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Page 1
URB937 Prevents the Development of Mechanical Allodynia in Male Rats with Trigeminal Neuralgia.
Demartini C, Greco R, Zanaboni AM, Francavilla M, Facchetti S, Tassorelli C. Demartini C, et al. Pharmaceuticals (Basel). 2023 Nov 18;16(11):1626. doi: 10.3390/ph16111626. Pharmaceuticals (Basel). 2023. PMID: 38004491 Free PMC article.
When administered after allodynia development, URB937 prevented IoN-CCI-induced changes in CGRP and cytokine gene expression; this was not associated with a significant abrogation of the mechanical allodynia. These findings suggest that URB937 may counteract, but no …
When administered after allodynia development, URB937 prevented IoN-CCI-induced changes in CGRP and cytokine gene expression; this wa …
Characterization of the peripheral FAAH inhibitor, URB937, in animal models of acute and chronic migraine.
Greco R, Demartini C, Zanaboni A, Casini I, De Icco R, Reggiani A, Misto A, Piomelli D, Tassorelli C. Greco R, et al. Neurobiol Dis. 2021 Jan;147:105157. doi: 10.1016/j.nbd.2020.105157. Epub 2020 Oct 28. Neurobiol Dis. 2021. PMID: 33129939 Free article.
The current study is aimed at profiling the behavioral and biochemical effects of URB937 in animal models of acute and chronic migraine. We evaluated the effects of URB937 in two rat models that capture aspects of acute and chronic migraine, and are based on single …
The current study is aimed at profiling the behavioral and biochemical effects of URB937 in animal models of acute and chronic migrai …
URB937, a peripherally restricted inhibitor for fatty acid amide hydrolase, reduces prostaglandin E2 -induced bladder overactivity and hyperactivity of bladder mechano-afferent nerve fibres in rats.
Aizawa N, Gandaglia G, Hedlund P, Fujimura T, Fukuhara H, Montorsi F, Homma Y, Igawa Y. Aizawa N, et al. BJU Int. 2016 May;117(5):821-8. doi: 10.1111/bju.13223. Epub 2015 Aug 19. BJU Int. 2016. PMID: 26189783
RESULTS: During CMG, 1 mg/kg URB937, but not vehicle or 0.1 mg/kg URB937, counteracted the PGE2 -induced changes in urodynamic variables. PGE2 increased the SAAs of C-fibres, but not Adelta-fibres. URB937 (1 mg/kg) depressed Adelta-fibre SAA and abolished the …
RESULTS: During CMG, 1 mg/kg URB937, but not vehicle or 0.1 mg/kg URB937, counteracted the PGE2 -induced changes in urodynamic …
Pharmacokinetics, pharmacodynamics and safety studies on URB937, a peripherally restricted fatty acid amide hydrolase inhibitor, in rats.
Vozella V, Ahmed F, Choobchian P, Merrill CB, Zibardi C, Tarzia G, Mor M, Duranti A, Tontini A, Rivara S, Piomelli D. Vozella V, et al. J Pharm Pharmacol. 2019 Dec;71(12):1762-1773. doi: 10.1111/jphp.13166. Epub 2019 Oct 3. J Pharm Pharmacol. 2019. PMID: 31579946 Free PMC article.
OBJECTIVES: URB937, a peripheral fatty acid amide hydrolase (FAAH) inhibitor, exerts profound analgesic effects in animal models. ...The favourable pharmacokinetic and pharmacodynamic properties of URB937, along with its tolerability, encourage further development s …
OBJECTIVES: URB937, a peripheral fatty acid amide hydrolase (FAAH) inhibitor, exerts profound analgesic effects in animal models. ... …
Effects of peripheral FAAH blockade on NTG-induced hyperalgesia--evaluation of URB937 in an animal model of migraine.
Greco R, Bandiera T, Mangione AS, Demartini C, Siani F, Nappi G, Sandrini G, Guijarro A, Armirotti A, Piomelli D, Tassorelli C. Greco R, et al. Cephalalgia. 2015 Oct;35(12):1065-76. doi: 10.1177/0333102414566862. Epub 2015 Jan 21. Cephalalgia. 2015. PMID: 25608877 Free article.
Furthermore, we investigated whether URB937 affects NTG-induced c-Fos expression in the brain. RESULTS: During the tail flick test, URB937 showed an antinociceptive effect in baseline conditions and it blocked NTG-induced hyperalgesia. URB937 also proved effe …
Furthermore, we investigated whether URB937 affects NTG-induced c-Fos expression in the brain. RESULTS: During the tail flick test, …
The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system.
