Opioids mediate their effects via opioid receptors: mu, delta, and kappa. At the neuronal level, opioid receptors are generally inhibitory, presynaptically reducing neurotransmitter release and postsynaptically hyperpolarizing neurons.

Opioid receptors are distributed widely in the brain, in the spinal cord, on peripheral neurons, and digestive tract. By the mid-1960s, it had become apparent from pharmacologic studies that opioids were likely to exert their actions at specific receptor sites, and that there were likely to be multiple such sites. [4] .

2018年5月22日 · Researchers found that opioid drugs and the brain’s natural opioids differ in how they activate receptors in nerve cells. This difference may help researchers develop better treatments that are less addictive than currently available opioid drugs.

We discuss how future studies can consider potential cell-type, regional, and neural pathway-specific effects of opioid receptors in order to better understand how opioid receptors modulate brain function.

2023年11月22日 · Opioids interact with classical opioid receptors known as mu, delta, kappa, and nociceptive opioid receptors (MOR, DOR, KOR, and NOPR, respectively 17) and produce different behavioral responses depending on the opioid …

2023年7月24日 · To date, five types of opioid receptors have been discovered-mu receptor (MOR), kappa receptor (KOR), delta receptor (DOR), nociception receptor (NOR) and zeta receptor (ZOR). Within these different types are a subset of subtypes, mu1, mu2, mu3, kappa1, kappa2, kappa3, delta1, and delta2.

2021年1月1日 · Opioid receptors can signal through Gαi/o subunits, inhibit activity of adenyl cyclase, and reduce cyclic AMP production. Stimulation of opioid receptors can also results in the activation of potassium ion channels (Christie et al., 1987), which have been shown to have inhibitory effects on neurons (Torrecilla et al., 2002).

2018年9月24日 · They reveal multiple layers of complexity of opioid receptor function, including a spatiotemporal specificity in opioid receptor-induced cellular signaling, ligand-directed biased...

Some investigators [6,7, 141–143] have demonstrated that opioid receptor activation, by opioid agonists, protects brain from ischemia and extended the animal survival time during severe hypoxia, while others [1–4, 144, 145] showed opioid receptor inhibition by intravenous injection of high dose naloxone that interacts with DOR, MOR and KOR ...

2023年1月1日 · Opioids act on the endogenous G-protein-coupled receptors comprising four sub-types, namely, mu, delta, kappa, and nociceptin as well as four peptide families, namely, β-endorphin, enkephalins, dynorphins, and nociceptin/orphanin FQ.