Histamine H1 receptors in UC-11MG astrocytes and their regulation of cytoplasmic Ca2+.

Experiments were carried out on UC-11MG human astrocytoma cells, a continuous cell line that expresses a broad range of the biochemical and electrophysiological properties found in well-differentiated astrocytes. Because of a number of recent reports that astrocytes may express receptors for a variety of neuro-active substances, we measured the effects of 12 different neurotransmitters on intracellular free Ca2+ (Ca2+i) in UC-11MG cells. Of these neurotransmitters only histamine was found to have a significant effect. Further characterization of the nature of the histamine response showed that UC-11MG cells express mepyramine-sensitive H1 receptors the activation of which causes both mobilization of Ca2+ from intracellular stores and entry of Ca2+ from the extracellular solution. No evidence was found for the presence of H2 receptors. The Ca2+i response was maximal at 300 microM histamine and was attenuated by increasing cell density. We suggest that this neurotransmitter may play a role in astrocytic function in the human CNS.