of α 2 -adrenergic receptors in glial cells. (springer.com)
- The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer-type chicks. (biomedsearch.com)
- Regulation of angiotensin II receptors on ventricular myocytes after myocardial infarction in rats. (semanticscholar.org)
Smooth muscle contraction1
- α1-receptors primarily mediate smooth muscle contraction, but have important functions elsewhere as well. (gutenberg.org)
- Synthetic peptide, corresponding to amino acids 200-299 of Human alpha 1b Adrenergic Receptor. (abcam.com)
- METHODOLOGY/PRINCIPAL FINDINGS: Using a rat model we studied the long-term action of antibodies against the alpha(1)-adrenergig receptor either induced by immunization with a receptor peptide or applied by intravenous injection. (mdc-berlin.de)
- Gentaur Molecular :Neuromi \ Alpha 2a Adrenergic Receptor, control peptide, 50 ul. (antibody-antibodies.com)
- Product Detail : P14110 Alpha 2a Adrenergic Receptor, control peptide, 50 ul. (antibody-antibodies.com)
- We have also other products like : Alpha 2a Adrenergic Receptor, control peptide, 50 ul. (antibody-antibodies.com)
Subtypes increase inhibition2
- good selectivity over α1B, α1D and α2A subtypes further partial agonistic imidazole compounds A-61603 Metaraminol Tamsulosin: for treatment of benign prostatic hyperplasia Silodosin: for treatment of benign prostatic hyperplasia Doxazosin: for treatment of benign prostatic hyperplasia and/or Hypertension Risperidone WB-4101 Ziprasidone Most Tricyclic antidepressant α1A-adrenergic receptor subtypes increase inhibition at dendrodendritic synapses, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors. (wikipedia.org)
-  α1-adrenergic receptor subtypes increase inhibition in the olfactory system, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors. (gutenberg.org)
- Auf www.antikoerper-online.de finden Sie aktuell 4 Adrenergic, alpha-1B-, Receptor (ADRA1B) Proteine von 1 unterschiedlichen Herstellern. (antikoerper-online.de)
- 81 Adrenergic, alpha-1B-, Receptor (ADRA1B) Antibodies from 13 manufacturers are available on www.antibodies-online.com. (antibodies-online.com)
- protein kinase C modulates alpha1B-adrenergic receptor transfer to late endosomes and that Rab9 regulates this process and participates in G protein -mediated signaling turn-off. (antikoerper-online.de)
- Ten commercial antibodies for alpha-1-adrenergic receptor subtypes are nonspecific. (abcam.com)
- Antibodies directed predominantly against the alpha(1)-adrenergig receptor were detected in patients suffering from widespread diseases such as hypertension and type 2 diabetes. (mdc-berlin.de)
- We postulate that antibodies to the alpha(1)-adrenergig receptor are relevant pathomolecules in diseases of the central nervous system associated with vascular impairments. (mdc-berlin.de)
- CONCLUSION/SIGNIFICANCE: We present evidence that antibodies to the α(1)-adrenergig receptor cause cerebrovascular impairments in the rat. (mdc-berlin.de)
- Identification and characterization of alpha 2D-adrenergic receptors in bovine pineal gland. (aspetjournals.org)
- Pharmacological characterization was performed simultaneously using six cloned alpha-1AR subtypes (human and rat alpha-1a/d, human and hamster alpha-1b, human and bovine alpha-1c) stably expressed in rat-1 fibroblasts at approximately equal receptor concentrations (1-2 pmol/mg of total protein). (duke.edu)
- Pharmacological and molecular cloning studies have demonstrated heterogeneity of alpha 1-adrenergic receptors. (nih.gov)
- The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
- Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. (aspetjournals.org)
- More recently, three human genes or cDNAs for alpha 2-adrenergic receptors have been identified by molecular cloning. (aspetjournals.org)
- In order to resolve this issue, we have compared the pharmacological characteristics of the receptors identified by molecular cloning and expressed in COS-7 cells with the characteristics of the pharmacologically defined receptors in their respective prototypic tissue or cell line. (aspetjournals.org)
- Bruno JF, Whittaker J, Song JF, Berelowitz M: Molecular cloning and sequencing of a cDNA encoding a human alpha 1A adrenergic receptor. (drugbank.com)
