Table 1.
Receptors in pain pathways that undergo stimulation-induced endocytosis.
| Receptor family | Endogenous stimuli | Localization (unstimulated) | Pain/Stimulus-induced trafficking | Reference |
|---|---|---|---|---|
| Mu and Delta Opioid Receptors (MOR, DOR) | Enkephalins Dynorphins | PM TGN | PM → Endosomes Direct activation on TGN by morphine | Sternini et al. (1996), Haberstock-Debic et al. (2005) and Stoeber et al. (2018) |
| Endocannabinoid Receptors (CB1, CB2) | AEA 2-AG | PM | PM, Endosomes | Rozenfeld and Devi (2008), Lever et al. (2009) and Flores-Otero et al. (2014) |
| Metabotropic Glutamate Receptor 5 (mGluR5) | Glutamate | PM ER Nucleus | PM Direct activation on Nuclear inner membrane | O’Malley et al. (2003) and Vincent et al. (2016), Vincent et al. (2017) |
| Protease-Activated Receptor 2 (PAR2) | Trypsin, Tryptase, Elastase, Cathepsin S | PM TGN | PM → Endosomes PM → Lysosomes | DeFea et al. (2000), Ricks and Trejo (2009) and Jimenez-Vargas et al. (2018) |
| Neurokinin 1 Receptor (NK1R) | Substance P Neurokinin A/B | PM | PM → Endosomes | Mantyh et al. (1995a,b) and Jensen et al. (2017) |
| Calcitonin Receptor-Like Receptor; Receptor Activity-Modifying Protein 1 (CLR/RAMP1) | CGRP Amylin | PM | PM → Endosomes | Padilla et al. (2007) and Yarwood et al. (2017) |
| Angiotensin Receptor 1 (AT1R) | Angiotensin II | PM | PM → Endosomes | Hein et al. (1997) |
| 5-Hydroxytryptamine Receptor (5-HT2A) | Serotonin | PM | PM → Endosomes | Bhattacharyya et al. (2002) and Freeman et al. (2006) |
PM, plasma membrane; ER, endoplasmic reticulum, TGN, trans-Golgi Network; → denotes direction of receptor trafficking, from unstimulated receptor location to stimulated receptor location.