Talnetant hydrochloride
Based on 3 publication(s) in Google Scholar
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies.
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- CAS. Nr.: 204519-66-4
- Formel: C25H23ClN2O2
- Molecular Weight:418.92
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Talnetant hydrochloride
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Biologische Aktivität
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NK3R |
Talnetant (SB 223412) hydrochloride (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Dunkin-Hartley guinea pig[3]
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Dosage:1, 3, 10, 30 or 100 mg/kg
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Administration:Intraperitoneal injection; 1 h
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Result:Showed a significant attenuation of wet dog shake (WDS) behavior from 31.1 to 16.7 at 30 mg/kg.
Significantly increased extracellular DA levels to 238% and NE levels to 227.1%, without affecting 5-HT levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 204519-66-4
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Molecular Weight 418.92
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Formel C25H23ClN2O2
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SMILES
OC1=C(C(N[C@H](C2=CC=CC=C2)CC)=O)C3=C(N=C1C4=CC=CC=C4)C=CC=C3.[H]Cl
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Synonyms
SB 223412 hydrochloride; SB 223412-A
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
Reinheit & Dokumentation
Verweise
[1]. Giardina GA, et al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412). J Med Chem. 1999 Mar 25;42(6):1053-65. [Content Brief]
[2]. Houghton LA, et al. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterol Motil. 2007 Sep;19(9):732-43. [Content Brief]
[3]. Dawson LA, et al. In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Talnetant hydrochloride Related Classifications
HY-14552A Related Classifications
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