- Dr. Simpson is highly respected in the field of molecular cardiology and internationally-recognized for his contributions to our understanding of cardiac hypertrophy and alpha-1-adrenergic receptor (AR) biology. (grantome.com)
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (drugbank.ca)
- Transgenic mice were generated by using the alpha-myosin heavy chain promoter coupled to the coding sequence of a constitutively active mutant alpha 1B-adrenergic receptor (AR). (duke.edu)
- α1-AR gain-of-function in cardiac transgenic models generally supports the KO results, although phenotypes vary greatly with receptor level, promoter, and absence or presence of an activating mutation. (pubmedcentralcanada.ca)
- Myocardial expression of a constitutively active alpha 1B-adrenergic receptor in transgenic mice induces cardiac hypertrophy. (duke.edu)
- These transgenic animals demonstrated cardiac-specific expression of this alpha 1-AR with resultant activation of phospholipase C as shown by increased myocardial diacylglycerol content. (duke.edu)
- Wright CD, Chen Q, Baye NL, Huang Y, Healy CL, Kasinathan S, O'Connell TD: Nuclear alpha1-adrenergic receptors signal activated ERK localization to caveolae in adult cardiac myocytes. (drugbank.com)
- Wright CD, Wu SC, Dahl EF, Sazama AJ, O'Connell TD: Nuclear localization drives alpha1-adrenergic receptor oligomerization and signaling in cardiac myocytes. (drugbank.com)
- Surprisingly, the function of the human cardiac alpha-1-AR subtypes is unknown, and alpha-1-ARs have never been studied in human heart cells. (grantome.com)
- Collectively these Aims will establish a broader understanding of human cardiac alpha-1-AR biology and the mechanisms of HF. (grantome.com)
- In particular it is well known that: (a) levels of cathecolamines are directly correlated with mortality and functional status in heart failure, (b) β 1 -adrenergic receptor subtype is down-regulated in heart failure, (c) heart failure-dependent cardiac adrenergic responsiveness reduction is related to changes in G proteins activity. (frontiersin.org)
- Rabbit Polyclonal to Adrenergic Receptor alpha-2A However, the pancytopenia gradually worsened, and protein anabolic steroids (metenolone, 20 mg/day time) were added to the treatment in 2009 2009. (bostonscienceandengineeringlectures.com)
- Rabbit Polyclonal to PKC alpha (phospho-Tyr657). (researchreportone.com)
- Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. (tripdatabase.com)
- The investigators intend to determine the effect of adrenergic blockade on 1) short-term physiology, behavior, and cognition and 2) long-term neuropsychological outcomes after severe Traumatic Brain Injury (TBI). (clinicaltrials.gov)
- The primary hypothesis is that adrenergic blockade after severe TBI will be associated with increased ventilator-free days. (clinicaltrials.gov)
- Blockade of these receptors in the bladder neck decreases outflow resistance. (medscape.com)
- In paired studies, we exercised sheep on a treadmill at a speed of 4 mph, and measured blood flow and pressures across the pulmonary circulation with and without inhibition of NO synthase (N omega-nitro-L-arginine 20 mg/kg intravenous [i.v.]), alpha receptor blockade (phentolamine 5 mg i.v.), beta receptor blockade (propranolol 1 mg i.v.), and combined alpha and beta receptor blockade. (jci.org)
- Belongs to the G-protein coupled receptor 1 family. (abcam.com)
- Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM, KD = 2.5 nM, Bmax = 160 fmol/mg protein) and competition studies indicated that [3H]rauwolscine labeled the alpha 2-receptor. (nih.gov)
- Zusätzlich bieten wir Ihnen alpha 1 Adrenergic Receptor Antikörper (92) und alpha 1 Adrenergic Receptor Proteine (7) und viele weitere Produktgruppen zu diesem Protein an. (antikoerper-online.de)
- The deduced amino acid sequence of clone RA42 encodes a protein of 560 amino acids whose putative topology is similar to that of the family of G-protein-coupled receptors. (nih.gov)
