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1 ceptor (1000-fold selectivity over the beta1-adrenoceptor).
2 does not occur in the closely related beta2-adrenoceptor.
3 of such shape-shifting system as the beta(2)-adrenoceptor.
4 SAT and very little expression of the beta3-adrenoceptor.
5 protein-coupled receptors such as the beta2-adrenoceptor.
6 angiotensin II type 1 receptor and the beta2 adrenoceptor.
7 e antagonists/inverse agonists of the alpha2-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 orepinephrine inhibits outgrowth via beta(1)-adrenoceptors.
13 ts antagonistic effects on presynaptic beta1-adrenoceptors.
14 D -8.95) and is very selective for the beta2-adrenoceptor (1000-fold selectivity over the beta1-adren
16 onflicting functional activity at the alpha2-adrenoceptor, a G-protein-coupled receptor with relevanc
17 s) to directly probe activation of the beta2-adrenoceptor, a prototypical GPCR, and its cognate G pro
18 we decipher the ascending circuitry linking adrenoceptor-activated sacral CPGs and lumbar flexor mot
21 dy investigated the hypothesis that alpha(2)-adrenoceptor activation inhibits icilin-induced WDS.
24 so found that antagonism of hippocampal beta-adrenoceptor activity with local infusions of propranolo
25 ion variant of the gene encoding the alpha2b-adrenoceptor (ADRA2B), which has been linked to emotiona
28 epatic progenitor/oval cells (HPCs) and beta-adrenoceptor agonism will expand HPCs to reduce AILI.
29 ill inevitably be taking a long-acting beta2-adrenoceptor agonist (LABA)/ICS combination therapy, we
30 e have further characterized the novel beta2 adrenoceptor agonist C26 (7-[(R)-2-((1R,2R)-2-benzyloxyc
31 y intra-BAT injections of the specific beta3-adrenoceptor agonist CL316,243 in one pad and the vehicl
32 xidase (MAO) inhibitor harmane, the alpha(2)-adrenoceptor agonist clonidine, the mu-opioid receptor a
34 ed using multiple concentrations of the beta-adrenoceptor agonist isoproterenol (ISO) and by varying
36 after 2 min of phenylephrine (PE; an alpha1 -adrenoceptor agonist) infusion via brachial artery cathe
37 erial infusion of phenylephrine (PE; alpha1 -adrenoceptor agonist) were calculated during (1) infusio
38 e dexmedetomidine, a highly selective alpha2 adrenoceptor agonist, could safely decrease the incidenc
39 d with APAP (350 mg/kg) followed by the beta-adrenoceptor agonist, isoproterenol (ISO), or the beta-a
40 f 0.3 M NaCl after sc injections of the beta-adrenoceptor agonist, isoproterenol, a hypotensive drug
41 ment with a peripherally restricted alpha(2)-adrenoceptor agonist, ST91 (0.075, 0.15 mg/kg), also dec
43 combinations (with the Y4 receptor or beta2-adrenoceptor), agonist and antagonist pharmacology was e
44 significantly enhanced by long-acting beta2-adrenoceptor agonists (LABAs) and may contribute to the
45 inetics of several clinically relevant beta2-adrenoceptor agonists and antagonists and demonstrated t
46 am cAMP/PKA signaling attenuated, while beta-adrenoceptor agonists and cAMP/PKA activators enhanced,
47 s that are currently available such as beta2-adrenoceptor agonists and corticosteroids, it takes litt
48 with limited clinical experience, are beta3 adrenoceptor agonists and phosphodiesterase type 5 inhib
49 PD therapy involving anticholinergics, beta2-adrenoceptor agonists and/or corticosteroids, do not spe
50 Muscarinic receptor antagonists and beta-adrenoceptor agonists are used in the treatment of obstr
53 inone 2-aminoindan derived series of beta(2)-adrenoceptor agonists have been prepared and evaluated f
55 cal trial study show the efficacy of alpha-2 adrenoceptor agonists in decreasing stress-induced drug
56 of novel, potent, and selective human beta2 adrenoceptor agonists incorporating a sulfone moiety on
57 atecholamine surrogates present in the beta2-adrenoceptor agonists procaterol and BI-167107 (4), we d
58 mically and pharmacodynamically diverse beta-adrenoceptor agonists, isoproterenol and salmeterol.
