Table 2.
Pharmacological studies examining subtype-specific mGlu receptor compounds on sleep in rodents.
| Awake | NREM | REM | |||||||
|---|---|---|---|---|---|---|---|---|---|
| Compound | Duration | Duration | Latency | Bouts | Bout duration | Duration | Latency | Bouts | Bout duration |
| mGlu5 receptor NAMS (within 4–6h post-dosing) | |||||||||
| MPEP1,2 (1–20mg/kg, IP) | ↑ | ↑ | n.s. | ↓ | ↑ | ↓ | ↑ | ↓ | ↓ |
| MTEP1 (1–10 mg/kg, IP) | n.s. | ↑ | n.s. | ↓ | ↑ | ↓ | ↑ | n.s. | ↓ |
| GRN-5293 (0.32–1mg/kg, SC) | ↑ | ↓ | — | — | — | ↓ | — | — | — |
| Mavoglurant3 (1–3.2mg/kg, SC) | ↑ | ↓ | — | — | — | ↓ | — | — | — |
| Basimglurant4 (0.03–0.3mg/kg, PO) | ↑ | ↓ | ↑ | — | — | ↓ | ↑ | — | — |
| VU04242385 (1–30mg/kg, IP) | ↑ | ↓ | n.s. | — | — | ↓ | ↑ | — | — |
| M-5MPEP (partial NAM)5 (18–56.6 mg/kg, IP) | n.s. | n.s. | n.s. | — | — | ↓ | ↑ | — | — |
| mGlu5 Receptor PAMS (within 4–6h post-dosing) | |||||||||
| LSN28146171,6 (2.5–10mg/kg, PO) | ↑ | ↓ | ↑ | ↓ | ↓ | ↓ | ↑ | ↓ | ↓ |
| LSN24633596 (0.3–3mg/kg, PO) | ↑ | ↓ | ↑ | — | — | ↓ | — | — | — |
| ADX472731,6 (10–300 mg/kg, PO) | ↑ | ↓ | ↑ | n.s. | ↓ | ↓ | ↑ | ↓ | n.s. |
| CDPPB6,7 (30mg/kg, IP) | ↑ ; n.s. | ↓ | n.s. | — | — | ↓ | — | — | — |
| mGlu2/3 Receptor Antagonists/NAMS (within 4–6h post-dosing) | |||||||||
| LY341495 (antagonist)8,9 (1–10mg/kg, SC) | ↑ | ↓ | ↑ | — | — | ↓ | ↑ | — | — |
| LY3020371 (antagonist)10 (3–10mg/kg, IP) | ↑ | ↓ | — | — | — | ↓ | — | — | — |
| Ro4491533 (NAM)8 (2.5–40 mg/kg, PO) | ↑ | ↓ | ↑ | — | — | ↓ | ↑ | — | — |
| mGlu2/3 Receptor Agonists/PAMS (within 4–6h post-dosing) | |||||||||
| LY379268 (agonist)10,11 (10 mg/kg, PO10; 0.25–1 mg/kg SC11) | n.s. (dark) ↑(light) | n.s. (dark) ↓(light) | — | — | — | ↓ | — | — | — |
| LY354740 (agonist)12 (1–10mg/kg, SC) | n.s. | n.s. | n.s. | n.s. | n.s. | ↓ | ↑ | ↓ | ↓ |
| BINA (PAM)12 (1–40mg/kg, SC) | n.s. | n.s. | — | ↑ | ↓ | ↓ | ↑ | ↓ | ↓ |
| JNJ-42153605 (PAM)13 (3 mg/kg, PO) | n.s. | n.s. | — | — | — | ↓ | n.s. | — | — |
| JNJ-40411813 (PAM)14 (3–30mg/kg, PO) | ↓ | ↑ | — | — | — | ↓ | ↑ | — | — |
| JNJ-40068782 (PAM)15 (3–30mg/kg, PO) | n.s. | n.s. | — | — | — | ↓ | ↑ | — | — |
| THIIC (PAM; 12h post-dosing)16 (10–30mg/kg, PO) | — | ↑ | — | ↑ | — | ↓ | — | — | — |
| mGlu2/3 receptor agonists/PAMS (within 4–6h post-dosing) | |||||||||
| (S)-3,4-dicarboxyphenylglycine17 (5–20mg/kg, IP) | n.s. | n.s. | n.s. | n.s. | n.s. | n.s. | n.s. | n.s. | n.s. |
n.s., not significant; —, not determined; IP, intraperitoneal; SC, subcutaneous; PO, per os (oral).
1Ahnaou, Langlois, Steckler, Bartolome-Nebreda and Drinkenburg (2015), 2Cavas et al. (2013b), 3Harvey et al. (2013), 4Lindemann et al. (2015), 5Holter et al. (2021), 6Gilmour et al. (2013), 7Parmentier-Batteur et al. (2012), 8Ahnaou, ver Donck, and Drinkenburg (2014), 9Feinberg, Schoepp, Hsieh, Darchia, and Campbell (2005), 10Wood et al. (2018), 11Feinberg, Campbell, Schoepp, and Anderson (2002), 12Ahnaou et al. (2009), 13Cid et al. (2012), 14Lavreysen et al. (2015), 15Lavreysen et al. (2013), 16Fell et al. (2011), 17Cavas, Scesa, Martín-López, and Navarro (2017).