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1 ceptor (1000-fold selectivity over the beta1-adrenoceptor).
2 SAT and very little expression of the beta3-adrenoceptor.
3 protein-coupled receptors such as the beta2-adrenoceptor.
4 e antagonists/inverse agonists of the alpha2-adrenoceptor.
5 does not occur in the closely related beta2-adrenoceptor.
6 of such shape-shifting system as the beta(2)-adrenoceptor.
7 angiotensin II type 1 receptor and the beta2 adrenoceptor.
8 to contain the highest densities of alpha2C adrenoceptors.
9 lamus, regions with low densities of alpha2C adrenoceptors.
10 otracer for in vivo imaging of brain alpha2C adrenoceptors.
11 macrophages, which was independent of alpha1 adrenoceptors.
12 cules that could bias signalling in the beta-adrenoceptors.
13 D -8.95) and is very selective for the beta2-adrenoceptor (1000-fold selectivity over the beta1-adren
15 onflicting functional activity at the alpha2-adrenoceptor, a G-protein-coupled receptor with relevanc
16 s) to directly probe activation of the beta2-adrenoceptor, a prototypical GPCR, and its cognate G pro
17 eart disease and heart attack) and many beta-adrenoceptor acting drugs are listed on the WHO Model Li
19 we decipher the ascending circuitry linking adrenoceptor-activated sacral CPGs and lumbar flexor mot
22 e the autophagy effect of sustained beta(2) -adrenoceptor activation in rodents with neurogenic myopa
23 dy investigated the hypothesis that alpha(2)-adrenoceptor activation inhibits icilin-induced WDS.
24 abolishes the beneficial effects of beta(2) -adrenoceptor activation on the skeletal muscle proteosta
27 pporting an autophagy mechanism for beta(2) -adrenoceptor activation, skeletal muscle-specific deleti
28 so found that antagonism of hippocampal beta-adrenoceptor activity with local infusions of propranolo
29 ion variant of the gene encoding the alpha2b-adrenoceptor (ADRA2B), which has been linked to emotiona
31 epatic progenitor/oval cells (HPCs) and beta-adrenoceptor agonism will expand HPCs to reduce AILI.
32 isk of Parkinson's disease with chronic beta-adrenoceptor agonist (eg, salbutamol) use, and by functi
33 ed corticosteroid (ICS)/long-acting beta (2)-adrenoceptor agonist (LABA) combination therapy should b
34 al cells, formoterol, a long-acting beta (2)-adrenoceptor agonist (LABA), enhanced the expression of
35 ill inevitably be taking a long-acting beta2-adrenoceptor agonist (LABA)/ICS combination therapy, we
37 e have further characterized the novel beta2 adrenoceptor agonist C26 (7-[(R)-2-((1R,2R)-2-benzyloxyc
38 y intra-BAT injections of the specific beta3-adrenoceptor agonist CL316,243 in one pad and the vehicl
39 xidase (MAO) inhibitor harmane, the alpha(2)-adrenoceptor agonist clonidine, the mu-opioid receptor a
42 ed using multiple concentrations of the beta-adrenoceptor agonist isoproterenol (ISO) and by varying
45 after 2 min of phenylephrine (PE; an alpha1 -adrenoceptor agonist) infusion via brachial artery cathe
46 erial infusion of phenylephrine (PE; alpha1 -adrenoceptor agonist) were calculated during (1) infusio
47 e dexmedetomidine, a highly selective alpha2 adrenoceptor agonist, could safely decrease the incidenc
48 d with APAP (350 mg/kg) followed by the beta-adrenoceptor agonist, isoproterenol (ISO), or the beta-a
50 combinations (with the Y4 receptor or beta2-adrenoceptor), agonist and antagonist pharmacology was e
52 significantly enhanced by long-acting beta2-adrenoceptor agonists (LABAs) and may contribute to the
53 changes produced by the long-acting beta (2)-adrenoceptor agonists (LABAs) salmeterol, indacaterol, a
54 inetics of several clinically relevant beta2-adrenoceptor agonists and antagonists and demonstrated t
55 am cAMP/PKA signaling attenuated, while beta-adrenoceptor agonists and cAMP/PKA activators enhanced,
56 s that are currently available such as beta2-adrenoceptor agonists and corticosteroids, it takes litt
57 PD therapy involving anticholinergics, beta2-adrenoceptor agonists and/or corticosteroids, do not spe
58 Muscarinic receptor antagonists and beta-adrenoceptor agonists are used in the treatment of obstr
63 cal trial study show the efficacy of alpha-2 adrenoceptor agonists in decreasing stress-induced drug
64 of novel, potent, and selective human beta2 adrenoceptor agonists incorporating a sulfone moiety on
65 on's disease seen in patients receiving beta-adrenoceptor agonists is likely to be indirectly mediate
66 atecholamine surrogates present in the beta2-adrenoceptor agonists procaterol and BI-167107 (4), we d
67 s disease, while the chronic use of the beta-adrenoceptor agonists was associated with a decreased ri
68 mically and pharmacodynamically diverse beta-adrenoceptor agonists, isoproterenol and salmeterol.