59 of muscarinic receptor antagonists and beta-adrenoceptor agonists, the full value of such combinatio
62 Recent progress in structural data of beta-adrenoceptors allows us to understand and predict key in
64 nd serotonin (5-HT) receptors, we found that adrenoceptor alpha 2C (Adra2c) and serotonin receptor 2a
65 cific heteromerization between the alpha(1A)-adrenoceptor (alpha(1A)AR) and CXC chemokine receptor 2
66 crystal structure, we modeled the alpha(1B)-adrenoceptor (alpha(1B)-AR) to help identify the alloste
68 e actions of noradrenaline at spinal alpha2 -adrenoceptors, although serotonin, acting on facilitator
72 , at a locus between the membrane-bound beta-adrenoceptor and the intracellular cAMP formation site.
73 discovered much later than beta1- and beta2-adrenoceptors and exhibits unique properties which make
74 ed with altered signal transduction via beta-adrenoceptors and G proteins and with reduced cAMP forma
75 osteric inhibitor pharmacophore for alpha(1)-adrenoceptors and mechanistic insight and a new set of s
76 iction or on activation of alpha1- and beta1-adrenoceptors and miR-212/132 led to repression of MeCP2
77 uperoxide production that stimulates alpha2C-adrenoceptors and Rho-kinase-mediated MLC phosphorylatio
78 ha1A-adrenergic G protein-coupled receptors (adrenoceptors) and P2X1-purinoceptor ligand gated ion ch
79 -32), dopamine receptors-1 and -2, alpha-2C- adrenoceptor, and striatally enriched protein tyrosine p
80 nd beta1-adrenoceptors, chimeric beta2/beta1-adrenoceptors, and receptors with single-point mutations
82 by intrathecal administration of the alpha2-adrenoceptor antagonist idazoxan and intra-LC co-injecti
83 ntagonist propranolol, the mixed alpha-/beta-adrenoceptor antagonist labetalol, and the alpha1-adreno
85 that the administration of the beta1-, beta2-adrenoceptor antagonist propranolol decreases cardiac wo
86 mia was significantly attenuated by the beta-adrenoceptor antagonist propranolol, the mixed alpha-/be
88 eted for hypertension as a nonselective beta-adrenoceptor antagonist with alpha(1)AR antagonist prope
89 (1) adrenoceptor antagonist WB4101, alpha(2) adrenoceptor antagonist yohimbine and mu-opioid receptor
90 were administered hydrocortisone, the alpha2-adrenoceptor antagonist yohimbine, or both before they w
92 luated LK 204-545 (1), (1) a selective beta1-adrenoceptor antagonist, and discovered it possessed sig
93 drenergic tone using atipamezole, an alpha-2 adrenoceptor antagonist, could induce a long-term improv
95 ted that (11)C-yohimbine, a selective alpha2-adrenoceptor antagonist, is an appropriate ligand for PE
98 ere significantly reduced by alpha- and beta-adrenoceptor antagonists (-40%, p < 0.001 and -30%, p <
99 ulation of astrocytes was inhibited by alpha-adrenoceptor antagonists and abolished by depletion of n
105 , cimaterol) are potently inhibited by beta1-adrenoceptor antagonists, and 2) a low-affinity secondar
107 ns containing oxymetazoline (OXY), an alpha1-adrenoceptor (AR) agonist of the imidazoline class.
109 sents approximately 25% of the total beta(2)-adrenoceptor (AR) population as determined with the anta
111 n the airways, muscarinic receptors and beta-adrenoceptors are expressed in different locations, indi
115 fied transmembrane region (TM)4 of the beta1-adrenoceptor as key for this low-affinity conformation.