- A gene on chromosome 8p21.2 that encodes alpha-1A-adrenergic receptor, a member of the G protein-coupled receptor superfamily, which activates a phosphatidylinositol-calcium second messenger system, triggering mitogenic responses and regulating growth, proliferation and signalling through the Gq/11 family of G proteins. (thefreedictionary.com)
- Receptor subtypes within families of G protein-coupled receptors that are activated by similar ligands can regulate distinct intracellular effectors. (nih.gov)
- We identified conserved motifs within intracellular domains 2 and 3 of selective subtypes of several G protein-coupled receptor families that confer coupling to the Na-H exchanger, NHE1. (nih.gov)
- These findings indicate that motifs shared by different subfamilies of G protein-coupled receptors, but not necessarily by receptor subtypes within a subfamily, can confer coupling to a common effector. (nih.gov)
- 3H] Rauwolscine bound in a saturable manner to a single class of receptors, with an equilibrium dissociation constant (KD) of 1.4 nM and a density (Bmax) of 71 fmol/mg of protein, in crude synaptic membrane preparations from bovine pineal gland. (aspetjournals.org)
- BACKGROUND: Circulating agonistic autoantibodies acting at G protein-coupled receptors have been associated with numerous sever pathologies in humans. (mdc-berlin.de)
- Alpha-1B adrenergic receptor acts through G-protein beta/gamma of pertussis toxin-sensitive Alpha activating activity polypeptide O ( G-protein alpha-o ) [ 3 ], [ 5 ]. (bio-rad.com)
- These results indicate that calcium- and phospholipid-dependent protein kinase may play an important role in regulating the function of receptors that are coupled to the inositol phospholipid cycle by phosphorylating and deactivating them. (duke.edu)
- 100 µ g) The α -2-adrenergic receptor is a member of the G-protein coupled receptor superfamily. (allelebiotech.com)
- The α 1 receptors at GI smooth muscle are again G-protein coupled receptors but not coupled with IP3/DAG instead coupled with opening of potassium channels leading to hyperpolarisation. (egpat.com)
- α 2 adrenergic receptors are again G-protein coupled receptors coupled with inactivation of adenylyl cyclase. (egpat.com)
- Alpha-2-adrenergic receptors are members of the G protein-coupled receptor superfamily. (nih.gov)
- G protein-coupled receptors (GPCRs) are seven-transmembrane spanning proteins that are responsible for communicating information in the form of extracellular stimuli across lipid membranes into distinct intracellular signals with precise accuracy. (pnas.org)
- We have cloned cDNAs encoding three human alpha-1 adrenergic receptor (AR) subtypes and characterized pharmacological properties of the expressed receptor protein. (duke.edu)
- The alpha-1 ( α 1 ) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the G q heterotrimeric G-protein . (gutenberg.org)
- As assessed by NaDodSO4/polyacrylamide gel electrophoresis, the Mr 80,000 alpha 1-receptor ligand-binding subunit is a phosphopeptide containing 1.2 mol of phosphate per mol of alpha 1 receptor. (duke.edu)
- These GPCR interacting proteins (or GIPs) are largely receptor subtype and cell context specific, include both membrane and cytosolic proteins, and typically play a highly specific supporting role for GPCR function (i.e., trafficking, ligand binding, enhancing signaling, signal termination, and/or degradation) ( 2 - 4 ). (pnas.org)
- In spite of significant sequence differences between human alpha-1ARs and their other species counterparts, previously established ligand selectivity remains fairly comparable. (duke.edu)
- The human gene encoding this receptor has the symbol ADRA2B. (wikipedia.org)
- alpha 2-Adrenergic receptors (as determined by [3H]clonidine binding) appear in rat submandibular gland membranes following reserpine treatment. (jneurosci.org)
- 125I]PIC binds to the alpha 2B-AR in NG-10815 cell membranes with a Kd of 0.5 +/- 0.1 nM. (biomedsearch.com)
- Any of a group of receptors on cell membranes that are thought to be associated with vasoconstriction, relaxation of intestinal muscle, and contraction of the nictitating membrane, iris dilator muscle, smooth muscle of the spleen, and muscular layer of the uterine wall. (thefreedictionary.com)
- A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. (uchicago.edu)
