A simple and rapid in vitro test system for the screening of histamine H3 ligands.
A simple and rapid functional test system for the screening of histamine H3 ligands is described. It is based on the inhibitory effect of histamine H3 agonists on electrically-evoked contractile response of isolated guinea pig intestine. Whole jejunum segments are continuously stimulated maximally (15 V) by electrical pulses with a frequency of 0.1 Hz and a duration of 0.5 msec. The resulting twitches are recorded isotonically (1.0 g) and can be completely abolished by atropine (0.1 mcM).
Vollinga
R C
RC
Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.
Zuiderveld
O P
OP
Scheerens
H
H
Bast
A
A
Timmerman
H
H
D000109:Acetylcholine / Q000378:metabolism; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004558:Electric Stimulation; D006168:Guinea Pigs; D017442:Histamine Agonists / Q000494:pharmacology; D066298:In Vitro Techniques; D007551:Isotonic Contraction / Q000187:drug effects; D007583:Jejunum / Q000187:drug effects / Q000502:physiology; D008024:Ligands; D008297:Male; D008761:Methylhistamines / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects / Q000502:physiology; D010880:Piperidines / Q000494:pharmacology; D011968:Receptors, Histamine / Q000187:drug effects*; D018100:Receptors, Histamine H3
D017442:Histamine Agonists; D008024:Ligands; D008761:Methylhistamines; D010880:Piperidines; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; C069357:alpha-methylhistamine; D001285:Atropine; C052075:thioperamide; D000109:Acetylcholine