Copyright
©The Author(s) 2016.
World J Gastroenterol. Dec 21, 2016; 22(47): 10275-10286
Published online Dec 21, 2016. doi: 10.3748/wjg.v22.i47.10275
Published online Dec 21, 2016. doi: 10.3748/wjg.v22.i47.10275
Table 2 Preclinical studies investigating the effects of protease-activated receptor-targeting molecules on visceral hypersensitivity
| PAR | Agonist/antagonist | Species (hypersensitivity model) | Study type | Effect | Ref. |
| PAR-1 | Agonist (thrombin, TFLLR-NH2) | Rat (carrageenan) | In vivo | ↓ hyperalgesia | [56] |
| PAR-1 | Agonist (TFLLR-NH2) | Mice (capsaicin) | In vivo | ↓ hyperalgesia | [55] |
| PAR-2 | Agonist (SLIGRL-NH2) | Mice (PAR2-agonist) | In vivo | ↑ hyperalgesia | [59] |
| PAR-2 | Agonist (SLIGRL-NH2, trypsin) | Rat (PAR2-agonist) | In vivo | ↑ hyperalgesia | [60] |
| PAR-2 | Agonist (SL-NH2, trypsin, typtase) | Guinea pig submucosal neurons (PAR2-agonist) | Ex vivo | ↑ neuron excitability | [61] |
| PAR-2 | Agonist (SLIGRL-NH2, Tc-NH2, trypsin, tryptase) | Mice, rat (PAR2-agonist) | KO | ↑ hyperalgesia, absent in KO | [62] |
| PAR-2 | Agonist (2-furoyl-LIGRL-NH2) | Mice (capsaicin) | KO | ↑ hyperalgesia, absent in KO | [63] |
| PAR-2 | Antagonist (ENMD-1068) | Mice (IBS-supernatant) | KO | ↓ hypersensitivity, absent in KO | [41] |
| PAR-2 | / | Mice DRG (IBS-D supernatant) | KO | ↑ neuron excitability, absent in KO | [64] |
| PAR-4 | Agonist (PAR-4-AP, Cat-G) | Mice (IBS-D supernatant) | In vivo | ↓ hypersensitivity | [49] |
| PAR-4 | Agonist (AYPGKF-NH2) | Mice (PAR2-agonist, TRPV4-agonist) | In vivo | ↓ hypersensitivity | [57] |
- Citation: Ceuleers H, Van Spaendonk H, Hanning N, Heirbaut J, Lambeir AM, Joossens J, Augustyns K, De Man JG, De Meester I, De Winter BY. Visceral hypersensitivity in inflammatory bowel diseases and irritable bowel syndrome: The role of proteases. World J Gastroenterol 2016; 22(47): 10275-10286
- URL: https://www.wjgnet.com/1007-9327/full/v22/i47/10275.htm
- DOI: https://dx.doi.org/10.3748/wjg.v22.i47.10275