The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site

A Pazos, D Hoyer, JM Palacios - European journal of pharmacology, 1984 - Elsevier
European journal of pharmacology, 1984Elsevier
The kinetic and pharmacological characteristics of the binding of [3 H] 5-HT (serotonin),[3 H]
8-OH-DPAT (8-OH-2-di-n-propylaminotetraline),[3 H] LSD,[3 H] ketanserin and [3 H]
mesulergine to membranes from frontal cortex, hippocampus and choroid plexus of pig brain
were studied. The binding of these ligands to frontal cortex and hippocampus demonstrated
the presence of 5-HT 1 and 5-HT 2 sites in both tissues, although hippocampus was richer in
5-HT 1 (subtype 5-HT 1A) sites.[3 H] 5-HT,[3 H] mesulergine and [3 H] LSD labeled the pig …
Abstract
The kinetic and pharmacological characteristics of the binding of [3H]5-HT (serotonin), [3H]8-OH-DPAT (8-OH-2- di-n-propylaminotetraline), [3H]LSD, [3H]ketanserin and [3H]mesulergine to membranes from frontal cortex, hippocampus and choroid plexus of pig brain were studied. The binding of these ligands to frontal cortex and hippocampus demonstrated the presence of 5-HT1 and 5-HT2 sites in both tissues, although hippocampus was richer in 5-HT1 (subtype 5-HT1A) sites. [3H]5-HT, [3H]mesulergine and [3H]LSD labeled the pig choroid plexus with high affinity. The pharmacological profiles of [3H]5-HT and [3H]mesulergine binding to this tissue were closely comparable. Ligands reported as selective for 5-HT1A, 5-HT1B or 5-HT2 subtypes did not show high affinity for these binding sites. Therefore, these 5-HT binding sites in pig choroid plexus could be named 5-HT1C. Other drugs with a high affinity for these sites were methysergide and mianserine. In pig frontal cortex, [3H]5-HT labeled the different subtypes of 5-HT1 sites. In contrast, [3H]mesulergine bound in pig frontal cortex to a small population of sites with pharmacological properties similar to those of the choroid plexus 5-HT1C sites. Possible physiological functions in which these sites might be involved are discussed.
Elsevier