Modelling and mutation studies on the histamine H1-receptor agonist binding site reveal different binding modes for H1-agonists: Asp116 (TM3) has a constitutive role in receptor stimulation

1995 ◽  
Vol 9 (4) ◽  
pp. 319-330 ◽  
Author(s):  
Anton M. ter Laak ◽  
Hendrik Timmerman ◽  
Rob Leurs ◽  
Paul H. J. Nederkoorn ◽  
Martine J. Smit ◽  
...  
Keyword(s):  
Binding Site ◽  
Receptor Agonist ◽  
Binding Modes ◽  
Agonist Binding ◽  
H1 Receptor ◽  
Receptor Stimulation ◽  
Histamine H1 Receptor

Linking agonist binding to histamine H1 receptor activation

2005 ◽  
Vol 1 (2) ◽  
pp. 98-103 ◽  
Author(s):  
Aldo Jongejan ◽  
Martijn Bruysters ◽  
Juan A Ballesteros ◽  
Eric Haaksma ◽  
Remko A Bakker ◽  
...  
Keyword(s):  
Receptor Activation ◽  
Agonist Binding ◽  
H1 Receptor ◽  
Histamine H1 Receptor

scholarly journals The role of Asp-107, the putative binding site of histamine, in histamine H1 receptor functions.

1994 ◽  
Vol 64 ◽  
pp. 168
Author(s):  
Kazumi Ota ◽  
Katsumi Fujimoto ◽  
Ikuo Imamura ◽  
Hideyuki Hayashi ◽  
Hiroyuki Kagamiyama ◽  
...  
Keyword(s):  
Binding Site ◽  
H1 Receptor ◽  
Histamine H1 Receptor ◽  
Putative Binding Site

scholarly journals THE EFFECT OF HISTAMINE H1 RECEPTOR ANTAGONISTS ON THE MORPHINE-INDUCED ANTINOCICEPTION IN THE ACUTE TRIGEMINAL MODEL OF NOCICEPTION IN RATS

2016 ◽  
Vol 10 (1) ◽  
pp. 76 ◽  
Author(s):  
Emad Khalilzadeh ◽  
Farzin Azarpey ◽  
Reza Hazrati
Keyword(s):  
Receptor Antagonist ◽  
Intraperitoneal Injection ◽  
Receptor Agonist ◽  
Pain Response ◽  
Combined Treatments ◽  
H1 Receptor ◽  
Receptor Antagonists ◽  
Corneal Surface ◽  
Histamine H1 Receptor ◽  
Trigeminal Pain

ABSTRACTObjective: In this study, the effect of different classes of histamine H receptor antagonists (chlorpheniramine, cetirizine, and fexofenadine), µopioid receptor agonist (morphine), and opioid receptor antagonist (naloxone) in separate and combined treatments were investigated on the acutetrigeminal model of pain in rats.1Methods: Eye wiping test used for induction of acute trigeminal pain by putting a drop of NaCl, 5 M solution (40 µl) on the corneal surface of the eye,and the number of eye wipes counted during the first 30 seconds.Results: Intraperitoneal injection of both chlorpheniramine and cetirizine at doses of 10 and 20 mg/kg significantly inhibited the acute trigeminal pain.However, fexofenadine did not change corneal pain response. Morphine at doses of 1.25, 2.5, and 5 mg/kg reduced eye wipe responses. Administrationof both chlorpheniramine and cetirizine but not fexofenadine before morphine-enhanced morphine analgesic activity, also pretreatment of animalswith naloxone inhibited morphine, chlorpheniramine, and cetirizine-induced analgesia in the acute corneal pain.Conclusion: Our results showed that chlorpheniramine as a histamine H antagonist that efficiently Penetrates blood-brain barrier (BBB) andcetirizine with less penetration of BBB but not fexofenadine (an H11 receptor antagonist with a negligible brain-accessibility) could induce analgesiain the acute corneal pain via opioidergic mechanism. Coadministration of morphine with chlorpheniramine or cetirizine could enhance its analgesicactivity in the acute trigeminal model of pain in rats.Keywords: Trigeminal pain, Morphine, Histamine H1 receptor antagonists, Naloxone, Rats.

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