1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Talnetant

Talnetant (Synonyms: SB 223412)

Cat. No.: HY-14552 Purity: 99.43%
Handling Instructions

Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, 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.

For research use only. We do not sell to patients.

Talnetant Chemical Structure

Talnetant Chemical Structure

CAS No. : 174636-32-9

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10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
10 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 677 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, 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. IC50 Value: 1.4 nM (hNK-3-CHO binding Ki) [1] Target: NK3 receptor 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) [1]. 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) [3]. in vivo: Rectal barostat tests were performed on 102 healthy volunteers, randomized to receive either oral talnetant 25 or 100 mg or placebo over 14-17 days [2]. 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 [3]. Toxicity: Talnetant had no effect on rectal compliance, sensory thresholds or intensity ratings compared with placebo [2]. Clinical trial: Study Of Talnetant Versus Placebo And Risperidone In Schizophrenia. Phase 2

Clinical Trial
Molecular Weight

382.45

Formula

C₂₅H₂₂N₂O₂

CAS No.

174636-32-9

SMILES

OC1=C(C(N[[email protected]](C2=CC=CC=C2)CC)=O)C3=C(N=C1C4=CC=CC=C4)C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (261.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6147 mL 13.0736 mL 26.1472 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.43%

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Keywords:

TalnetantSB 223412SB223412SB-223412Neurokinin ReceptorNK receptorInhibitorinhibitorinhibit

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Talnetant
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