The effects of various pharmacological agents on the distribution of antihistamine activity of rat tissue extracts

1969 ◽  
Vol 47 (9) ◽  
pp. 755-762 ◽  
Author(s):  
M. Lefcort ◽  
L. E. Francis ◽  
K. I. Melville

Extracts of rat tissues (ear and abdominal skin, heart, cerebrum, spleen, kidney, lung, liver, stomach, and jejunum) were tested for their ability to antagonize histamine on the guinea pig ileum preparation. Antihistamine activity varied considerably between tissues; it was found to be highest in the ear skin and lowest in the jejunum and stomach. After pretreatment with semicarbazide (plus a pyridoxine-free diet) or reserpine, or after adrenalectomy, the antihistamine activity was reduced in some tissues but was increased in others. The variation in the behavior of the different tissues with these treatments made it impossible to interpret the distribution of antihistamine activity in terms of known sites of amine formation. After treatment with compound 48/80, however, there was an apparent parallelism between loss of antihistamine activity and depletion of mast cell histamine.

Author(s):  
Priya Gupta ◽  
Vanita Kanase

The purpose of the present work were intended to determine the antihistaminic activity of ethanolic extract of Capparis moonii W. fruits (EECM). Capparis moonii W. had been historically used in the diagnosis of cough and asthma and so we undertook this study to validate scientifically using appropriate animal models. Antihistamine is considered to be helpful for the treatment of allergic, thus, the antihistamine activity of an ethanolic extract of Capparis moonii W. in the current work was evaluated. To determine the doses, acute oral toxicity tests were conducted. Clonidine and haloperidol that induced cataleptic effect in Swiss albino mice were evaluated for antihistaminic activity at the different doses of 50mg/kg, 100mg/kg and 200mg/kg, p.o. and the evaluation is also done on guinea pig ileum tissue. The ethanolic extract of Capparis moonii W. fruits (50, 100, 200mg/kg, p.o.) and chlorpheniramine maleate (i.p.,10mg/kg) significantly inhibited (****P<0.0001) clonidine induced catalepsy but the extract donot inhibit haloperidol-induced catalepsy and histamine-induced contraction in guinea pig ileum tissue preparation shows that ethanolic extract of Capparis moonii W. inhibited the contractile activity of histamine. The result of our work shows that the ethanolic extract possesses antihistaminic activity. It can be reported that flavonoid present in the extract may be important for an antihistaminic effect and therefore may have a role in the asthma treatment.


1960 ◽  
Vol 38 (1) ◽  
pp. 585-589 ◽  
Author(s):  
Pierre Bois ◽  
Ernest H. Byrne ◽  
Leonard F. Bélanger

The decrease in subcutaneous mast cell population observed in rats on a magnesium-deficient diet has been confirmed. Pretreatment with histamine liberator compound 48/80 accentuates the decrease in mast cell counts. This condition was apparently the result of defective regeneration. The decrease in the number of subcutaneous mast cells was accompanied by a parallel reduction of histamine as appreciated by the guinea pig ileum assay. The peripheral vasodilation, which is an early sign of magnesium deficiency, did not appear in rats pretreated with 48/80.


1960 ◽  
Vol 38 (6) ◽  
pp. 585-589 ◽  
Author(s):  
Pierre Bois ◽  
Ernest H. Byrne ◽  
Leonard F. Bélanger

The decrease in subcutaneous mast cell population observed in rats on a magnesium-deficient diet has been confirmed. Pretreatment with histamine liberator compound 48/80 accentuates the decrease in mast cell counts. This condition was apparently the result of defective regeneration. The decrease in the number of subcutaneous mast cells was accompanied by a parallel reduction of histamine as appreciated by the guinea pig ileum assay. The peripheral vasodilation, which is an early sign of magnesium deficiency, did not appear in rats pretreated with 48/80.