69 of muscarinic receptor antagonists and beta-adrenoceptor agonists, the full value of such combinatio
70 Recent progress in structural data of beta-adrenoceptors allows us to understand and predict key in
72 nd serotonin (5-HT) receptors, we found that adrenoceptor alpha 2C (Adra2c) and serotonin receptor 2a
73 cific heteromerization between the alpha(1A)-adrenoceptor (alpha(1A)AR) and CXC chemokine receptor 2
74 crystal structure, we modeled the alpha(1B)-adrenoceptor (alpha(1B)-AR) to help identify the alloste
77 e actions of noradrenaline at spinal alpha2 -adrenoceptors, although serotonin, acting on facilitator
81 discovered much later than beta1- and beta2-adrenoceptors and exhibits unique properties which make
82 ed with altered signal transduction via beta-adrenoceptors and G proteins and with reduced cAMP forma
83 osteric inhibitor pharmacophore for alpha(1)-adrenoceptors and mechanistic insight and a new set of s
84 iction or on activation of alpha1- and beta1-adrenoceptors and miR-212/132 led to repression of MeCP2
85 uperoxide production that stimulates alpha2C-adrenoceptors and Rho-kinase-mediated MLC phosphorylatio
86 ha1A-adrenergic G protein-coupled receptors (adrenoceptors) and P2X1-purinoceptor ligand gated ion ch
87 nd beta1-adrenoceptors, chimeric beta2/beta1-adrenoceptors, and receptors with single-point mutations
88 Since intrathecal injection of an alpha(2A)-adrenoceptor antagonist (BRL 44408) partially reversed t
91 ntagonist propranolol, the mixed alpha-/beta-adrenoceptor antagonist labetalol, and the alpha1-adreno
93 d a link between the chronic use of the beta-adrenoceptor antagonist propranolol and an increased ris
94 that the administration of the beta1-, beta2-adrenoceptor antagonist propranolol decreases cardiac wo
95 mia was significantly attenuated by the beta-adrenoceptor antagonist propranolol, the mixed alpha-/be
97 eted for hypertension as a nonselective beta-adrenoceptor antagonist with alpha(1)AR antagonist prope
98 (1) adrenoceptor antagonist WB4101, alpha(2) adrenoceptor antagonist yohimbine and mu-opioid receptor
99 were administered hydrocortisone, the alpha2-adrenoceptor antagonist yohimbine, or both before they w
101 luated LK 204-545 (1), (1) a selective beta1-adrenoceptor antagonist, and discovered it possessed sig
102 Prazosin, a potent and selective alpha1-adrenoceptor antagonist, displaces 25% of (11)C-CUMI-101
103 ted that (11)C-yohimbine, a selective alpha2-adrenoceptor antagonist, is an appropriate ligand for PE
106 ere significantly reduced by alpha- and beta-adrenoceptor antagonists (-40%, p < 0.001 and -30%, p <
107 ulation of astrocytes was inhibited by alpha-adrenoceptor antagonists and abolished by depletion of n
108 r a causal relationship between use of beta2-adrenoceptor antagonists and the increased risk of Parki
114 of Parkinson's disease associated with beta-adrenoceptor antagonists use can be explained by reverse
115 risk of Parkinson's disease because of beta-adrenoceptor antagonists use corresponds to one case in
117 , cimaterol) are potently inhibited by beta1-adrenoceptor antagonists, and 2) a low-affinity secondar
119 ns containing oxymetazoline (OXY), an alpha1-adrenoceptor (AR) agonist of the imidazoline class.
