Roxindole

SKU: orb1701643

Description

Roxindole (EMD 49980) is a dual-acting small molecule that functions as a dopamine autoreceptor agonist, a 5-HT1A receptor agonist, and a serotonin reuptake inhibitor. Its pharmacological profile supports its use in preclinical research for studying psychiatric and neurological conditions, including depression, psychosis, and Parkinson's disease, in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 112192-04-8
• MW: 346.47
• Purity: 99.08% (May vary between batches)
• Formula: C₂₃H₂₆N₂O
• SMILES: OC=1C=CC=2NC=C(C2C1)CCCCN3CC=C(C=4C=CC=CC4)CC3
• Target: Dopamine Receptor,5-HT Receptor,Serotonin Transporter

Bioactivity

• In Vivo:
  Roxindole（EMD 49980） inhibited apomorphine-induced climbing behavior in mice and stereotyped behavior in rats with ED50 of 1.4 mg/kg s.c. and 0.65 mg/kg s.c., respectively, and also inhibited conditioned avoidance responses in rats (ED50 = 1. 5 mg/kg s.c) ;In the paradigm of co-treatment with haloperidol (1 mg/kg per day, orally), Roxindole（EMD 49980） (10 mg/kg per day, orally) did not alter the behavioral hypersensitivity measured after the drug washout phase as compared with the effect of haloperidol alone; if administration of Roxindole（EMD 49980） (10 mg/kg, i.v.) after the drug washout phase induced only weak stereotyped behaviors in haloperidol-hypersensitized rats, Roxindole（EMD 49980） did not induce either desensitization of the presynaptic or supersensitivity of the postsynaptic dopamine D2 receptor; Roxindole (EMD 49980) (1, 3, 10 mg/kg; s.c) inhibits both effects of 8-OH-DPAT (flattened body and forepaw stamping) in normal rats (male Wistar 200-350g) .
• In Vitro:
  Roxindole has high affinity for hD3 as well as hD2 (short isomer) and hD4 (4-repeat isomer) receptors (pKi values of 8.93, 8.55 and 8.23, respectively). In addition, it had a high affinity for the hS-HT1A receptor (pKi = 9.42), but a low affinity for the 5-HT1B and 5-HT1D receptors (pKi values of 6.00 and 7.05, respectively).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dopamine Receptor, Dopamine, DopamineReceptor, 5HTReceptor, 5HT Receptor, 5-HT1A, EMD 49980, Roxindole

Compound Identifiers

PubChem CID

219050