Effects of 138–355, a β3-adrenoceptor selective agonist, on relaxation of the human detrusor muscle in vitro

2006 ◽  
Vol 25 (7) ◽  
pp. 815-819 ◽  
Author(s):  
Tomonori Yamanishi ◽  
Kosaku Yasuda ◽  
Satoshi Kitahara ◽  
Hideo Nakai ◽  
Ken-Ichiro Yoshida ◽  
...  
Keyword(s):  
Detrusor Muscle ◽  
Selective Agonist ◽  
Human Detrusor

In vitro Effect of Amikacin on Rat and Human Detrusor Muscle Contraction

2008 ◽  
Vol 81 (1) ◽  
pp. 94-100
Author(s):  
M. Gardi ◽  
F. Nigro ◽  
E. Ragazzi ◽  
A. Volpe ◽  
A. Totaro ◽  
...  
Keyword(s):  
Muscle Contraction ◽  
Detrusor Muscle ◽  
Vitro Effect ◽  
Human Detrusor

Effect of Treatment with Calcium Antagonists in Vitro and in Vivo on the Contractile Response of Isolated Rat and Human Detrusor Muscle

1996 ◽  
Vol 91 (4) ◽  
pp. 467-474 ◽  
Author(s):  
Ruth A. Elliott ◽  
Robert I. Norman ◽  
Stuart G. Parker ◽  
R. Paul Whitaker ◽  
C. Mark Castleden
Keyword(s):  
Single Dose ◽  
Calcium Antagonists ◽  
Contractile Response ◽  
Detrusor Muscle ◽  
Significant Difference ◽  
Effect Of Treatment ◽  
Human Detrusor ◽  
Isolated Rat

1. The effect of calcium antagonists on the contractile response of human and rat isolated detrusor muscle in vitro was investigated. The effect of treatment with nimodipine on rat detrusor muscle in vivo was also examined. 2. Nimodipine 0.1 μmol/l, nifedipine 0.1 μmol/l, nifedipine 0.25 μmol/l and verapamil 1.5 μmol/l reduced the maximum contractile response of isolated human detrusor muscle to carbachol by 42%, 35%, 41% and 28% respectively (P < 0.01). Verapamil 0.1 μmol/l had no significant effect on contractile response. 3. Nimodipine 0.1 μmol/l reduced the maximum contractile response of isolated rat detrusor muscle in vitro to electrical field stimulation and carbachol by 53% and 84% respectively (P < 0.01). 4. Rats were pretreated with nimodipine for 8 days (5 mg day−1 kg−1) or with a single dose. Serum nimodipine concentrations were higher in rats treated for 8 days. In rats treated with nimodipine for 8 days there was no significant difference in detrusor contractile response compared with controls. However, after one dose of nimodipine the maximum contractile response was significantly reduced compared with controls (P < 0.05). 5. At the concentrations studied, nimodipine had a greater inhibitory effect on the contractile response of isolated human detrusor muscle. Nimodipine significantly reduced the contractile response of rat detrusor muscle in vitro and after a single dose in vivo, but had no significant effect after 8 days' treatment in vivo. It is possible that chronic oral treatment with nimodipine caused an up-regulation of 1,4-dihydropyridine-sensitive calcium channels, which may explain the lack of clinical effect of chronic treatment with calcium antagonists in patients with detrusor instability.

Amikacin: A Novel Modulator of Vesical and Prostate Efferences. An in vitro Experimental Study

2007 ◽  
Vol 74 (4) ◽  
pp. 217-227
Author(s):  
M. Gardi ◽  
F. Nigro ◽  
E. Ragazzi ◽  
A. Volpe ◽  
A. Totaro ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Urinary Tract ◽  
Electrical Field Stimulation ◽  
Smooth Muscle Contraction ◽  
Detrusor Muscle ◽  
Detrusor Smooth Muscle ◽  
Related Compounds ◽  
Human Detrusor ◽  
Isolated Rat

The autonomic efferent neurotransmission to the bladder and prostate smooth muscle is a potential target for drug therapy of specific low urinary tract disfunction (LUTD). Since amikacin and other amynoglicosides were reported to affect neurotransmission by a pre-junctional mechanism, we investigated the effect of amikacin on isolated rat and human detrusor smooth muscle contraction and on isolated rat and human prostate contraction, to further evaluate its potential relaxant properties. Materials and Methods Samples of detrusor smooth muscle and prostate tissue, obtained from 97 rats and 16 patients undergoing surgery, were studied through the measurement of isometric contraction induced by electrical field stimulation (EFS) and other pharmacological stimuli in the presence or absence of 1mM amikacin in a low-Ca medium. Results Amikacin 1 mM significantly reduced contraction of isolated rat and human detrusor muscle and prostate, achieved with pre-junctional stimulation, while no significant effect was observed on contraction induced by pharmacological post-junctional stimulators. EFS contraction inhibited by amikacin was restored after addition of calcium chloride. The amikacin effect was comparable to the effect of magnesium ions, which are known to exert a pre-junctional inhibition of neurotransmitter release. Conclusions Amikacin significantly inhibited rat and human detrusor and prostate contraction evoked by pre-junctional stimulation in vitro, suggesting a depressant effect on autonomic efferent neurotransmission. Further pharmacokinetics studies and researches on related compounds may hold potential for future development in the treatment of specific low urinary tract disfunction (LUTD).