121 sents approximately 25% of the total beta(2)-adrenoceptor (AR) population as determined with the anta
122 n the airways, muscarinic receptors and beta-adrenoceptors are expressed in different locations, indi
128 fied transmembrane region (TM)4 of the beta1-adrenoceptor as key for this low-affinity conformation.
129 Green Fluorescent Protein (GFP)-taggedbeta2 adrenoceptor at a slow rate, with half-life (t1/2) value
130 Thus, unlike at the human beta1-wild-type adrenoceptor, at beta1-TM4 mutant receptors, cimaterol a
131 four active-state structures of the beta(1)-adrenoceptor (beta(1)AR) bound to conformation-specific
133 the architecture of agonist-occupied beta(2)-adrenoceptor (beta(2)AR) in complex with the heterotrime
135 es using knock-out mice suggest that beta(3)-adrenoceptor (beta(3)-AR) signaling is dependent on cave
136 ctivity (SNA) coupled with dysregulated beta-adrenoceptor (beta-AR) signaling is postulated as a majo
138 udy, we examined the impact of AnxA4 on beta-adrenoceptor (beta-AR)/cAMP-dependent signal transductio
141 adiols mediate P-UAEC proliferation via beta-adrenoceptors (beta-AR) and independently of classic oes
142 ling by soluble stress hormones through beta-adrenoceptors (beta-AR) reduces the deformability of mac
143 ery endothelial cells (P-UAECs) through beta-adrenoceptors (beta-ARs) and independently of the classi
146 sites into the C-terminal tail of the beta2-adrenoceptor (beta2AR) and demonstrate that this mutant,
147 Vps34 is required for recycling of the beta2-adrenoceptor (beta2AR), a prototypical GPCR, and then in
148 uch as adrenaline, which activates the beta2-adrenoceptor (beta2AR), bind with relatively low affinit
149 s simulations of lipid-embedded active beta2-adrenoceptor (beta2AR*) in complex with C-terminal pepti
150 acetylcholine receptors (mAChRs) and beta-2-adrenoceptors (beta2ARs) are important regulators of air
151 ld lower Na(+) concentrations, and the beta3 adrenoceptor (beta3 AR) mediates pump stimulation in myo
152 l studies suggest that stress activates beta-adrenoceptors (betaARs) to enhance metastasis from prima
153 llenges in designing and validating targeted adrenoceptor-binding radiotracers, namely the heavily we
156 were performed during local alpha- and beta-adrenoceptor blockade (via a brachial artery catheter) t
158 mygdala (BLA) to examine the effects of beta-adrenoceptor blockade on immediate and delayed extinctio
161 pal D1/D5 receptor blockade and resistant to adrenoceptor blockade: memory enhancement and long-lasti
162 y of other combinations, for example, alpha1-adrenoceptor blocker and 5alpha-reductase inhibitor, has
163 patients with septic shock using the beta-1 adrenoceptor blocker, esmolol, with specific focus on sy
164 wn that both antimuscarinic drugs and alpha1-adrenoceptor blockers can be useful for treatment of mal
166 , combinations of antimuscarinics and alpha1-adrenoceptor blockers have produced the most promising r
167 nhibitors seems to be as effective as alpha1-adrenoceptor blockers in male lower urinary tract sympto
168 ast years new formulations of several alpha1-adrenoceptor blockers were introduced to the market.