Moreno-Sanz G, Barrera B, Guijarro A, d'Elia I, Otero JA, Alvarez AI, Bandiera T, Merino G, Piomelli D. Moreno-Sanz G, et al. Pharmacol Res. 2011 Oct;64(4):359-63. doi: 10.1016/j.phrs.2011.07.001. Epub 2011 Jul 7. Pharmacol Res. 2011. PMID: 21767647 Free PMC article.
Despite its limited distribution, URB937 exhibits marked analgesic properties in rodent models of pain. Pharmacological evidence suggests that the extrusion of URB937 from the CNS may be mediated by the ABC membrane transporter ABCG2 (also called Breast cancer resis …
Despite its limited distribution, URB937 exhibits marked analgesic properties in rodent models of pain. Pharmacological evidence sugg …
The Fatty Acid Amide Hydrolase Inhibitor URB937 Ameliorates Radiation-Induced Lung Injury in a Mouse Model.
Li R, Chen G, Zhou L, Xu H, Tang F, Lan J, Tong R, Deng L, Xue J, Lu Y. Li R, et al. Inflammation. 2017 Aug;40(4):1254-1263. doi: 10.1007/s10753-017-0568-7. Inflammation. 2017. PMID: 28478515
Treatment with URB937 decreased leukocyte migration and inflammatory cytokines in bronchoalveolar lavage fluid and plasma at day 30. ...Mouse survival examined in a separate group of experimental subjects indicated that URB937 could prolong animal survival. Experime …
Treatment with URB937 decreased leukocyte migration and inflammatory cytokines in bronchoalveolar lavage fluid and plasma at day 30. …
Pharmacological characterization of the peripheral FAAH inhibitor URB937 in female rodents: interaction with the Abcg2 transporter in the blood-placenta barrier.
Moreno-Sanz G, Sasso O, Guijarro A, Oluyemi O, Bertorelli R, Reggiani A, Piomelli D. Moreno-Sanz G, et al. Br J Pharmacol. 2012 Dec;167(8):1620-8. doi: 10.1111/j.1476-5381.2012.02098.x. Br J Pharmacol. 2012. PMID: 22774772 Free PMC article.
Despite its limited access to the CNS, URB937 produces marked antinociceptive effects in rodents. URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2. ...Furthermore, we evaluated the interaction of URB937 wi …
Despite its limited access to the CNS, URB937 produces marked antinociceptive effects in rodents. URB937 is actively extruded …
Posttreatment With the Fatty Acid Amide Hydrolase Inhibitor URB937 Ameliorates One-Lung Ventilation-Induced Lung Injury in a Rabbit Model.
Yin H, Li X, Xia R, Yi M, Cheng Y, Wu Y, Ke B, Wang R. Yin H, et al. J Surg Res. 2019 Jul;239:83-91. doi: 10.1016/j.jss.2019.01.009. Epub 2019 Feb 26. J Surg Res. 2019. PMID: 30822695
Twenty-four male rabbits were randomly divided into four groups (n = 6): TLV-S (2.5-h two-lung ventilation [TLV] + 1.5 mL/kg saline + 1-h TLV), OLV-S (2.5-h OLV + 1.5 mL/kg saline + 0.5-h OLV + 0.5-h TLV), U-OLV (1.5 mL/kg URB937 + 3.0-h OLV + 0.5-h TLV), and OLV-U (2.5-h …
Twenty-four male rabbits were randomly divided into four groups (n = 6): TLV-S (2.5-h two-lung ventilation [TLV] + 1.5 mL/kg saline + 1-h TL …
Peripheral FAAH inhibition causes profound antinociception and protects against indomethacin-induced gastric lesions.
Sasso O, Bertorelli R, Bandiera T, Scarpelli R, Colombano G, Armirotti A, Moreno-Sanz G, Reggiani A, Piomelli D. Sasso O, et al. Pharmacol Res. 2012 May;65(5):553-63. doi: 10.1016/j.phrs.2012.02.012. Epub 2012 Mar 7. Pharmacol Res. 2012. PMID: 22420940 Free PMC article.
When administered by the oral route in mice, URB937 was highly active (median effective dose, ED(50), to inhibit liver FAAH activity: 0.3mgkg(-1)) and had a bioavailability of 5.3%. ...The results indicate that the peripheral FAAH inhibitor URB937 is more effective …
When administered by the oral route in mice, URB937 was highly active (median effective dose, ED(50), to inhibit liver FAAH activity: …
35 results