The minor population of M3-receptors mediate contraction of human detrusor muscle in vitro

2001 ◽  
Vol 21 (5) ◽  
pp. 243-248 ◽  
Author(s):  
R. Chess-Williams ◽  
C. R. Chapple ◽  
T. Yamanishi ◽  
K. Yasuda ◽  
D. J. Sellers
Keyword(s):  
Detrusor Muscle ◽  
M3 Receptors ◽  
Minor Population ◽  
Human Detrusor

165: β-Adrenoceptor Subtype 1, 2 and 3 Mrna are all Present in Human Detrusor Muscle and Urothelium

2005 ◽  
Vol 173 (4S) ◽  
pp. 45-45 ◽  
Author(s):  
Catherine A. Thomas ◽  
Shachi Tyagi ◽  
Hitoshi Masuda ◽  
Naoki Yoshimura ◽  
Michael B. Chancellor ◽  
...  
Keyword(s):  
Detrusor Muscle ◽  
Human Detrusor

scholarly journals Role of Satb1 and Satb2 Transcription Factors in the Glutamate Receptors Expression and Ca2+ Signaling in the Cortical Neurons In Vitro

2021 ◽  
Vol 22 (11) ◽  
pp. 5968
Author(s):  
Egor A. Turovsky ◽  
Maria V. Turovskaya ◽  
Evgeniya I. Fedotova ◽  
Alexey A. Babaev ◽  
Viktor S. Tarabykin ◽  
...  
Keyword(s):  
Transcription Factors ◽  
Nmda Receptor ◽  
Cortical Neurons ◽  
Target Genes ◽  
Cortical Cell ◽  
Inhibitory System ◽  
Selective Agonist ◽  
Genes Encoding ◽  
Deficient Mice

Transcription factors Satb1 and Satb2 are involved in the processes of cortex development and maturation of neurons. Alterations in the expression of their target genes can lead to neurodegenerative processes. Molecular and cellular mechanisms of regulation of neurotransmission by these transcription factors remain poorly understood. In this study, we have shown that transcription factors Satb1 and Satb2 participate in the regulation of genes encoding the NMDA-, AMPA-, and KA- receptor subunits and the inhibitory GABA(A) receptor. Deletion of gene for either Satb1 or Satb2 homologous factors induces the expression of genes encoding the NMDA receptor subunits, thereby leading to higher amplitudes of Ca2+-signals in neurons derived from the Satb1-deficient (Satb1fl/+ * NexCre/+) and Satb1-null mice (Satb1fl/fl * NexCre/+) in response to the selective agonist reducing the EC50 for the NMDA receptor. Simultaneously, there is an increase in the expression of the Gria2 gene, encoding the AMPA receptor subunit, thus decreasing the Ca2+-signals of neurons in response to the treatment with a selective agonist (5-Fluorowillardiine (FW)). The Satb1 deletion increases the sensitivity of the KA receptor to the agonist (domoic acid), in the cortical neurons of the Satb1-deficient mice but decreases it in the Satb1-null mice. At the same time, the Satb2 deletion decreases Ca2+-signals and the sensitivity of the KA receptor to the agonist in neurons from the Satb1-null and the Satb1-deficient mice. The Satb1 deletion affects the development of the inhibitory system of neurotransmission resulting in the suppression of the neuron maturation process and switching the GABAergic responses from excitatory to inhibitory, while the Satb2 deletion has a similar effect only in the Satb1-null mice. We show that the Satb1 and Satb2 transcription factors are involved in the regulation of the transmission of excitatory signals and inhibition of the neuronal network in the cortical cell culture.

Further pharmacological evaluation of a novel synthetic peptide bradykinin B2 receptor agonist

2013 ◽  
Vol 394 (3) ◽  
pp. 353-360 ◽  
Author(s):  
Martin Savard ◽  
Julie Labonté ◽  
Céléna Dubuc ◽  
Witold Neugebauer ◽  
Pedro D’Orléans-Juste ◽  
...  
Keyword(s):  
Knockout Mice ◽  
Synthetic Peptide ◽  
Receptor Agonist ◽  
Rabbit Lung ◽  
Hypotensive Action ◽  
Duration Of Action ◽  
Selective Agonist ◽  
Comparable Magnitude

Abstract We recently identified a novel human B2 receptor (B2R) agonist [Hyp3,Thi5,NChg7,Thi8]-bradykinin (NG291) with greater in vitro and in vivo potency and duration of action than natural bradykinin (BK). Here, we further examined its stability and selectivity toward B2R. The hypotensive, antithrombotic, and profibrinolytic functions of NG291 relative to BK and its analogue ([Hyp3,Thi5,(4-Me)Tyr8(ΨCH2NH)Arg9]-BK) (RMP-7) were also tested. Contraction assays using isolated mouse stomachs (containing kinin B1R, B2R, and kininase I- and II-like activities) showed that NG291 is a more potent contractant than BK and is inhibited by HOE-140 (B2R antagonist) but unaffected by R954 (B1R antagonist), whereas both decreased the potency of BK. In stomach tissues from B2R knockout mice, BK maintained its activity via B1R, whereas NG291 had no contractile effect, indicating that it was selective for B2R. Unlike BK, NG291 was not degraded by rabbit lung ACE. Comparing intravenously administered BK and NG291 revealed that NG291 exhibited more potent and prolonged hypotensive action and greater antithrombotic and profibrinolytic activities. These effects were of comparable magnitude to RMP-7 and were absent in B2R knockout mice. We concluded that NG291 is a novel biostable B2R-selective agonist that may prove suitable for investigating the (pre)clinical cardioprotective efficacy of B2R activation.

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