# Recent Advances in Ionic Mechanisms in Pituitary Cells: Implications for Electrophysiological and Electropharmacological Research

**Authors:** Sheng-Nan Wu, Ya-Jean Wang, Zi-Han Gao, Rasa Liutkevičienė, Vita Rovite

PMC · DOI: 10.3390/jcm14093117 · Journal of Clinical Medicine · 2025-04-30

## TL;DR

This review explores the ionic mechanisms in pituitary cells and how drugs affect these currents, offering insights into their roles in cell function and disease.

## Contribution

The paper provides a comprehensive overview of ion currents in pituitary cells and their modulation by various compounds.

## Key findings

- GH3-cell exposure to GV-58 increases INa magnitude and inactivation time constant.
- Risperidone and di(2-ethylhexyl)-phthalate suppress IK(erg) amplitude.
- Rufinamide and QO-40 enhance BKCa channel activity.

## Abstract

Pituitary cells are specialized cells located within the pituitary gland, a small, pea-sized gland situated at the base of the brain. Through the use of cellular electrophysiological techniques, the electrical properties of these cells have been revealed. This review paper aims to introduce the ion currents that are known to be functionally expressed in pituitary cells. These currents include a voltage-gated Na+ current (INa), erg-mediated K+ current (IK(erg)), M-type K+ current (IK(M)), hyperpolarization-activated cation current (Ih), and large-conductance Ca2+-activated K+ (BKCa) channel. The biophysical characteristics of the respective ion current were described. Additionally, we also provide explanations for the effect of various drugs or compounds on each of these currents. GH3-cell exposure to GV-58 can increase the magnitude of INa with a concurrent rise in the inactivation time constant of the current. The presence of esaxerenone, an antagonist of the aldosterone receptor, directly suppresses the magnitude of peak and late INa. Risperidone, an atypical antipsychotic agent, is effective at suppressing the IK(erg) amplitude directly, and di(2-ethylhexyl)-phthalate suppressed IK(erg). Solifenacin and kynurenic acid can interact with the KM channel to stimulate IK(M), while carisbamate and cannabidiol inhibit the Ih amplitude activated by sustained hyperpolarization. Moreover, the presence of either rufinamide or QO-40 can enhance the activity of single BKCa channels. To summarize, alterations in ion currents within native pituitary cells or pituitary tumor cells can influence their functional activity, particularly in processes like stimulus–secretion coupling. The effects of small-molecule modulators, as demonstrated here, bear significance in clinical, therapeutic, and toxicological contexts.

## Linked entities

- **Chemicals:** GV-58 (PubChem CID 71463101), esaxerenone (PubChem CID 25052023), risperidone (PubChem CID 5073), di(2-ethylhexyl)-phthalate (PubChem CID 8343), solifenacin (PubChem CID 154059), kynurenic acid (PubChem CID 3845), carisbamate (PubChem CID 6918474), cannabidiol (PubChem CID 644019), rufinamide (PubChem CID 129228), QO-40 (PubChem CID 51356808)

## Full-text entities

- **Genes:** NR3C2 (nuclear receptor subfamily 3 group C member 2) [NCBI Gene 4306] {aka MCR, MLR, MR, NR3C2VIT}
- **Diseases:** pituitary tumor (MESH:D010911)
- **Chemicals:** GV-58 (-), rufinamide (MESH:C079703), di(2-ethylhexyl)-phthalate (MESH:D004051), K+ (MESH:D011188), Risperidone (MESH:D018967), Na+ (MESH:D012964), cannabidiol (MESH:D002185), esaxerenone (MESH:C000607547), kynurenic acid (MESH:D007736), Solifenacin (MESH:D000069464), carisbamate (MESH:C518914)
- **Cell lines:** GH3 — Rattus norvegicus (Rat), Rat pituitary gland neoplasm, Cancer cell line (CVCL_0273)

## Full text

_Full body text omitted from this summary view._ Fetch the complete paper as Markdown: https://tomesphere.com/paper/PMC12072979/full.md

## Figures

16 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12072979/full.md

## References

161 references — full list in the complete paper: https://tomesphere.com/paper/PMC12072979/full.md

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Source: https://tomesphere.com/paper/PMC12072979