Effects of Spasmogens on Relaxant Dose-Response Curves to Full or Partial Agonists at β-Adrenoceptors of Guinea Pig Isolated Trachea

Pharmacology ◽  
1987 ◽  
Vol 34 (2-3) ◽  
pp. 80-88 ◽  
Author(s):  
Penelope A. Hutson ◽  
J.R. Carpenter
1979 ◽  
Vol 57 (12) ◽  
pp. 1375-1380 ◽  
Author(s):  
L. B. Rosenberger ◽  
D. J. Triggle

45Ca uptake associated with the mechanical responses to a series of muscarinic agonists including carbachol, cis-2-methyl-4-dimethylaminomethyl-1,3-dioxolane methiodide, and three related 1,3-dioxolanes, including full and partial agonists, has been measured. Generally good agreement is found between the dose–response curves for 45Ca uptake and mechanical response, indicating that the processes of 45Ca entry, believed to be mediated through Ca2+ channels, and contractile response are closely linked. Consistent with this, partial agonists show (relative to full agonists) a reduced 45Ca uptake. The dose–response curves for carbachol-mediated contractile response and 45Ca uptake are compared with available literature data for carbachol action in the guinea pig ileal smooth muscle including binding, depolarization, and phosphatidylinositol turnover.


1987 ◽  
Vol 65 (11) ◽  
pp. 2163-2167 ◽  
Author(s):  
Akihiro Nakagoshi ◽  
Katsuo Koike ◽  
Issei Takayanagi

The effect of pretreatment with egg albumin was examined on the beta-adrenoceptors in guinea pig isolated trachea. Befunolol and carteolol acted as partial agonists and their pA2 values were significantly larger than their corresponding pD2 values in tracheae from both untreated guinea pigs and those treated with egg albumin, suggesting that the beta-adrenoceptors contain two different affinity sites. The Scatchard plot of specific [3H]befunolol binding showed two affinity sites of the receptor (high and low affinity sites) in tracheae from both untreated animals and those treated with egg albumin. The pKD values of befunolol for both low and high affinity sites were in agreement with their respective pD2 and pA2 values. The intrinsic activities of befunolol and carteolol and the pD2 values of the test drugs were decreased by the treatment with egg albumin. The treatment with egg albumin also decreased the total amount of the two affinity sites of the receptor without any change in affinity. The present results support the partial blockade of beta-adrenoceptors in asthma proposed by Szentivanyi.


1968 ◽  
Vol 46 (1) ◽  
pp. 67-69 ◽  
Author(s):  
André L. Gascon

The response of the isolated guinea pig ileum to angiotensin, bradykinin, eledoisin, and acetylcholine was studied before and during exposure to morin. Dose–response curves were made for each agonist in the presence of different concentrations of the flavonoid (1 to 8 μg/ml). Under these conditions, the responses of the ileum to eledoisin, angiotensin, and acetylcholine were modified to various degrees depending upon the concentration of morin. With morin 1 μg/ml, the effect of eledoisin was reduced, and the activity of this polypeptide progressively decreased with an increase in the concentration of the inhibitor. On the other hand, the activity of acetylcholine was potentiated while that of bradykinin and angiotensin was unchanged. With higher concentrations of morin (4 and 8 μg/ml), the effect of both angiotensin and acetylcholine was slightly reduced. On the rat blood pressure, morin did not modify the effect of agonists. From these results it is concluded that morin is a specific and noncompetitive inhibitor of eledoisin on the isolated guinea pig ileum.


1974 ◽  
Vol 32 (02/03) ◽  
pp. 356-365 ◽  
Author(s):  
F Haverkate ◽  
D. W Traas

SummaryIn the fibrin plate assay different types of relationships between the dose of applied proteolytic enzyme and the response have been previously reported. This study was undertaken to determine whether a generally valid relationship might exist.Trypsin, chymotrypsin, papain, the plasminogen activator urokinase and all of the microbial proteases investigated, including brinase gave a linear relationship between the logarithm of the enzyme concentration and the diameter of the circular lysed zone. A similar linearity of dose-response curves has frequently been found by investigators who used enzyme plate assays with substrates different from fibrin incorporated in an agar gel. Consequently, it seems that this linearity of dose-response curves is generally valid for the fibrin plate assay as well as for other enzyme plate bioassays.Both human plasmin and porcine tissue activator of plasminogen showed deviations from linearity of semi-logarithmic dose-response curves in the fibrin plate assay.


1962 ◽  
Vol 41 (1) ◽  
pp. 143-153 ◽  
Author(s):  
U. Henriques

ABSTRACT A bioassay of thyroid hormone has been developed using Xenopus larvae made hypothyroid by the administration of thiourea. Only tadpoles of uniform developmental rate were used. Thiourea was given just before the metamorphotic climax in concentrations that produced neoteni in an early metamorphotic stage. During maintained thiourea neotoni, 1-thyroxine and 1-triiodothyronine were added as sodium salts to the water for three days and at the end of one week the stage of metamorphosis produced was determined. In this way identical dose-response curves were obtained for the two compounds. No qualitative differences between their effects were noted except that triiodothyronine seemed more toxic than thyroxine in equivalent doses. Triiodothyronine was found to be 7–12 times as active as thyroxine.


2005 ◽  
Vol 8 (4) ◽  
pp. E269-E274 ◽  
Author(s):  
Sydney L. Gaynor ◽  
Gregory D. Byrd ◽  
Michael D. Diodato ◽  
Yosuke Ishii ◽  
Anson M. Lee ◽  
...  

2001 ◽  
Author(s):  
Quinton J. Nottingham ◽  
Jeffrey B. Birch ◽  
Barry A. Bodt

2021 ◽  
Vol 3 (1) ◽  
pp. 181-188
Author(s):  
Peter Bracke ◽  
Eowyn Van de Putte ◽  
Wouter R. Ryckaert

Dose-response curves for circadian phase shift and melatonin suppression in relation to white or monochromatic nighttime illumination can be scaled to melanopic weighed illumination for normally constricted pupils, which makes them easier to interpret and compare. This is helpful for a practical applications.


2021 ◽  
Vol 21 (1) ◽  
pp. 69-110 ◽  
Author(s):  
Brian G. Vegetabile ◽  
Beth Ann Griffin ◽  
Donna L. Coffman ◽  
Matthew Cefalu ◽  
Michael W. Robbins ◽  
...  

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