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Elektriksel Olarak Uyarılan Sıçan İleum Kasılma Yanıtları Üzerine Histamin H3 Reseptörleri ve Nitrik Oksitin Rolü

The Effects of Histamine H3 Receptors and Nitric Oxide on Electrically Stimulated Rat Ileum Contractile Responses

Journal Name:

  • Cerrahpaşa Tıp Dergisi

Publication Year:

  • 2006

Key Words:

Keywords (Original Language):

Author NameUniversity of AuthorFaculty of Author
Abstract (2. Language): 
The aim of the study is to determine the effects of histamine receptors on the ileum smooth muscle contractions and the role of nitric oxide on these effects. Isolated rat ileum preparations were mounted on organ bath and histamine receptor agonist and antagonists were added to the bath solution, then the electrical field stimulation-induced contractile responses were evaluated. Since NO donor Derivative 28 has H3 antagonistic effect we investigated any interaction between H3 receptors and NO. After blocking one of the histamine receptors H1, H2 and H3; contractile responses were observed. Then, other two receptors were blocked one by one or combination of them, to observe the changes on the contractile responses given to the electrical stimulation. To block histamine receptors; pyrilamine (10-6 Μ) as H1 receptor blocker, famotidine (10-6 Μ) as H2 receptor blocker and thioperamide (10-5 Μ) as H3 receptor blocker and various combination of them were used. All groups were treated with H3 receptor antagonist thioperamide (10-5 Μ) and agonist (R)-α-methylhistamine on 10-8, 10- 7, 10-6 ve 10-5 molar concentrations cumulatively, to observe its mediator effects on contractile responses. To view any possible interaction between histamine H3 receptors and nitric oxide, in the presence of nitric oxide precursore L-arginine (10-4 Μ) and nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester or combination of them the same procedures were carried out. While H1 and H2 receptor blockers decreased the contractile responses given to the electrical field stimulation, H3 receptor blocker increased the responses. Possibly, H3 receptors act contrary to H1 and H2 receptors and mediates inhibition on rat ileum smooth muscle contractility. Selective H3 agonist (R)-α-methylhistamine caused a significant inhibition on the contractile responses where these effects were abolished by selective H3 receptor antagonist thioperamide. In different series nitric oxide precursore L-arginine (10-4 Μ) and nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (10-4 Μ) were added to the bath solution but no significant differences observed in the contractile responses. In conclusion it was observed that nitric oxide has no effect on histamine receptor mediated contractile activity in rat ileum.
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REFERENCES

References: 