- 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. (uchicago.edu)
- These drugs competitively inhibit the binding of acetylcholine to the muscarinic cholinergic receptor, thereby suppressing involuntary bladder contraction of any etiology. (medscape.com)
- It also induces contraction of the urinary bladder ,   although this effect is minor compared to the relaxing effect of β 2 -adrenergic receptors . (gutenberg.org)
- It is concluded that clonidine produces (or potentiates) analgesic effects of various drugs and that the analgesic effect of nitrous oxide is attributed to the effect on the central noradrenergic system, possibly by an activation of the descending inhibitory system and/or inhibition of the primary sensory afferent neuron via alpha-2 adrenergic receptors. (nii.ac.jp)
- This gene encodes alpha-1D-adrenergic receptor. (wikipedia.org)
- alpha1A -adrenergic receptors are stably expressed and stimulate cell migration and TGF-beta1 (zeige TGFB1 ELISA Kits ), IGF-1 (zeige IGF1 ELISA Kits ), hyaluronan and PIP (zeige PIP ELISA Kits ) production in human skin fibroblasts. (antikoerper-online.de)
- Alpha-1 adrenergic receptor: binding and phosphoinositide breakdown in human myometrium. (aspetjournals.org)
- These results indicate that alpha-1 adrenergic receptors in human myometrium at the end of pregnancy are linked to phosphoinositide hydrolysis and that this response occurs mainly in the outer layer. (aspetjournals.org)
- The bovine pineal alpha 2-adrenergic receptor appears to represent a pharmacological subtype distinct from the three currently proposed subtypes, i.e., alpha 2A found in a human colonic adenocarcinoma cell line (HT29 cell), alpha 2B found in rat lung, and alpha 2C found in an opossum kidney cell line (OK cell). (aspetjournals.org)
- Correlation analyses of the pKi values indicate that the alpha 2A subtype, as defined in the HT29 cell line, the alpha 2B receptor of the neonatal rat lung, and the alpha 2C subtype, as defined in an oppossum kidney cell line, correspond to the cloned human alpha 2-C10, alpha 2-C2, and alpha 2-C4 receptor subtypes, respectively. (aspetjournals.org)
- Ramarao CS, Denker JM, Perez DM, Gaivin RJ, Riek RP, Graham RM: Genomic organization and expression of the human alpha 1B-adrenergic receptor. (drugbank.com)
- the most major differences occur for the human alpha-1a/dAR. (duke.edu)
- In addition, much lower inactivation (approximately 20%) by the alkylating agent chloroethylclonidine is noted in this study compared to previous reports for both human and bovine alpha-1cAR membrane preparations. (duke.edu)
- All six alpha-1AR subtypes couple to phosphoinositide hydrolysis in a pertussis toxin-insensitive manner, including the cloned human alpha-1a/dAR which had not been expressed previously. (duke.edu)
- The research plan follows naturally from the applicant's recent novel work identifying the tissue distribution of the 3 alpha-1-AR subtypes in the human heart. (grantome.com)
- III) Identify the functional alpha-1-AR subtypes in human coronary smooth muscle and endothelial cells. (grantome.com)
- Abundant data from cell and animal studies show that alpha-1-adrenergic receptors (ARs) play beneficial roles in the heart and protect against heart failure (HF), but little is known about these receptors in the human heart. (grantome.com)
- The proposed work will expand significantly our knowledge of alpha-1-ARs in the human heart and is essential to the long-term aim of the project, which is the development of a novel therapy for HF targeting alpha-1-ARs. (grantome.com)
- These regional and strain differences in the metabolism of alpha-methyldopa suggest that the production of methylnorepinephrine in brain stem nuclei is most correlated with the hypotensive action of methyldopa. (ahajournals.org)
- Phorbol esters promote alpha 1-adrenergic receptor phosphorylation and receptor uncoupling from inositol phospholipid metabolism. (duke.edu)
Presynaptic alpha 2 receptors1
- While these results establish the existence of postsynaptic alpha 2-adrenergic receptors in an innervated tissue, the concomitant presence of a low density of presynaptic alpha 2 receptors has not been eliminated. (jneurosci.org)
