Characterization of β-adrenoceptor subtypes in the ferret urinary bladder in vitro and in vivo

Takeda, Hiroo; Igawa, Yasuhiko; Komatsu, Yoshimitsu; Yamazaki, Yoshinobu; Akahane, Masuo; Nishizawa, Osamu; Ajisawa, Yukiyoshi

doi:10.1016/s0014-2999(00)00586-0

Cited by 21 publications

(22 citation statements)

References 25 publications

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“…In rat models, ␤ 3 -AR agonists have been shown to increase micturition interval in bladder instability evoked by cerebral infarction (Kaidoh et al, 2002), intravesical acetic acid or prostaglandin E 2 (Woods et al, 2001;Takeda et al, 2002b); inhibit sponta- jpet.aspetjournals.org neous intermicturition contractions in obstruction-induced bladder hyperplasia (Woods et al, 2001); and decrease the frequency of rhythmic bladder contractions (Takasu et al, 2007). ␤ 3 -AR-mediated bladder relaxation is also observed in the anesthetized ferret (Takeda et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

“…Evidence suggests that species differences exist in the distributions and roles of ␤-ARs in the bladder (for comprehensive review, see Michel and Vrydag, 2006). Bladder relaxation evoked by ␤-AR agonists is mediated mainly via ␤ 1 -ARs in cats (Nergardh et al, 1977) and guinea pigs (Li et al, 1992), by ␤ 2 -ARs in rabbits, by both ␤ 2 -and ␤ 3 -ARs in rats (Yamazaki et al, 1998) and pigs (Yamanishi et al, 2002), and by ␤ 3 -ARs in the ferrets (Takeda et al, 2000), dogs (Yamazaki et al, 1998), and primates (Takeda et al, 2002a). Based on mRNA expression, at least 95% of the adrenoceptor message in human bladder comprises the ␤ 3 -AR subtype (Nomiya and Yamaguchi, 2003).…”

Section: Gw427353 Evoked Relaxation That Was Attenuated By the Nonselmentioning

confidence: 99%

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GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

Hicks

McCafferty²,

Riedel³

et al. 2007

J Pharmacol Exp Ther

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Section: Discussionmentioning

confidence: 99%

Section: Gw427353 Evoked Relaxation That Was Attenuated By the Nonselmentioning

confidence: 99%

GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

Hicks

McCafferty²,

Riedel³

et al. 2007

J Pharmacol Exp Ther

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“…It is therefore concluded that the relaxation of the monkey detrusor is mediated almost entirely via the b3-adrenoceptor. There are many reports of b3-adrenoceptors coexisting with other subtypes of badrenoceptors in urinary bladders: for example, b1-and b3-adrenoceptors in dog (12), b2-and b3-adrenoceptors in rat (12), and b 3-and an atypical b -adrenoceptor in both ferret (13) and human (5). So far, the monkey is the only instance of detrusor relaxation being mediated by the b3-adrenoceptor alone (although we cannot entirely exclude a very small contribution by another subtype).…”

Section: Discussionmentioning

confidence: 99%

Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey

Takeda

Yamazaki

Akahane

et al. 2002

Japanese Journal of Pharmacology

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ABSTRACT-We first investigated the relaxations of the urinary bladder induced by b-adrenoceptor agonists in anesthetized cynomolgus monkeys and then employed a variety of b-adrenoceptor agonists and antagonists in vitro to identify the b -adrenoceptor subtype responsible for the relaxation (using isolated monkey detrusors). Isoprenaline reduced bladder pressure in a dose-dependent manner. Isoprenaline, noradrenaline and adrenaline each produced a concentration-dependent relaxation of isolated detrusor strips, the rank order of relaxing potencies being isoprenaline > noradrenaline > adrenaline. Subtype-selective b-adrenoceptor agonists also relaxed isolated detrusor strips, the rank order of potencies being CGP-12177 > BRL 37344 > dobutamine, salbutamol, procaterol > xamoterol. In the antagonist experiment, bupranolol (b-antagonist, 10 -6 to 10 -5 M) and SR 58894A (b3-antagonist, 10 -7 to 10 -5 M) caused a rightward shift of the concentration-relaxation curve for isoprenaline, but CGP-20712A (b1-antagonist, 10 -9 to 10 -7 M) and ICI-118551 (b 2-antagonist, 10 -9 to 10 -7 M) did not. The present functional study provides the first evidence that relaxation of the monkey detrusor by b -adrenoceptor activation is mediated via the b3-subtype.

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“…In addition, β 3 -adrenoceptor agonists have fewer and weaker cardiovascular effects than those produced by β-adrenoceptor agonists acting on β 1 -and/or β 2 -adrenoceptors (Takeda et al 2000). Therefore, a selective β 3 -adrenoceptor agonist is expected to be useful clinically for the treatment of bladder dysfunctions, such as pollakiuria and urinary incontinence.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory mechanism of BRL37344 on muscarinic receptor-mediated contractions of the rat urinary bladder smooth muscle

Kubota

Nakahara

Yunoki

et al. 2002

Naunyn-Schmiedeberg's Archives of Pharmacology

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We examined the inhibitory mechanism of BRL37344, a beta-adrenoceptor agonist that is considered to be specific to beta(3)-subtype, on muscarinic receptor-mediated contraction of the rat urinary bladder smooth muscle. BRL37344 produced apparently biphasic concentration-relaxation curves in the urinary bladder smooth muscle contracted with carbachol (0.6 microM). The first and second phases had estimated p D(2) (-logEC(50)) values of 7.80+/-0.34 and 4.62+/-0.18, respectively ( n=6). The first component of the BRL37344 concentration-response curve was not affected by propranolol (1 microM), whereas it was inhibited by higher concentrations of the drug (10 microM or 30 microM). The second component was completely resistant to propranolol. On the other hand, BRL37344 produced monophasic concentration-relaxation of 30 mM KCl-precontracted urinary bladder smooth muscle with a p D(2) value of 8.34+/-0.18 ( n=6). Pretreatment of the urinary bladder smooth muscles with BRL37344 (30, 100 and 300 microM) significantly ( P<0.05) shifted the concentration-response curves for carbachol-induced contractions. In radioligand binding experiments, BRL37344 concentration-dependently displaced the specific binding of [(3)H] N-methyl scopolamine to muscarinic receptors on rat urinary bladder smooth muscle membranes. Additionally, BRL37344 inhibited [(3)H] N-methyl scopolamine binding to cloned human muscarinic receptors (M(1)-M(5)) expressed in Chinese hamster ovary cells. These results suggest that BRL37344 attenuates muscarinic receptor-mediated contractions through prevention of the agonists binding to their receptors, in addition to stimulation of beta(3)-adrenoceptors, in rat urinary bladder.

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Characterization of β-adrenoceptor subtypes in the ferret urinary bladder in vitro and in vivo

Cited by 21 publications

References 25 publications

GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey

Inhibitory mechanism of BRL37344 on muscarinic receptor-mediated contractions of the rat urinary bladder smooth muscle

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Characterization of β-adrenoceptor subtypes in the ferret urinary bladder in vitro and in vivo

Cited by 21 publications

References 25 publications

GW427353 (Solabegron), a Novel, Selective β3-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

GW427353 (Solabegron), a Novel, Selective β3-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey

Inhibitory mechanism of BRL37344 on muscarinic receptor-mediated contractions of the rat urinary bladder smooth muscle

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Product

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GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog

GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog