Talnetant

SKU: orb1299718

Description

Talnetant (SB-223412) is a selective, brain-penetrant antagonist of the neurokinin 3 (NK3) receptor. It is used in research to investigate the modulation of dopaminergic pathways, with applications in studying psychiatric and neurological conditions in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 174636-32-9
• MW: 382.45
• Purity: 98.00% (May vary between batches)
• Formula: C₂₅H₂₂N₂O₂
• SMILES: CC[C@H](NC(=O)c1c(O)c(nc2ccccc12)-c1ccccc1)c1ccccc1
• Target: Neurokinin receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.46 mM);DMSO:100 mg/mL (261.47 mM)

Bioactivity

• Target IC50:
  NK-3-CHO cells (human):1.4 nM(ki)
• In Vivo:
  Talnetant competitively antagonized neurokinin B (NKB)-induced responses at the human recombinant receptor in both calcium and phosphoinositol second messenger assay systems (pA2 of 8.1 and 7.7, respectively). In guinea pig brain slices, talnetant antagonized NKB-induced increases in neuronal firing in the medial habenula (pKB = 7.9) and senktide-induced increases in neuronal firing in the substantia nigra pars compacta (pKB = 7.7) with no diminution of maximal agonist efficacy, suggesting competitive antagonism at native NK3 receptors. Talnetant (3-30 mg/kg i.p.) significantly attenuated senktide-induced 'wet dog shake' behaviors in the guinea pig in a dose-dependent manner. Microdialysis studies demonstrated that acute administration of talnetant (30 mg/kg i.p.) produced significant increases in extracellular dopamine and norepinephrine in the medial prefrontal cortex and attenuated haloperidol-induced increases in nucleus accumbens dopamine levels in the freely moving guinea pigs.

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

inhibit, NK3, NK3 receptor, NK receptor, Neurokinin receptor, Neurokinin Receptor, Neurokininreceptor, hNK-2, Inhibitor, SB223412, SB-223412, SB 223412, schizophrenia, Talnetant, Tachykinin receptor

Compound Identifiers

PubChem CID

5311424