Peripheral neural serotonin receptors: identification and characterization with specific antagonists and agonists.

摘要: Serotonin (5-hydroxytryptamine, 5-HT) has been shown to be a neurotransmitter in the enteric nervous system (ENS). Although 5-HT is mediator of slow excitatory postsynaptic potentials evoked by stimulation interganglionic connectives, precise role it plays physiology gut unclear. Research hampered an inadequate knowledge types receptor ENS and thus lack well-characterized antagonists. We now report identification two classes neural receptor, effects activating these receptors on myenteric type II/AH neurons, their characterization with specific agonists One class, which we propose call 5-HT1P, characterized high affinity for [3H]5-HT radioligand binding assays. This class mediates depolarization neurons associated increase input resistance. Agonists at this include, addition (in order potency), 5- 6-hydroxyindalpine 2-methyl-5-HT. 5-HT1P-mediated responses are specifically antagonized 5-hydroxytryptophyl-5-hydroxytryptophan amide. The other 5-HT2P, appears not have [3H]5-HT. brief fall 2-Methyl-5-HT, low concentrations, agonist ICS 205-930 antagonist. Binding membranes inhibited 5-HT1P antagonists but 5-HT2P antagonist or MDL 72222, another compound reported peripheral receptors.