Abstract
Histamine H 3 receptor ligands are usually tested in guinea-pig intestine preparations. A possible desensitization of agonist-induced twitch inhibition was studied in longitudinal muscle-myenteric plexus from ileal segments. A cumulative concentration–response curve for R- α-methylhistamine was made; when a second curve was made 30 min afterwards, a marked decrease of pD 2 and a more modest decrease of E max were observed without changes in tissue sensitivity to electrical stimulation or morphine inhibition. At 120 min, pD 2 and E max were not different from those for the first curve. Receptor desensitization seems homologous and reversible and could interfere with repetitive testing of histamine H 3 receptor ligands.
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