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MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB)[1][2][3]. | [in vivo]
MIF-1 TFA (Melanostatin, 1 mg/kg; i.p.; once, for 1 hour; male Wistar rats) modulates the analgesic effects, including stress-induced analgesia (SIA)[1].
MIF-1 TFA (Melanostatin, 1 mg/kg; i.p.; daily, for 8 weeks; Sprague-Dawley rats) attenuates spiroperidol-induced impairment of development of striatal dopamine D2 receptors in rats[3]. | Animal Model: | Male Wistar rats[1] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; once, for 1 hour | | Result: | Decreased the analgesic effect. Increased the pain threshold for at least 1 h. |
| Animal Model: | Sprague-Dawley rats[3] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; daily, for 8 weeks | | Result: | Attenuated the ontogenic impairment of striatal D2 receptors that was produced by spiroperidol (HY-B1371) treatment. |
| [References]
[1] Bocheva A, et, al. Antiopioid properties of the TYR-MIF-1 family. Methods Find Exp Clin Pharmacol. 2004 Nov;26(9):673-7. DOI:10.1358/mf.2004.26.9.872564
[2] Valentijn JA, et, al. Melanostatin (NPY) inhibited electrical activity in frog melanotrophs through modulation of K+, Na+ and Ca2+ currents. J Physiol. 1994 Mar 1;475(2):185-95. DOI:10.1113/jphysiol.1994.sp020060
[3] Saleh MI, et, al. MIF-1 attenuates spiroperidol alteration of striatal dopamine D2 receptor ontogeny. Peptides. 1989 Jan-Feb;10(1):35-9. DOI:10.1016/0196-9781(89)90072-7 |
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