β3-Adrenoceptor Agonists and (Antagonists as) Inverse Agonists

Perrone, Maria Grazia; Scilimati, Antonio

doi:10.1016/b978-0-12-381298-8.00011-3

Cited by 21 publications

(9 citation statements)

References 84 publications

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“…Structurally, most of the ligands share a similar backbone, with three domains: a left- and right-hand side connected by a linker. The left-hand side is typically an arylethanolamine or aryloxypropanolamine [34], the linker has various structures including both aromatic and aliphatic moieties, the right-hand side typically contains polar and/or ionizable functionalities [35]. A great number of ligands have been tested so far, but their assignment to either one or the other category remains controversial [36,37].…”

Section: Pharmacology Of the Receptormentioning

confidence: 99%

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Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask)

Schena

Caplan

2019

Cells

105

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The beta-3 adrenergic receptor (β3-AR) is by far the least studied isotype of the beta-adrenergic sub-family. Despite its study being long hampered by the lack of suitable animal and cellular models and inter-species differences, a substantial body of literature on the subject has built up in the last three decades and the physiology of β3-AR is unraveling quickly. As will become evident in this work, β3-AR is emerging as an appealing target for novel pharmacological approaches in several clinical areas involving metabolic, cardiovascular, urinary, and ocular disease. In this review, we will discuss the most recent advances regarding β3-AR signaling and function and summarize how these findings translate, or may do so, into current clinical practice highlighting β3-AR’s great potential as a novel therapeutic target in a wide range of human conditions.

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Section: Pharmacology Of the Receptormentioning

confidence: 99%

“…β 3 -AR agonists fall in two classes depending on the time of their discovery [35]: the first-generation compounds such as BRL37344 and CL316243, were developed in the 1990s while the second-generation followed or were improved later (see Table 1 for a list of agonists tested in clinical trials).…”

Section: Pharmacology Of the Receptormentioning

confidence: 99%

Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask)

Schena

Caplan

2019

Cells

105

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“…However, their benefits are limited because of associated significant adverse cardiovascular effects [ 12 , 13 ]. In turn, there is in vitro evidence that the potential cardiovascular effects of β 3 -adrenoreceptor agonists is less than that of β 2 -adrenoreceptor agonists [ 14 ]. Nevertheless, before β 3 -adrenoreceptor agonists become therapeutic drugs with a potential target for tocolysis, it is vital to obtain more comprehensive studies on functions mediated by this receptor subtype in humans [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Altered uterine contractility in response to β-adrenoceptor agonists in ovarian cancer

Modzelewska

Jóźwik

et al. 2016

J Physiol Sci

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We aimed to prospectively examine β-adrenoceptor-mediated uterine contractility in women suffering from gynecological malignancies. Myometrial specimens were obtained from non-pregnant women undergoing hysterectomy for benign gynecological disorders, and ovarian, endometrial, synchronous ovarian–endometrial, and cervical cancer. Contractions of myometrial strips in an organ bath before and after cumulative dosages of β2- and β3-adrenoceptor agonists with preincubation of propranolol, SR 59230A, and butoxamine were studied. All agonists induced a dose-dependent attenuation for uterine contractility in endometrial or cervical cancer, similar to that observed in the reference group. Contradictory effects were observed for ovarian cancer alone or in combination with endometrial cancer. CL 316243 or ritodrine abolished the relaxation, whereas BRL 37344 increased the uterine contractility in ovarian cancer. Moreover, β-adrenoceptor antagonists caused varied effects for β2- or β3-adrenoceptor agonists. Our experiments demonstrate that ovarian cancer, alone or as synchronous ovarian–endometrial cancer, substantially alters uterine contractility in response to β-adrenoceptor agonists.Electronic supplementary materialThe online version of this article (doi:10.1007/s12576-016-0500-1) contains supplementary material, which is available to authorized users.

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“… 23 – 25 The β 3 -ARs agonists can be divided in two groups, as the first-generation compounds such as BRL37344 and CL316243, and the second-generation compounds such as mirabegron, amibegron, solabegron, ritobegron, and vibegron. 2 , 26 At the time the first generation of compounds was used in human and animal experimental studies, the second generation of compounds was also being used in clinical studies. 9 , 27 , 28 Subsequently, using β 3 -ARs in the treatment of obesity and type 2 diabetes mellitus has been questioned, and the use of β 3 -ARs agonist clinically is largely focused on the treatment of overactive urinary bladder, and mirabegron was approved and widely used in OAB.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the Effect of a Novel β3-Adrenergic Agonist on Choroidal Vascularity

Topçuoğlu¹,

Aslan²

2021

Invest. Ophthalmol. Vis. Sci.

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To determine the effect of the new β 3 -agonist (mirabegron), which is used for overactive bladder (OAB) treatment, on central retinal thickness (CRT) and choroidal vascularity.MATERIAL AND METHODS. The 26 eyes of 26 cases using 50 mg tablet mirabegron once per day for OAB were included in this prospective case control study. The CRT, choroidal thickness (ChT), and choroidal vascularity were measured at baseline, week 1 (W1), month 1 (M1), month 2 (M2), and month 3 (M3). Subfoveal ChT measurement included the total subfoveal choroidal thickness (SFCT), and the small and large choroidal vessel layer (SCVL and LCVL) thickness. The total choroidal area (TCA), lumen area (LA), stromal area (SA), stroma/lumen ratio, and choroidal vascularity index (CVI) were measured with the Image-J software. RESULTS.The largest SFCT increase compared to baseline was at M1 (26.8 ± 40.8 μm, P = 0.001). The subfoveal SCVL thickness showed a significant decrease at M2 and M3 (−6.0 ± 8.9 μm, P = 0.002; −7.8 ± 13.4 μm, P = 0.046, respectively). LCVL thickness showed a significant increase at W1, M1, and M2, with the largest at M1. CVI showed a significant increase at M1, M2, and M3 (P < 0.05 for all). The TCA, LA, and SA showed a significant increasing trend at all follow-up periods. LA/SA decreased at W1 because of stromal expansion but increased at M3 with more prominent vascular dilatation. CRT values showed no significant change. CONCLUSIONS.Mirabegron had a significant effect on choroidal thickness. Choroidal vascular response is in the form of narrowing in the choriocapillaris and enlargement in the Haller's layer.

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β3-Adrenoceptor Agonists and (Antagonists as) Inverse Agonists

Cited by 21 publications

References 84 publications

Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask)

Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask)

Altered uterine contractility in response to β-adrenoceptor agonists in ovarian cancer

Evaluation of the Effect of a Novel β3-Adrenergic Agonist on Choroidal Vascularity

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