Neurochemical and neuropharmacological aspects of histamine receptors.

Histamine H(1) and H(2) receptors have been identified in the mammalian central nervous system. Both receptor subtypes have been indirectly characterized by a variety of receptor-mediated biological assays and directly through the utilization of radioligand binding techniques. Two types of psychotherapeutic agents, the antidepressants and neuroleptics, are potent inhibitors of H(1) and H(2) receptors. However, most compounds tested have a higher affinity for H(1) receptors. Like many other neurotransmitter receptors, H(1) receptor function can be regulated by guanine nucleotides, various ions, and by the degree of agonist stimulation.