1980 ◽  
Vol 238 (3) ◽  
pp. E258-E266
Author(s):  
A. Perez-Castillo ◽  
E. Blazquez

To show that glucagon, glucagonlike immunoreactivity (GLI), and insulin are synthetized by organs other than the pancreas and the gastrointestinal tract, different rat tissue acid-ethanol extracts were obtained and analyzed by immunoassay using specific antisera. Significant amounts of glucagon were found in the gastrointestinal tract (44.77 +/- 5.4 ng), salivary glands (1.50 +/- 0.17 ng), thymus (2.80 +/- 0.46 ng), thyroid (0.25 +/- 0.02 ng), and adrenal glands (0.25 +/- 0.06 ng). Whereas GLI appeared in the gut mucosa, adrenal and salivary glands, genuine insulin was detected only in the pancreas. Aliquots of the tissue extracts, fractionated on Bio Gel P 30 columns, gave a 3,500 mol wt immunoreactive (30 K) peak that behaved as pancreatic glucagon on acrylamide gel electrophoresis and displaced 125I-labeled glucagon previously bound to its hepatic receptors. Arginine, epinephrine, and low glucose concentrations stimulated glucagon release from parotid, thymus, and thyroid. Active glucagon biosynthesis by these organs was established by the incorporation of L-[3H]tryptophan into a 3,500 mol wt polypeptide with specific immune reaction with 30 K antiserum. These results suggest that different rat tissues can contribute to the circulating levels of glucagon and GLI and therefore to metabolic homeostasis.


2002 ◽  
Vol 282 (4) ◽  
pp. E739-E745 ◽  
Author(s):  
Venkatesh Rajapurohitam ◽  
Nathalie Bedard ◽  
Simon S. Wing

The activity of the ubiquitin-dependent proteolytic system in differentiated tissues under basal conditions remains poorly explored. We measured rates of ubiquitination in rat tissue extracts. Accumulation of ubiquitinated proteins increased in the presence of ubiquitin aldehyde, indicating that deubiquitinating enzymes can regulate ubiquitination. Rates of ubiquitination varied fourfold, with the highest rate in the testis. We tested whether ubiquitin-activating enzyme (E1) or ubiquitin-conjugating enzymes (E2s) could be limiting for conjugation. Immunodepletion of the E2s UBC2 or UBC4 lowered rates of conjugation similarly. Supplementation of extracts with excess UBC2 or UBC4, but not E1, stimulated conjugation. However, UBC2-stimulated rates of ubiquitination still differed among tissues, indicating that tissue differences in E3s or substrate availability may also be rate controlling. UBC2 and UBC4 stimulated conjugation half-maximally at concentrations of 10–50 and 28–44 nM, respectively. Endogenous tissue levels of UBC2, but not UBC4, appeared saturating for conjugation, suggesting that in vivo modulation of UBC4 levels can likely control ubiquitin conjugation. Thus the pool of ubiquitin conjugates and therefore the rate of degradation of proteins by this system may be controlled by E2s, E3s, and isopeptidases. The regulation of the ubiquitin pathway appears complex, but precise.


2012 ◽  
Vol 10 (4) ◽  
pp. 49-53
Author(s):  
Kirill Leonidovich Kryshen ◽  
Dmitriy Valentinovich Demchenko ◽  
Olga Nikolayevna Pozharitskaya ◽  
Marina Nikolayevna Makarova ◽  
Yaroslav Aleksandrovich Gushchin ◽  
...  

The effect of the peptide substance on the induced production of histamine by culture of basophile, interaction of the preparation with the H1-histamine receptors and possible sedative effect on animal models were studied. The introduction of the peptide substance in cell culture of basophile didn’t have a significant effect on the histamine release. Study of the interaction of the polypeptide substance with H1-histamine receptors of guinea pig ileum showed that the preparation inhibits the response of unstriated muscles to histamine. The effect was similar to antihistamine drug - ketotifen. In the models of “open field” and “elevated criss-cross labyrinth” it was found that the peptide preparation hasn’t a sedative effect.


1976 ◽  
Vol 54 (4) ◽  
pp. 297-300
Author(s):  
Guy Pelletier ◽  
P. Gauthier ◽  
G. Laflamme ◽  
P. Coan ◽  
M. Lepage

A natural antihistamine substance (NAS) present in bile has been investigated. It was found that the antihistamine activity was not due to proteins, lipids, pigments, or amino acids. On ion exchange chromatography and thin-layer chromatography, this activity was associated with bile acids. Many bile acids could, in varying degrees, inhibit the histamine induced guinea pig ileum contraction, desoxycholic acid being the most potent. However NAS activity could be separated from bile acids and their conjugates using a different solvent system. Furthermore, NAS showed a higher antihistamine activity than bile acids. This substance seems to be responsible for 15–20% of the activity of whole bile. The substance has not yet been identified.


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