Talnetant
Cat. No. :YN320885
CAS No. :174636-32-9
86-020-82000279
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order@ubiochem.com| Product Name: | Talnetant |
| CAS NO.: | 174636-32-9 |
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| Molecular Weight: | 382.45 |
| Molecular Formula: | C₂₅H₂₂N₂O₂ |
| SMILES: | OC1=C(C(N[C@H](C2=CC=CC=C2)CC)=O)C3=C(N=C1C4=CC=CC=C4)C=CC=C3 |
| Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Transportation: | Room temperature in continental US; may vary elsewhere. |
| Description: | Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. in vitro: In vitro studies demonstrated that 53 is a potent functional antagonist of the hNK-3 receptor (reversal of senktide-induced contractions in rabbit isolated iris sphincter muscles and reversal of NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor), while in vivo this compound showed oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced miosis in rabbits) . Talnetant has high affinity for recombinant human NK3 receptors (pKi 8.7) and demonstrates selectivity over other neurokinin receptors (pKi NK2 = 6.6 and NK1<4). In native tissue-binding studies, talnetant displayed high affinity for the guinea pig NK3 receptor (pKi 8.5) . in vivo: Rectal barostat tests were performed on 102 healthy volunteers, r and omized to receive either oral talnetant 25 or 100 mg or placebo over 14-17 days . 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 . Toxicity: Talnetant had no effect on rectal compliance, sensory thresholds or intensity ratings compared with placebo . Clinical trial: Study Of Talnetant Versus Placebo and Risperidone In Schizophrenia. Phase 2 |
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