An overview on functional receptor autoradiography using [35S]GTPγS

Hypocretin (Orexin) Receptor Subtypes Differentially Enhance Acetylcholine Release and Activate G Protein Subtypes in Rat Pontine Reticular Formation

“…35 S]GTP␥S autoradiography has been used successfully to quantify the functional activity of many different G protein coupled receptors (Sóvágó et al, 2001). Agonist-activated […”

“…35 S]GTP␥S binding in the brain is thought to preferentially label inhibitory (G i/o , G z ), rather than stimulatory (G s , G q ), G proteins (Sóvágó et al, 2001;Harrison and Traynor, 2003;Laitinen, 2004). Pertussis toxin selectively inactivates G i/o proteins, and pertussis toxin has been shown to be effective following microinjection into rat striatum (van der Ploeg et al, 1991), ventral tegmental area (Gronier and Rasmussen, 1999), substantia nigra compacta (Gronier and Rasmussen, 1999), and hippocampus (Tzavara et al, 2003).…”

Hyperactivity to novelty induced by social isolation is not correlated with changes in D2 receptor function and binding in striatum

“…In particular, the GTPgS binding is being used to study the first step of the intracellular signaling pathway and has been shown to be a suitable method to measure the functional sensitivity of D2 receptors under physiological and pathological circumstances (Sóvµgó et al 2001). Specifically, recent work from our laboratory (Terasmaa et al 2000) has shown increased D2-stimulated GTPgS binding (supersensitive D2 receptors) in the striatum of rats with lesions of the nigrostriatal dopaminergic pathway.…”

Functional autoradiography of neuropeptide Y Y1 and Y2 receptor subtypes in rat brain using agonist stimulated [35S]GTPγS binding

“…Upon agonist activation, the GDP bound to the a subunit is exchanged for [ 35 S]GTPgS instead of endogenous GTP and receptor activation can be evaluated by quantitating the radioactivity bound to the G protein (Weiland and Jakobs, 1994). This technique has also been applied to tissue sections in a method referred to as functional autoradiography (Só vágó et al, 2001). This assay combines the ability of quantitating agonist induced-receptor activation with anatomical localization of the receptors.…”