Table 6.
Overview of anticonvulsant effects of ghrelin-R ligands in experimental epilepsy models. D1R: Dopamine 1 receptor; i.v.: intravenous; i.h.: intrahippocampal; IHKA: intrahippocampal kainic acid; i.p.: intraperitoneal; KA: kainic acid; min: minute; pilo: pilocarpine; Ref: reference; SP: [D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P.
| Compound | Dose | Administration Regimen |
Anticonvulsant | Animal Model | Ref |
|---|---|---|---|---|---|
| Agonists | |||||
| Macimorelin | 0.33 mg/kg | i.p 10 min prior to pilo |
no | Pilocarpine i.p. rat model |
[31,115] |
| Macimorelin | 5 mg/kg | i.p., 20 min prior to stimulus | yes | Acute 6- Hzmouse model |
[124] |
| Macimorelin | 5 mg/kg | i.v. infusion | yes | Fully kindled 6-Hz mouse model | [124] |
| Macimorelin | 5 mg/kg | 30 min prior to SKF | yes | D1R-mediated kindling mouse model | [125] |
| Macimorelin | 5 mg/kg | 14 days, 2×/day | yes | IHKA mouse model |
[126] |
| Capromorelin | 0.01–10 µM | i.h. infusion 120 min prior to pilo | yes | Pilocarpine i.h. infusion rat model |
[116] |
| Hexarelin | 0.33 mg/kg | i.p. 10 min prior to pilo |
yes | Pilocarpine i.p. rat model |
[115] |
| Hexarelin | 0.33 mg/kg | i.p. 10 min prior to KA |
no | KA i.p. rat model |
[115] |
| Antagonists | |||||
| EP-80317 | 0.33 mg/kg | i.p. 10 min prior to pilo |
yes/no | Pilocarpine i.p. rat model |
[115] |
| EP-80317 | 0.33 mg/kg | i.p. 10 min prior to KA |
no | KA i.p. rat model |
[115] |
| EP-80317 | 0.33 mg/kg | i.p. 10–15 min prior to stimulus | yes | 6-Hz repeated mouse model |
[131] |
| JMV-2959 | 0.33 mg/kg | i.p. 10 min prior to pilo |
no | Pilocarpine i.p. rat model |
[115] |
| JMV-2959 | 10 mg/kg | i.p. 20 min prior to stimulus | no | Acute 6-Hz mouse model |
[124] |
| JMV-2959 | 10 mg/kg | i.v. infusion | no | 6-Hz fully kindled mice |
[124] |
| JMV-2959 | 5 mg/kg | i.p. 30 min prior to SKF |
no | D1R-mediated kindling mouse model | [125] |
| D-Lys-3-GHRP-6 | 1–100 µg | i.c.v. 30 min prior to stimulus |
no | Amygdala kindling rat model | [133] |
| Inverse Agonists | |||||
| A778193 | 0.01–10 µM | i.h. infusion 120 min prior to pilo |
yes | Pilocarpine i.h. infusion rat model |
[116] |
| SP | 0.01–10 µM | i.h. infusion 120 min prior to pilo |
yes | Pilocarpine i.h. infusion rat model |
[116] |
| Biased Agonists | |||||
| YIL781 | 5 mg/kg | i.p. 30 min prior to SKF |
no | D1R-mediated kindling mouse model | [125] |