Effects and Selectivity of CL 316243, Beta-3-Adrenoceptor Agonist, in Term-Pregnant Rat Myometrium

Kaya, Tijen; Karadaş, Barış; Altun, Ahmet; Sarac, İkram; Bağcıvan, İhsan

doi:10.1159/000332393

Cited by 7 publications

(5 citation statements)

References 51 publications

(35 reference statements)

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“…Briefly, in the control and saline-injected uteri, NA led to decrease in tension, amplitude and frequency versus the period before NA addition. Above data are similar to those revealed in healthy uteri of pigs [21,24,30,31] and other animal species [7,11,[32][33][34]. Comparing to the period before NA application, NA in the E. coli group reduced the amplitude and frequency.…”

Section: Discussionsupporting

confidence: 88%

Effect of blocking of alpha1-adrenoreceptor isoforms on the noradrenaline-induced changes in contractility of inflamed pig uterus

Jana

Całka

2023

PLoS ONE

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Background Disturbances in uterine contractility often lead to the origin, development and maintenance of endometritis and metritis, which are a very common and serious pathologies in domestic animals. Here we aimed to investigate the role of α1A-, α1B- and α1D-adrenoreceptors (ARs) in noradrenaline (NA)-induced contractility of inflammatory-changed porcine uterus. Methods On Day 3 of the estrous cycle, either Escherichia coli (E. coli) suspension (E. coli group) or saline (SAL group) was injected into uterine horns, or only laparotomy was performed (CON group). Eight days later, infected gilts developed severe acute endometritis. Results Compared to the period before NA application, NA reduced the contractile amplitude and frequency in myometrium (MYO) and endometrium (ENDO)/MYO strips from the CON, SAL and E. coli groups. In the last group, the amplitude in MYO and the frequency in ENDO/MYO were lowered versus other groups. After using α1A-ARs antagonist with NA, a greater decrease or occurrence of a drop in the amplitude and frequency in all groups (ENDO/MYO) were found compared to this neurotransmitter action alone. Such results were noted for NA action on the frequency after α1B-ARs blocking in the CON (both kinds of strips) and SAL (ENDO/MYO) groups. In response to α1D-ARs antagonist with NA, a greater decrease or occurrence of a drop in the amplitude was noted in the CON (both kinds of strips) and SAL and E. coli (MYO) groups. Use of these factors caused the similar changes in the frequency in CON and E. coli (MYO) and SAL (ENDO/MYO) groups. In response to NA, α1A,B,D-ARs antagonist led to a greater reduction or appearance of a drop in the amplitude in the CON and SAL (ENDO/MYO) and E. coli (both kinds of strips) as well as in the frequency in the CON and SAL (ENDO/MYO) and E. coli (MYO) groups. Conclusions In conclusion, activation of α1A- and α1D-ARs by NA promotes the contractile amplitude and frequency in the inflamed pig uterus; pharmacological modulation of these receptors can be utilized to enhance systolic activity of myometrium.

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Section: Discussionsupporting

confidence: 88%

Effect of blocking of alpha1-adrenoreceptor isoforms on the noradrenaline-induced changes in contractility of inflamed pig uterus

Jana

Całka

2023

PLoS ONE

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“…Earlier, the role of β2- and β3-ARs in myometrial relaxation under physiological conditions in humans 22 , 23 , pigs 26 , 27 and rats 24 , 25 was reported. This effect in a mouse uterus is mediated by β1- and β3-ARs 28 , 29 .…”

Section: Discussionmentioning

confidence: 99%

“…It is known that NA reduces the contractile activity of healthy pig uteri 3 , 19 , 20 , 26 , 27 , 32 as well as other animal species 21 , 24 , 25 , 28 , 29 . The present study demonstrating the NA ability to decrease tension, amplitude and frequency in the control and saline-treated pig uteri compared to the period before this neurotransmitter addition, confirms the above findings.…”

Section: Discussionmentioning

confidence: 99%

“…With reference to the participation of NA in the contractility of healthy uteri, it is known that in various species this neurotransmitter stimulates (via α-ARs) and inhibit (via β-ARs) myometrial contractile activity 18 – 21 . Moreover, the role of β2- and β3-ARs in relaxation of human 22 , 23 , rat 24 , 25 and pig 26 , 27 MYO was indicated. In mice, the decrease in uterine contractility is mediated by β1- and β3-ARs 28 , 29 .…”