1. Zhang M, Venable JD, Thurnmond RL. The histamine
H4 receptor in autoimmune disease. Expert Opin Invest
Drugs 2006; 15: 1443-1452.
2. de Esch IJ, Thurmond RL, Jongejan A, et al. The histamine
H4 receptor as a new therapeutic target for inflammation.
Trends Pharmacol Sci 2005; 26: 462-469. .
3. Arrang JM, Garbarg M, Schwartz JC. Auto-inhibition
of brain histamine release mediated by a novel class
(H3) of histamine receptor. Nature 1983; 327: 117-123.
4. Leurs R, Brozius MM, Smit MJ, et al. Effects of histamine
H1- H2- and H3- receptor selective drugs on the mechanical
activity of guinea-pig small and large intestine.
Br J Pharmacol 1991; 102: 179-185.
5. Barajas-Lopez C, Peres AL and Espinosa-Luna R. Cellular
mechanism underlying adenosine actions on cholinergic
transmission in enteric neurons. Am J Physiol
1996; 271: 264-275.
6. Hill SJ, Ganellin CR, and Timmerman H, et al. Classification
of histamine receptors. Pharmacological Reviews
1997; 49: 253-278.
7. Hatta E, Yasuda K, Levi R. Activation of histamine H3
receptors inhibits carrier-mediated norepinephrine
release in a human mode of protracted myocardial
ischemia. Journal of Pharmacology and Experimental
Therapeutics 1997; 283: 494-500.
8. Schlicker E, Betz R, Gothert M. Histamine H3 receptormediated
inhibition of serotonin release in the rat brain
cortex. Naunyn-Schmied Arch Pharmacol 1988; 337:
588-590.
87
Cerrahpafla T›p Derg 2006; 37: 81 - 87
9. Schlicker E, Fink K, Detzner M, et al. Histamine inhibits
dopamine release in the mouse striatum via presynaptic
H3 receptors. J Neural Transmission 1993;
93: 1-10.
10. Dimitriadou V, Rouleau A, Trung Tuong MD, et
al. Functional relationships between sensory nerve
fibers and mast cells of dura mater in normal and
inflammatory conditions. Neuroscience 1997; 77:
829-839.
11. Schlicker E, Malinowska B, Kathmann M, et al.
Modulation of neurotransmitter release via histamine
H3 heteroreceptors. Fundamental & Clinical Pharmacology
1994; 8: 128-137.
12. Massimo Bertinaria. H3 receptor ligands: new imidazole
H3-antagonists endowed with NO-donor
properties. Il Farmaco 2003; 58: 279-283. .
13. Hew RWS and Hodgkinson CR. Characterization of
histamine H3-receptors in guinea pig ileum with H3-
selective ligands. Br J Pharmacol 1990; 101: 621-624.
14. EA-Kim L, Javellaud J and Oudart N. Endotheliumdependent
relaxation of rabbit middle cerebral artery
to a histamine H3 agonist is reduced by inhibitors of
nitric oxide and prostacyclin synthesis. Br J Pharmacol
1992; 105:103-106.
15. Martinez AC, Novella S, Raposo R, et al. Histamine
receptors in isolated bovine oviductal arteries. Eur
J Pharmacol 1997; 326: 163-173.
16. Oike M, Kitamura K and Kuriyama H. Histamine
H3-receptor activation augments voltage-dependent
Ca2+ current via GTP hydrolysis in rabbit saphenous
artery. J Physiol 1992; 448:133-152.
17. Ambache N and Aboo Zar M. An inhibitory action
of histamine on the guinea-pig ileum. Br J Pharmacol
1970; 38: 229-240.
18. Sung TS, La JH, Kim TW, et al. Alteration of nitrergic
neuromuscular transmission as a result of acute experimental
colitis in rat. J Vet Sci 2006; 7: 143-150.
19. Thatcher GR, Nicolescu AC, Bennett M, et al. Nitrates
and NO release: contemporary aspects in biological
and medicinal chemistry. Free Radic Biol Med, 2004;
37: 1122-1143.
20. Osinsky MA, Bass P. Chronic denervation of rat
jejunum results in cholinergic supersensitivity due
to reduction of cholinesterse activity. J Pharmacol
Exp Ther 1993; 266: 1684-1690.
21. Tuladhar BR , Costall B and Naylor RJ. Modulation
of 5-HT4 receptor function in the rat isolated ileum by
fluoxetine: the involvement of endogenous 5 hydroxytryptamine.
British J Pharmacology 2002; 136:150-
156.
22. Ogata N, Shibata T. Antidiarrheal Activity of Wood
Creosote: Inhibition of Muscle Contraction and Enterotoxin-
Induced Fluid Secretion in Rabbit Small Intestine.
Pharmacology 2001; 62:181-187. .
23. Kayaalp SO. Rasyonel tedavi yönünden t›bbi farmakoloji,
10. bask›, 2002: 979-980.
24. Kayaalp SO. Rasyonel tedavi yönünden t›bbi farmakoloji,
10. bask›, 2002: 549-553.
25. Franco R, Costa M and Furness JB. Evidence for the
release of endogenous substance P from intestinal
nerves. Naunyn-Schiedeberg's Arch Pharmacol 1979;
306:195-201.
26. Bertaccini G and Coruzzi G. An update on histamine
H3 receptors and gastrointestinal functions. Dig Dis
Sci 1995; 40:2052-2063.
27. Patel NM, Goyal RK and Verma SC. Histaminergic
H1 ve H2 excitatory receptors in the guinea pig uterus
and taenia coli. Can J Physiol Pharmacol 1980; 58:
1500-1503.
28. Barker LA and Ebersole BJ. Histamine H2 receptors
on guinea pig ileum myenteric plexus neurons
mediate the release of conractile agents. J Pharmacol
Exp Ther 1982; 221: 69-75.
29. Bertaccini G. Amines: Histamine in mediators and
drugs in gastrointestinal motility, ed. By G. Bertaccini,
Handbook Experimental Pharmacology; 1982: 59:
201-218.
30. Coruzzi G, Poli E and Bertaccini G. Histamine receptors
in isolated guinea pig duodenal muscle: H3 receptors
inhibit cholinergic neurotransmission. J Pharmacol
Exp. Ther 1991; 258: 325-331.
31. Bertaccini G, Zappia L. Histamine receptors in the
guinea pig duodenum. J Pharmacol 1981;33:590-
593.
32. Ishikawa S and Sperelakis N. A novel class (H3)
of histamine receptors on perivasculer nerve terminals.
Nature 1987; 327: 158-160.
33. Hemedah M, Loiacono R, Coupar IM, et al. Lack
of evidence for histamine H3 receptor function in
rat ileum and human colon. Naunyn Schiemedebergs
Arch Pharmacol 2001; 363: 133-138.
34. Schaefer U, Schneider A, Rudroff C, et al. Nitric
oxide mediates histamine induced down-regulation
of H2 receptor mRNA and internalization
of the receptor protein (R1). Cell Mol Life Sci 2003;
60: 1968-1981.
35. Osthaus LE and Galligan JJ. Antagonists of nitric
oxide synthesis inhibit nerve-mediated relaxations
of longitudinal muscle in guinea pig ileum. Pharmacology
and Experimental Therapeutics 1992;
260: 140-145.

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