169 compounds exert their effects at the alpha2-adrenoceptor both in vitro in human prefrontal cortex ti
171 fter activation of adipocyte-expressed beta3 adrenoceptors by catecholamines, and identified eosinoph
172 NDPK-C is a novel critical regulator of beta-adrenoceptor/cAMP signaling and cardiac contractility.
173 ll death, which is under the control of beta-adrenoceptor/cAMP/PKA axis through the regulation of PAR
174 aling and highlight the ability of the beta2-adrenoceptor/cAMP/PKA axis to rewire EphA2 signaling in
176 synthesis and release of catecholamines, the adrenoceptors catecholamines bind to, and the cardiac an
177 rrently thought that activation of the beta2-adrenoceptor causes c-AMP dependent activation of PKA; h
183 anolol, respectively) and abolished in beta1-adrenoceptors containing TM4 mutations vital for the sec
184 with significant, regional-dependent alpha1 adrenoceptor cross-reactivity, limiting its potential us
186 nding techniques were used to measure alpha1-adrenoceptor density and the affinity of CUMI-101 for th
190 rst, the ligand-recognition profile of beta3-adrenoceptors differs considerably from that of the othe
191 and parasympathetic nervous system, numerous adrenoceptor drugs were radiolabeled and potent radiolig
195 P 12177 (BODIPY-TMR-CGP)] at the human beta1-adrenoceptor expressed in Chinese hamster ovary cells re
198 d both mineralocorticoid receptor and alpha1-adrenoceptor expressions within 5 hours in human vascula
199 e (TM) regions of the human beta1- and beta2-adrenoceptors, followed by single point mutations, to de
200 ontrast, arrestin-3 interaction with a beta2-adrenoceptor fused to the carboxyl-terminal tail of the
201 tional deletion polymorphism in the alpha-2B adrenoceptor gene (ADRA2B) has been linked to emotional
202 at the 16 position (rs1042713) in the beta2-adrenoceptor gene (ADRB2) is associated with enhanced do
206 s that negative cooperativity across a beta1-adrenoceptor homodimer may be responsible for generating
207 ciation rate were markedly enhanced in beta1-adrenoceptor homodimers constrained by bimolecular fluor
208 the development of a PET tracer for alpha2C adrenoceptor imaging and its preliminary preclinical eva
209 L/6J mice, pharmacologic activation of beta2 adrenoceptors improved the severity of shock, including
210 ifying structural differences in the beta(1)-adrenoceptor in complex with beta-arrestin 1 versus a G
213 he maps of (11)C-yohimbine binding to alpha2 adrenoceptors in human brain had the highest values in c
215 mination of (11)C-CUMI-101 binding to alpha1-adrenoceptors in human cerebellum under in vivo conditio
216 egional differences in expression of alpha-1 adrenoceptors in human colon emphasize the translational
220 from cells subjected to fractional, beta (2)-adrenoceptor inactivation determined that PDE4 inhibitio
221 rough the use of X-ray data from ligand-beta-adrenoceptor (including ADRB1 and ADRB2) crystal structu
222 )R with the agonist-bound structures of beta-adrenoceptors indicates that the contraction of the liga
225 Second, the expression pattern of beta3-adrenoceptors is more restricted than that of other subt
227 hese amino acids to those found in the beta2-adrenoceptor (L195Q and W199Y), or mutation of a single
229 p between structural properties of the beta2-adrenoceptor ligands and their interactions with membran
233 sms, that is, direct catecholamine toxicity, adrenoceptor-mediated damage, epicardial and microvascul
235 of 5-HT neurons revealed that, while alpha1-adrenoceptor-mediated excitation was unchanged, excitato
238 hibition are critically involved in alpha(1)-adrenoceptor-mediated vascular smooth muscle contraction
239 senteric small arteries causes a large beta1-adrenoceptor-mediated vasodilatation, which contrasts wi
240 se cleavage-mediated) and reversible (alpha1 adrenoceptor-mediated) forms of channel activation.