116 Green Fluorescent Protein (GFP)-taggedbeta2 adrenoceptor at a slow rate, with half-life (t1/2) value
117 Thus, unlike at the human beta1-wild-type adrenoceptor, at beta1-TM4 mutant receptors, cimaterol a
120 ked by a C9 polymethylene chain to a beta(2)-adrenoceptor (beta(2)AR) agonist moiety, represented by
121 the architecture of agonist-occupied beta(2)-adrenoceptor (beta(2)AR) in complex with the heterotrime
123 es using knock-out mice suggest that beta(3)-adrenoceptor (beta(3)-AR) signaling is dependent on cave
124 hat certain beta-blockers, specifically beta-adrenoceptor (beta-AR) inverse agonists, may be useful i
125 ctivity (SNA) coupled with dysregulated beta-adrenoceptor (beta-AR) signaling is postulated as a majo
127 udy, we examined the impact of AnxA4 on beta-adrenoceptor (beta-AR)/cAMP-dependent signal transductio
128 adiols mediate P-UAEC proliferation via beta-adrenoceptors (beta-AR) and independently of classic oes
129 ery endothelial cells (P-UAECs) through beta-adrenoceptors (beta-ARs) and independently of the classi
132 sites into the C-terminal tail of the beta2-adrenoceptor (beta2AR) and demonstrate that this mutant,
133 Vps34 is required for recycling of the beta2-adrenoceptor (beta2AR), a prototypical GPCR, and then in
134 uch as adrenaline, which activates the beta2-adrenoceptor (beta2AR), bind with relatively low affinit
135 s simulations of lipid-embedded active beta2-adrenoceptor (beta2AR*) in complex with C-terminal pepti
136 acetylcholine receptors (mAChRs) and beta-2-adrenoceptors (beta2ARs) are important regulators of air
137 sustained activation of PKA induced by beta-adrenoceptor (betaAR) dictates signaling propagation for
138 l studies suggest that stress activates beta-adrenoceptors (betaARs) to enhance metastasis from prima
139 llenges in designing and validating targeted adrenoceptor-binding radiotracers, namely the heavily we
141 mg x kg(-1)) or central nervous system beta1-adrenoceptor blockade (intracerebroventricular metoprolo
144 were performed during local alpha- and beta-adrenoceptor blockade (via a brachial artery catheter) t
149 mygdala (BLA) to examine the effects of beta-adrenoceptor blockade on immediate and delayed extinctio
151 were performed during local alpha- and beta-adrenoceptor blockade to eliminate sympathoadrenal influ
154 pal D1/D5 receptor blockade and resistant to adrenoceptor blockade: memory enhancement and long-lasti
155 y of other combinations, for example, alpha1-adrenoceptor blocker and 5alpha-reductase inhibitor, has
157 patients with septic shock using the beta-1 adrenoceptor blocker, esmolol, with specific focus on sy
159 wn that both antimuscarinic drugs and alpha1-adrenoceptor blockers can be useful for treatment of mal
161 , combinations of antimuscarinics and alpha1-adrenoceptor blockers have produced the most promising r
162 nhibitors seems to be as effective as alpha1-adrenoceptor blockers in male lower urinary tract sympto
163 ast years new formulations of several alpha1-adrenoceptor blockers were introduced to the market.
164 this review is to highlight the evolution of adrenoceptor blockers with emphasis on newly approved dr
165 compounds exert their effects at the alpha2-adrenoceptor both in vitro in human prefrontal cortex ti
168 fter activation of adipocyte-expressed beta3 adrenoceptors by catecholamines, and identified eosinoph
169 in the BLA via an interaction with the beta-adrenoceptor-cAMP cascade, at a locus between the membra
171 NDPK-C is a novel critical regulator of beta-adrenoceptor/cAMP signaling and cardiac contractility.
172 ll death, which is under the control of beta-adrenoceptor/cAMP/PKA axis through the regulation of PAR
173 aling and highlight the ability of the beta2-adrenoceptor/cAMP/PKA axis to rewire EphA2 signaling in
175 rrently thought that activation of the beta2-adrenoceptor causes c-AMP dependent activation of PKA; h
181 anolol, respectively) and abolished in beta1-adrenoceptors containing TM4 mutations vital for the sec
182 with significant, regional-dependent alpha1 adrenoceptor cross-reactivity, limiting its potential us
184 nding techniques were used to measure alpha1-adrenoceptor density and the affinity of CUMI-101 for th
187 rst, the ligand-recognition profile of beta3-adrenoceptors differs considerably from that of the othe
188 and parasympathetic nervous system, numerous adrenoceptor drugs were radiolabeled and potent radiolig
192 P 12177 (BODIPY-TMR-CGP)] at the human beta1-adrenoceptor expressed in Chinese hamster ovary cells re
194 d both mineralocorticoid receptor and alpha1-adrenoceptor expressions within 5 hours in human vascula
195 e (TM) regions of the human beta1- and beta2-adrenoceptors, followed by single point mutations, to de
