Bioactivity | Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities[1][2][3]. |
In Vivo | Roxindole hydrochloride inhibits apomorphine-induced climbing in mice and stereotyped behavior in rats with ED50s of 1.4 mg/kg s.c. and 0.65 mg/kg s.c., respectively, and inhibits conditioned avoidance response in rats (ED50=1.5 mg/kg s.c.)[1].Roxindole hydrochloride (1, 3, 10 mg/kg; s.c) inhibits both effects of 8-OH-DPAT (flat body and forepaw treading) in normal rats (male Wistar 200-350g)[3]. |
Name | Roxindole hydrochloride |
CAS | 108050-82-4 |
Formula | C23H27ClN2O |
Molar Mass | 382.93 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
Reference | [1]. Bartoszyk GD, Harting J, Minck KO. Roxindole: psychopharmacological profile of a dopamine D2 autoreceptor agonist. J Pharmacol Exp Ther. 1996;276(1):41-48. [2]. Wetzel H, et al. Roxindole, a dopamine autoreceptor agonist, in the treatment of positive and negative schizophrenic symptoms. Am J Psychiatry. 1994;151(10):1499-1502. [3]. Maj J, et al. Roxindole, a dopamine autoreceptor agonist with a potential antidepressant activity. II. Effects on the 5-hydroxytryptamine system. Pharmacopsychiatry. 1997;30(2):55-61. [4]. Prehn JH, et al. Effects of serotonergic drugs in experimental brain ischemia: evidence for a protective role of serotonin in cerebral ischemia. Brain Res. 1993;630(1-2):10-20. |