244 G7 blunts the beneficial effects of beta(2) -adrenoceptor on skeletal muscle proteostasis and contrac
246 ia their binding to the active site of beta2-adrenoceptors on ASM, which triggers a signaling cascade
247 alcium-cAMP signaling by stimulating alpha2A-adrenoceptors on spines strengthens synaptic efficacy an
248 no effect on signaling and function of beta2-adrenoceptor or numerous procontractile GPCRs, but selec
252 agonism of the P2X1-purinoceptor and alpha1A-adrenoceptor provides a safe and effective therapeutic t
253 atic analysis, and the inability of targeted adrenoceptor radioligands to have an impact on clinical
254 Bronchodilators that do not target beta2-adrenoceptors represent a critical unmet need for asthma
255 ine the exact amino acids in the human beta2-adrenoceptor responsible for this very high selectivity.
257 odilatation, whereas 0.1 mum of the beta(2) -adrenoceptor selective antagonist ICI-118,551 had no eff
258 ile afforded 19, a ligand with similar beta1-adrenoceptor selectivity and partial agonism (log KD of
263 ampal synaptic plasticity by activating beta-adrenoceptor signaling and mitigating synaptotoxicity of
267 tion mediated via canonical beta1- and beta2-adrenoceptor signaling pathways; and (5) evidence for ad
268 ein LMBRD2 as a potential regulator of beta2 adrenoceptor signaling, underscoring the value of a dyna
270 n (mTOR) complex 2 has a novel role in beta3-adrenoceptor-stimulated glucose uptake in brown adipose
274 antagonists are available for the human beta-adrenoceptor subtype involved in these diseases, yet few
275 a docking study at the alpha2A- and alpha2C-adrenoceptor subtypes demonstrating the structural featu
276 file at both 5-HT(1A) receptors and alpha(1)-adrenoceptor subtypes was measured by binding assay and
278 human cerebellum reflects binding to alpha1-adrenoceptors, suggesting that the cerebellum is of limi
279 a hyperfunctional variant of the human beta1-adrenoceptor that carries an arginine at position 389 in
280 The pathway involves activation of beta2-adrenoceptors that increase cAMP levels and activate cAM
282 , is an appropriate ligand for PET of alpha2 adrenoceptors that passes readily from blood to brain ti
283 neering phosphorylation sites into the beta2-adrenoceptor the receptor showed prolonged interaction w
284 a single residue (W199D) in the human beta1-adrenoceptor thus abolished this secondary conformation
285 centration response at human beta1-wild-type adrenoceptors to a monophasic concentration response in
286 pathways linking chronic stimulation of beta-adrenoceptors to hypertrophy and associated arrhythmias.
287 e observed with cardiomyocyte-specific beta1-adrenoceptor transgenic mice and human heart biopsies.
288 igated the effects of blocking 5-HT and beta-adrenoceptor transmission in DH on drug seeking during E
290 quantify the density and affinity of alpha 2 adrenoceptors under condition of changing radioligand bi
291 ificity of (11)C-ORM-13070 binding to alpha2 adrenoceptors was demonstrated in rats pretreated with a
292 The cross-reactivity of CUMI-101 with alpha1 adrenoceptors was performed using in vitro radioligand b
295 so possess significant affinity for the a(2)-adrenoceptor, which complicates the interpretation of th
296 duction of in vitro affinity at the alpha(1)-adrenoceptor while both potency and efficacy were increa
297 h factor receptor (EGFR) with EGF, the beta2-adrenoceptor with dopamine, or the hepatocyte growth fac
298 s secondary conformation and created a beta1-adrenoceptor with only one high-affinity agonist conform
299 -fold, to within 4-fold of that of the beta1-adrenoceptor, without affecting the affinity or selectiv
300 y differs between the human and rodent beta3-adrenoceptor, yielding considerable species differences