Mianserin (hydrochloride)

Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy^{[1][2][3][4][5]}. In Vitro:Mianserin hydrochloride exhibits 12- and 18-fold higher affinity for human κ-opioid receptors than for μ-opioid receptors and δ-opioid receptors, respectively, with a K_i of 1.7 ± 0.3 μM for κ-opioid receptors^[1].
Mianserin hydrochloride selectively activates human κ-opioid receptors in CHO/KOP cells to stimulate [³⁵S]GTPγS binding with an EC₅₀ of 0.53 ± 0.05 μM, with no activity at μ-, δ-opioid receptors, or in untransfected CHO cells^[1].
Mianserin hydrochloride (1 μM, 10-120 min) stimulates ERK1/2 phosphorylation in CHO/KOP cells via κ-opioid receptors with an EC₅₀ of 1.5 ± 0.3 μM, peaking at 10 min and remaining elevated for up to 120 min^[1].
Mianserin hydrochloride (0.1-30 μM; 15 min) stimulates ERK1/2 phosphorylation in C6 rat glioma cells via endogenous κ-opioid receptors, with an EC₅₀ of 1.6 ± 0.3 μM^[1].
Mianserin hydrochloride (1 μM; 10-120 min) stimulates CREB phosphorylation in CHO/KOP cells and C6 rat glioma cells via κ-opioid receptors, with a peak 2-fold increase at 30 min in CHO/KOP cells^[1].
Mianserin hydrochloride selectively activates endogenous κ-opioid receptors in rat striatum and nucleus accumbens membranes to stimulate ³⁵S]GTPγS binding, with EC₅₀ values of 0.70 ± 0.05 μM and 0.39 ± 0.06 μM, respectively^[1].
Mianserin hydrochloride (10 μM; 10 min) inhibits p38 MAPK and ERK1/2 phosphorylation in primary mouse striatal and hippocampal neurons induced by dynorphin^[1].
Mianserin hydrochloride (60 min) potently inhibits specific [³H]octopamine binding to locust Locusta migratoria neuronal octopamine receptors with a K_i of 1.20 ± 0.27 nM^[3].
Mianserin hydrochloride inhibits cyclic AMP accumulation mediated by histamine H1 with a K_i of 0.003 μM^[5]. In Vivo:Mianserin hydrochloride (0.12-0.48 μmol/kg; i.p.; single dose) significantly reduces aggressive behavior in male CD1 mice during social encounters in a neutral cage, with minor effects on social and exploratory behaviors in the home cage at 0.48 μmol/kg^[2].
Mianserin hydrochloride (0.12-1.92 μmol/kg; p.o.; daily; 12-16 days) administered chronically significantly enhances social investigation in male CD1 mice during social encounters in both home and neutral cages at 0.12 μmol/kg, while 0.12 μmol/kg and 0.48 μmol/kg doses increase digging behavior in the neutral cage^[2].
Mianserin hydrochloride (30-40 mg/kg; i.p.; single dose, 30 minutes before testing) increases electroconvulsive threshold and potentiates the anticonvulsant action of select antiepileptics^[4].