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Roxindole hydrochloride

Names

[ CAS No. ]:
108050-82-4

[ Name ]:
Roxindole hydrochloride

[Synonym ]:
5-hydroxy-3-[4-(1,2,3,6-tetrahydro-4-phenyl-1-pyridyl)butyl]indole hydrochloride
3-[4-(4-Phenyl-3,6-dihydro-2H-pyridin-1-yl)-butyl]-1H-indol-5-ol
hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter

[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H27ClN2O

[ Molecular Weight ]:
382.92600

[ Exact Mass ]:
382.18100

[ PSA ]:
39.26000

[ LogP ]:
5.72540

Related Compounds