GHRP-6 · research summary

Ghrelin Modulates Voltage-Gated Ca2+ Channels through Voltage-Dependent and Voltage-Independent Pathways in Rat Gastric Vagal Afferent Neurons.

Molecular pharmacology · 2024. Summary drawn from the study's full text. Each statement is followed by the exact sentence it comes from. This is a research summary, not medical advice.

Study type

In vitro electrophysiological study using whole-cell patch-clamp on isolated rat gastric vagal afferent neurons
“Therefore, the purpose of the present study was to investigate the signaling mechanism by which GHSR1a inhibits voltage-gated Ca2+ channels in isolated rat gastric vagal afferent neurons using whole-cell patch-clamp electrophysiology.”

Subjects

Isolated rat gastric vagal afferent neurons
“Therefore, the purpose of the present study was to investigate the signaling mechanism by which GHSR1a inhibits voltage-gated Ca2+ channels in isolated rat gastric vagal afferent neurons using whole-cell patch-clamp electrophysiology.”

Sample size

n = 6 for antagonist exposure; n = 8 for PTX, YM-254890, and control groups
“Exposure to the GHSR1a receptor antagonist (D-Lys3)-GHRP-6 reduced ghrelin-mediated Ca2+ channel inhibition (29.4 ± 16.7% vs. 1.9 ± 2.5%, n = 6, P = 0.0064).”

Reported findings

Ghrelin inhibited Ca2+ currents with a log (Ic50) of –2.10 ± 0.44 and a maximal inhibition of 42.8 ± 5.0%
“The ghrelin pharmacological profile indicated that Ca2+ currents were inhibited with a log (Ic50) = –2.10 ± 0.44 and a maximal inhibition of 42.8 ± 5.0%.”
Activation of GHSR1a inhibited Ca2+ currents through both voltage-dependent and voltage-independent pathways
“Interestingly, we observed that activation of GHSR1a inhibited Ca2+ currents through both voltage-dependent and voltage-independent pathways.”
GHSR1a couples to both Gαi/o and Gαq/11 subunits, as blocking either pathway reduced ghrelin's effect on Ca2+ currents
“These results indicate GHSR1a can couple to both Gαi/o and Gαq/11 in gastric vagal afferent neurons.”

Source: PubMed 39187389 · DOI 10.1124/molpharm.124.000957 · all study summaries

Study type

In vitro electrophysiological study using whole-cell patch-clamp on isolated rat gastric vagal afferent neurons

“Therefore, the purpose of the present study was to investigate the signaling mechanism by which GHSR1a inhibits voltage-gated Ca2+ channels in isolated rat gastric vagal afferent neurons using whole-cell patch-clamp electrophysiology.”

Reported findings

Ghrelin inhibited Ca2+ currents with a log (Ic50) of –2.10 ± 0.44 and a maximal inhibition of 42.8 ± 5.0%

“The ghrelin pharmacological profile indicated that Ca2+ currents were inhibited with a log (Ic50) = –2.10 ± 0.44 and a maximal inhibition of 42.8 ± 5.0%.”

Activation of GHSR1a inhibited Ca2+ currents through both voltage-dependent and voltage-independent pathways

“Interestingly, we observed that activation of GHSR1a inhibited Ca2+ currents through both voltage-dependent and voltage-independent pathways.”

GHSR1a couples to both Gαi/o and Gαq/11 subunits, as blocking either pathway reduced ghrelin's effect on Ca2+ currents

“These results indicate GHSR1a can couple to both Gαi/o and Gαq/11 in gastric vagal afferent neurons.”