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Talnetant

Catalog No. T7549 CAS 174636-32-9

Synonyms: SB 223412

Talnetant (SB 223412) is a selective, competitive, brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission

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Talnetant, CAS 174636-32-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 132.00
25 mg	In stock	$ 279.00
50 mg	In stock	$ 515.00
100 mg	In stock	$ 783.00
1 mL * 10 mM (in DMSO)	In stock	$ 145.00

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Purity: 98%

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Description	Talnetant (SB 223412) is a selective, competitive, brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission
Targets&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[1].

Synonyms	SB 223412
Molecular Weight	382.45
Formula	C25H22N2O2
CAS No.	174636-32-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (261.47 mM)

References and Literature

1. Dawson L A , Cato K J , Scott C , 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[J]. Neuropsychopharmacology, 2008, 33(7):1642-1652. 2. Giuseppe A. M. Giardina,,‡, Luca F. Raveglia,‡, Mario Grugni,‡, 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]. Journal of Medicinal Chemistry, 1999, 42(6):1053-1065.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Bioactive Compound Library

Related Products

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Eledoisin Kassinin acetate(63968-82-1 free base) NK3R-IN-1 (R)-CJ 11974 Casopitant mesylate [Sar9,Met(O2)11]-Substance P acetate Neurokinin A(4-10) Physalaemin

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Keywords

Talnetant 174636-32-9 GPCR/G Protein Neuroscience Neurokinin receptor schizophrenia NK receptor SB-223412 Inhibitor hNK-2 Neurokinin Receptor Tachykinin receptor NK3 receptor SB223412 SB 223412 inhibit inhibitor

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