| Description | Orotirelin(CG 3509), a thyrotropin-releasing hormone analog, reversed pentobarbital-induced sleep time.Orotirelin may be beneficial in animals with focal cerebral ischemia. |
| In vivo | CG 3509 (2 μg; intrathecal administration; twice daily for 5 days; adult rats) on wet-dog shake (WDS) and forepaw-licking (FPL) behaviours and spinal cord TRH and indoleamine levels and choline acetyltransferase (ChAT) activity was examined. A rapid behavioural tolerance developed to repeated intrathecal injections of CG 3509; WDS and FPL behaviours were reduced by 57% and 34%, respectively, following the fifth injection and remained reduced at the ninth injection. Repeated CG 3509 administration selectively elevated ChAT activity and the level of 5-hydroxytryptamine (5-HT) in the ventral but not in the dorsal horn of the spinal cord, while 5-hydroxy indole acetic acid and TRH levels were unaltered in either region.[2] |
| Synonyms | CG 3509, Orotireline |
| molecular weight | 389.37 |
| Molecular formula | C16H19N7O5 |
| CAS | 62305-86-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (128.41 mM) |
| References | 1. Fone KC, et al. Involvement of catecholaminergic neurones and alpha-adrenoceptors in the wet-dog shake and forepaw licking behaviour produced by the intrathecal injection of an analogue of thyrotrophin-releasing hormone (CG 3509). Neuropharmacology. 1987 Aug;26(8):1147-55. 2. Fone KC, et al. Spinal effects of chronic intrathecal administration of the thyrotrophin-releasing hormone analogue (CG 3509) in rats. Brain Res. 1988 Jul 5;455(1):157-61. 3. Fone KC, et al. Involvement of 5-HT2 receptors in the behaviours produced by intrathecal administration of selected 5-HT agonists and the TRH analogue (CG 3509) to rats. Br J Pharmacol. 1989 Mar;96(3):599-608. 4. Sharp T, et al. Analeptic effects of centrally injected TRH and analogues of TRH in the pentobarbitone-anaesthetized rat. Neuropharmacology. 1984 Mar;23(3):339-48. |