G Protein‐coupled Receptors

Toll‐like receptors 2 and 4 modulate the contractile response induced by serotonin in mouse ileum: analysis of the serotonin receptors involved

“…In order to study the role of the 5‐HT receptors on the responses evoked by 5‐HT, ileum segments were incubated for 15 min with ritanserin 1 nM, ondansetron 10 nM, GR113808 1 nM, or SB269970 1 nM (antagonists of 5‐HT 2 , 5‐HT 3 , 5‐HT 4 , and 5‐HT 7 receptors, respectively) before adding 5‐HT 100 μ M for 3 min. The concentrations used are based on the pKi described by other authors for these antagonists …”

“…The concentrations used are based on the pKi described by other authors for these antagonists. 17,18 All intestinal segments included in the analyses showed spontaneous contractions. The amplitude and frequency of the spontaneous contractions of ileum were analyzed.…”

The role of cholesterol metabolism and various steroid abnormalities in autism spectrum disorders: A hypothesis paper

“…Theoretically, cholesterol supplementation might increase oxytocin receptor sensitivity and hence the positive effects of oxytocin on social interaction [Aneja & Tierney, ]. Not only is oxytocin receptor modulated by cholesterol, G‐protein coupled receptors are also modulated by cholesterol levels [for review see Alexander, Mathie, & Peters, ]. Synthesis of oxytocin (OT) occurs in neurons within the hypothalamus as part of a protein precursor, which, as it is transported axonally, is both enzymatically cleaved and amidated [Gainer, Altstein, & Whitnall, ].…”

Flumazenil, naloxone and the ‘coma cocktail’

“…Naloxone is a synthetic derivative of oxymorphone developed by Sankyo in the 1960s, in which the N ‐methyl group is replaced by an N ‐allyl group. The active levorotatory enantiomer is a nearly pure competitive antagonist at the μ, δ and κ opioid receptors . Thus, it competitively antagonizes the effects of both endogenous peptide ligands (e.g.…”