PDE4 inhibitors tested for their potential to induce emesis-like behavior (rodents) or emesis compared with rolipram
| Compound | Emetic(-like) Dose | Emetic(-like) Dose Ratio to Rolipram | Administration Route | Species | Test | Study |
|---|---|---|---|---|---|---|
| µg/kg | ||||||
| Rolipram | 300 | — | Intraperitoneal | Mouse | Xylazine/ketamine/anesthesia test | Vanmierlo et al., 2016 |
| Roflumilast | 3000 | 10 | ||||
| R-rolipram | 100 | — | Subcutaneous | Mouse | Xylazine/ketamine/anesthesia test | Robichaud et al., 2002b |
| S-rolipram | 1000 | 10 | ||||
| PMNPQ | 1 | 0.01 | ||||
| CT-2450 | >30,000 | >300 | ||||
| Rolipram | 100 | — | Intravenous | Mouse | Xylazine/ketamine/anesthesia test | Burgin et al., 2010 |
| D157140 | 10 | 0.1 | ||||
| D158681 | >1000 | >10 | ||||
| D159153 | 100 | 1 | ||||
| D159382 | 30 | 0.3 | ||||
| D159404 | >3000 | >30 | ||||
| D159687 | >3000 | >30 | ||||
| Rolipram | 30 | — | Subcutaneous | Mouse | Xylazine/ketamine/anesthesia test | Ricciarelli et al., 2017 |
| GEBR32a | >3000 | >30 | ||||
| Rolipram | 30 | — | Subcutaneous | Mouse | Xylazine/ketamine/anesthesia test | Bruno et al., 2011 |
| GEBR7b | 300 | 10 | ||||
| Rolipram | 500 | — | Intragastric | Mouse | Xylazine/ketamine/anesthesia test | Zhou et al., 2017 |
| 10j | >1500 | >3 | ||||
| Rolipram | 800 | — | Oral | Dog | Emesis incidence | Zhou et al., 2017 |
| 10j | >800 | >1 | ||||
| Rolipram | 400 | — | Oral | Rat | Pica feeding | Davis et al., 2009 |
| Roflumilast | 1570 | >3.5 | ||||
| Cilomilast | 6410 | >16 | ||||
| EPPA-1 | 24,260 | >60 | ||||
| Rolipram | 500 | — | Oral | Dog | Emesis incidence | Zhang et al., 2013 |
| Chlorbipram | >1000 | >2 | ||||
| Chlorbipram hydrochloride | >1070 | >2 | ||||
| Rolipram | <100 | — | Oral | Dog | Emesis incidence | Nose et al., 2016 |
| Roflumilast | 500 | >5 | ||||
| GPD-1116 | 1000 | >10 | ||||
| Rolipram | 3000 | — | Oral | Ferret | Emesis incidence | Aoki et al., 2001b |
| YM976 | 30,000 | 10 | ||||
| RP73401 | 3000 | 1 | ||||
| CPP840 | 30,000 | 10 | ||||
| Rolipram | 10,000 | — | Oral | Ferret | Emesis incidence | Gale et al., 2003 |
| V11294 | >30,000 | >3 | ||||
| Rolipram | 40 | — | Intraperitoneal | Mouse | Acute gastric retention measurement | McDonough et al., 2020a |
| Piclamilast | 200 | 5 | ||||
| YM976 | 1000 | 25 |