196 ontrast, arrestin-3 interaction with a beta2-adrenoceptor fused to the carboxyl-terminal tail of the
197 tional deletion polymorphism in the alpha-2B adrenoceptor gene (ADRA2B) has been linked to emotional
198 at the 16 position (rs1042713) in the beta2-adrenoceptor gene (ADRB2) is associated with enhanced do
202 s that negative cooperativity across a beta1-adrenoceptor homodimer may be responsible for generating
203 ciation rate were markedly enhanced in beta1-adrenoceptor homodimers constrained by bimolecular fluor
204 the development of a PET tracer for alpha2C adrenoceptor imaging and its preliminary preclinical eva
205 L/6J mice, pharmacologic activation of beta2 adrenoceptors improved the severity of shock, including
208 he maps of (11)C-yohimbine binding to alpha2 adrenoceptors in human brain had the highest values in c
210 mination of (11)C-CUMI-101 binding to alpha1-adrenoceptors in human cerebellum under in vivo conditio
214 rough the use of X-ray data from ligand-beta-adrenoceptor (including ADRB1 and ADRB2) crystal structu
215 e and epinephrine by acting through specific adrenoceptors increase the synthesis of proangiogenic fa
216 )R with the agonist-bound structures of beta-adrenoceptors indicates that the contraction of the liga
218 Second, the expression pattern of beta3-adrenoceptors is more restricted than that of other subt
220 hese amino acids to those found in the beta2-adrenoceptor (L195Q and W199Y), or mutation of a single
222 p between structural properties of the beta2-adrenoceptor ligands and their interactions with membran
226 sms, that is, direct catecholamine toxicity, adrenoceptor-mediated damage, epicardial and microvascul
227 of 5-HT neurons revealed that, while alpha1-adrenoceptor-mediated excitation was unchanged, excitato
230 hibition are critically involved in alpha(1)-adrenoceptor-mediated vascular smooth muscle contraction
231 se cleavage-mediated) and reversible (alpha1 adrenoceptor-mediated) forms of channel activation.
234 ave its structure determined was the beta(1)-adrenoceptor mutant beta(1)AR-m23 bound to the antagonis
235 systems converge in the activation of beta2-adrenoceptors of splenic regulatory lymphocytes to contr
239 ia their binding to the active site of beta2-adrenoceptors on ASM, which triggers a signaling cascade
240 alcium-cAMP signaling by stimulating alpha2A-adrenoceptors on spines strengthens synaptic efficacy an
241 no effect on signaling and function of beta2-adrenoceptor or numerous procontractile GPCRs, but selec
246 agonism of the P2X1-purinoceptor and alpha1A-adrenoceptor provides a safe and effective therapeutic t
247 atic analysis, and the inability of targeted adrenoceptor radioligands to have an impact on clinical
248 ion of their activities at the human beta(2)-adrenoceptor receptor showed symmetrical substitution of
250 r antagonism of D1, 5HT1A, or alpha- or beta-adrenoceptors, reproduced the profile of DAMGO effects.
251 ine the exact amino acids in the human beta2-adrenoceptor responsible for this very high selectivity.
254 th wash, are largely blocked by the alpha(1)-adrenoceptor-selective antagonist prazosin, and are mimi
255 ile afforded 19, a ligand with similar beta1-adrenoceptor selectivity and partial agonism (log KD of
260 ampal synaptic plasticity by activating beta-adrenoceptor signaling and mitigating synaptotoxicity of
262 in peripheral, as well as central, alpha(2)-adrenoceptor signaling oppose the behavioral stimulant e
263 tion mediated via canonical beta1- and beta2-adrenoceptor signaling pathways; and (5) evidence for ad
264 ein LMBRD2 as a potential regulator of beta2 adrenoceptor signaling, underscoring the value of a dyna
266 n (mTOR) complex 2 has a novel role in beta3-adrenoceptor-stimulated glucose uptake in brown adipose
269 constriction evoked by extraluminal alpha(1)-adrenoceptor stimulation is blunted by vasodilator COX p
272 antagonists are available for the human beta-adrenoceptor subtype involved in these diseases, yet few
273 The expression and characteristics of beta-adrenoceptor subtypes (beta1 and beta2) and their agonis
274 a docking study at the alpha2A- and alpha2C-adrenoceptor subtypes demonstrating the structural featu
275 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 force, MLCK FRET ratio activated by alpha(1)-adrenoceptors was approximately 60% of that activated by
292 ificity of (11)C-ORM-13070 binding to alpha2 adrenoceptors was demonstrated in rats pretreated with a
293 The cross-reactivity of CUMI-101 with alpha1 adrenoceptors was performed using in vitro radioligand b
295 2 inhibition by norepinephrine (via alpha(2)-adrenoceptors, which do not bind NHERF2), nor on Ca(V)2.
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
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