Section: Introductionmentioning

confidence: 99%

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Role of beta-adrenergic receptor subtypes in pig uterus contractility with inflammation

Jana

Całka

2021

Sci Rep

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Uterine inflammation is a very common and serious condition in domestic animals. To development and progression of this pathology often lead disturbances in myometrial contractility. Participation of β1-, β2- and β3-adrenergic receptors (ARs) in noradrenaline (NA)-influenced contractility of the pig inflamed uterus was studied. The gilts of SAL- and E.coli-treated groups were administered saline or E.coli suspension into the uterine horns, respectively. Laparotomy was only done in the CON group. Compared to the period before NA administration, this neurotransmitter reduced the tension, amplitude and frequency in uterine strips of the CON and SAL groups. In the E.coli group, NA decreased the amplitude and frequency, and these parameters were lower than in other groups. In the CON, SAL and E.coli groups, β1- and β3-ARs antagonists in more cases did not significantly change and partly eliminated NA inhibitory effect on amplitude and frequency, as compared to NA action alone. In turn, β2-ARs antagonist completely abolished NA relaxatory effect on these parameters in three groups. Summarizing, NA decreases the contractile amplitude and frequency of pig inflamed uterus via all β-ARs subtypes, however, β2-ARs have the greatest importance. Given this, pharmacological modulation of particular β-ARs subtypes can be used to increase inflamed uterus contractility.

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“…Yapılan çeşitli çalışmalarda β3 adrenerjik agonistinin potansiyel tokolitik ajan olduğu, düşüğü kontrol ettiği ve daha az kardiyovasküler yan etkisi olduğu 19 ve β2' den daha (viabilite) güvenilir kullanılabileceği rapor edilmiştir [65][66][67] .…”

Section: β3-ar Agonistleri Ile Preterm Doğumu öNleme çAlışmalarıunclassified

Story and Effects of Βeta 3 Adrenoceptors

Pekmezekmek

2022

Arşiv Kaynak Tarama Dergisi

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Sempatik sinirlerin insan vücudunda çeşitli etkilere yol açtığı 19.yüzyıldan itibaren bilinmektedir. Birden fazla adrenerjik reseptör olduğu Ahlquist tarafından ilk olarak 1948 yılında ileri sürülmüş ve birçok araştırıcı tarafından bu reseptörlerin sayısının bilinmediği ifade edilmiştir. Daha sonra 1984 yılında Arch adlı bilim adamı tarafından kemirgenlerde beyaz ve kahverengi yağda atipik bir β adrenoseptor (AR) varlığı ortaya konulmuş ve bu AR’ ler β3 AR olarak adlandırılmıştır. Bu bilgilerin ışığında 1989 yılında ilk insan β3-ARs klonlanmış ve bu AR’lerin kemirgen β3-AR’lerdeki gibi barsak ve yağ dokusunda lokalize olduğu bulunmuştur. Hayvan modellerinde yapılan çalışmalarda, β3 AR agonistlerinin termojenik, antilipojenik, anti obesitik, antidepresan etki gösterdiği, insan safra kesesi ve idrar kesesinde gevşemeye neden olduğu ve preterm doğumu önlemede kullanılabileceği yönünde bulgular elde edilmiştir. Preterm doğum, obstetrideki en karmaşık ve önemli zorluklardan biridir. Yaklaşık 40 yıllık araştırma ve klinik ilerlemeye rağmen günümüzde preterm doğum insidansı maalesef değişmemiştir. Bu konuda ileri çalışmalara ihtiyaç olduğu düşünülmektedir.

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Effects and Selectivity of CL 316243, Beta-3-Adrenoceptor Agonist, in Term-Pregnant Rat Myometrium

Cited by 7 publications

References 51 publications

Effect of blocking of alpha1-adrenoreceptor isoforms on the noradrenaline-induced changes in contractility of inflamed pig uterus

Effect of blocking of alpha1-adrenoreceptor isoforms on the noradrenaline-induced changes in contractility of inflamed pig uterus

Role of beta-adrenergic receptor subtypes in pig uterus contractility with inflammation

Story and Effects of Βeta 3 Adrenoceptors

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