- It is therefore likely that brain adrenergic alpha-2-receptors mediate the orexigenic effects of neuropeptide Y and beta-endorphin in layer-type chicks. (biomedsearch.com)
- During exercise, α 1 -adrenergic receptors in active muscles are attenuated in an exercise intensity-dependent manner, allowing the β 2 -adrenergic receptors which mediate vasodilation to dominate. (gutenberg.org)
- These agents are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells where they inhibit acid secretion. (medscape.com)
- An appropriate therapy for RH can be achieved by the addition of second line antihypertensive drugs: antialdosteronic diuretics, central agents, alpha blockers, direct vasodilating agents, and exogenous nitric oxide donors. (eurekaselect.com)
- However, literature about the use of alpha-1 adrenergic blockers in pediatric population with distal ureterolithiasis is still scarce. (scielo.br)
- This review has the objective to evaluate the use of alpha-1 adrenergic blockers as medical expulsive treatment in children with distal ureterolithiasis. (scielo.br)
- In the adult patient, there are various conservative treatments to treat calculi smaller than 12mm, such as the use of calcium blockers, non-steroidal anti-inflammatory agents, or alpha-1 adrenergic blockers, which is the better approach ( 9 ). (scielo.br)
- Among the most important and most widely used medications are thiazide diuretics , calcium channel blockers , ACE inhibitors , angiotensin II receptor antagonists (ARBs), and beta blockers . (rug.nl)
- In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACE inhibitors , or angiotensin II receptor antagonists . (rug.nl)
- The 8th Joint National Committee (JNC-8) recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with thiazide -type diuretics, ACE inhibitors , or angiotensin II receptor antagonists for all patients regardless of age or race. (rug.nl)
- In these subgroups plasma total and levels of low-density lipoprotein (LDL) cholesterol were inversely correlated with platelet aggregation but directly correlated with platelet receptor density. (nih.gov)
- PURPOSE: To examine the localization of a novel alpha 1-adrenergic receptor subtype of alpha 1C receptor in the eye, we compared the amount of alpha 1C receptor transcripts in bovine retinal pigment epithelium (RPE) and in neural retina by employing reverse transcription of mRNA and the polymerase chain reaction (RT-PCR) assay. (arvojournals.org)
- Doxazosin is a selective inhibitor of alpha1-adrenergic receptors. (medscape.com)
- The affinities (Ki values) of 12 subtype-selective alpha 2-adrenergic antagonists were determined for the alpha 2 receptor in the six preparations, by radioligand binding. (aspetjournals.org)
- In summary, these data represent the first side-by-side comparison of pharmacological properties between species homologs of alpha-1AR subtypes and should facilitate the development of alpha-1AR subtype selective drugs for clinical use. (duke.edu)
- What are adrenergic drugs? (healthline.com)
- Adrenergic drugs are medications that stimulate certain nerves in your body. (healthline.com)
- Adrenergic drugs stimulate the nerves in your body's sympathetic nervous system (SNS). (healthline.com)
- Adrenergic drugs also interact with these receptors. (healthline.com)
- These adrenergic drugs act on the beta receptors directly. (healthline.com)
- Side effects of adrenergic drugs vary and depend on the specific drug you're taking. (healthline.com)
- 1) Partial destruction of the presynaptic nerve terminals with 6- hydroxydopamine did not decrease the density of alpha 2-adrenergic receptors following subsequent reserpine administration. (jneurosci.org)
- 2) Duct ligation, which results in atrophy of the gland, markedly decreased the density of the receptors following subsequent reserpine administration. (jneurosci.org)
- The density of these receptors increased similarly with age in MHS and MNS rats. (ahajournals.org)
- 125I]PIC should prove useful in binding assays involving tissues with a low receptor density or in small tissue samples and in studies of cloned and expressed alpha 2-AR. (biomedsearch.com)