N,N-Diethyl-2-(1-pyridyl)ethylamine, a partial agonist for the histamine receptor in guinea pig ileum.
N,N-Diethyl-2-(1-pyridyl)ethylamine (E-2-P) produced 59 +/- 7% of the maximal response to histamine in guinea pig ileal longitudinal smooth muscle and antagonized the responses of this tissue to histamine. The estimated binding constant of E-2-P for the histamine receptor predicted a binding curve nearly coincident with the agonist concentration-response curve indicating no receptor reserve for this partial agonist. Diphenhydramine (30 nM) produced competitive antagonism of response to E-2-P (pKB = 8.3 +/- 0.13). Triprolidine (0.3 nM), a slower acting antihistamine, produced a depression of the maximal responses to E-2-P. This effect was analyzed in terms of a "hemi-equilibrium" hypothesis which approximates a pseudoirreversible antagonism of histamine receptors by triprolidine with respect to E-2-P. All data are consistent with the classification of E-2-P as a simple partial agonist for the histamine receptor of guinea pig ileum.
D000818:Animals; D004155:Diphenhydramine / Q000494:pharmacology; D005021:Ethylamines / Q000494:pharmacology*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D011968:Receptors, Histamine / Q000187:drug effects*; D011969:Receptors, Histamine H1 / Q000187:drug effects*; D014311:Triprolidine / Q000494:pharmacology
D005021:Ethylamines; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D014311:Triprolidine; C029085:N,N-diethyl-2-(1-pyridyl)ethylamine; D004155:Diphenhydramine