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Purity: ≥98%
Talnetant (formerly also known as SB 223412) is a potent and selective NK3 receptor antagonist with ki value of 1.4 nM (hNK-3-CHO); Selectivity studies versus the other neurokinin receptors (hNK-2-CHO and hNK-1-CHO) revealed that Talnetant is about 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 microM. Talnetant has been shown in vitro to be a potent functional antagonist of the hNK-3 receptor (reversing senktide-induced contractions in isolated rabbit iris sphincter muscles and reversing NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor). In vivo, however, this compound has been shown to exhibit oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced behavioral responses in rabbits). Talnetant may be used as a pharmacological tool in animal models of disease to evaluate the pathophysiological and functional role of the NK-3 receptor and to determine the appropriate use of non-peptide NK-3 receptor antagonists for therapeutic purposes, according to the biological data gathered thus far.
| ln Vitro |
Talnetant (SB 223412) (0.1–1 μM) has the ability to decrease the build-up of NKB-induced IP in human NK3 receptor-expressing U-2OS cells[3].
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| ln Vivo |
Talnetant (SB 223412) (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis caused by senktide (25µg, iv) in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits[1].
Talnetant (SB 223412) (i.p., 1-100 mg/kg, 1 h) can decrease haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex, and significantly attenuate "wet dog wagging" behavior induced by senktide in a dose-dependent manner[3].
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| Animal Protocol |
Male Dunkin-Hartley guinea pig
1, 3, 10, 30 or 100 mg/kg Intraperitoneal injection; 1 h |
| References |
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| Molecular Formula |
C25H22N2O2
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|---|---|
| Molecular Weight |
382.4544
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| Exact Mass |
382.17
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| Elemental Analysis |
C, 78.51; H, 5.80; N, 7.32; O, 8.37
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| CAS # |
174636-32-9
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| Related CAS # |
Talnetant hydrochloride; 204519-66-4
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| Appearance |
Solid powder
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| SMILES |
CC[C@@H](C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)O
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| InChi Key |
BIAVGWDGIJKWRM-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C25H22N2O2/c1-2-20(17-11-5-3-6-12-17)27-25(29)22-19-15-9-10-16-21(19)26-23(24(22)28)18-13-7-4-8-14-18/h3-16,20,28H,2H2,1H3,(H,27,29)/t20-/m0/s1
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| Chemical Name |
3-hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide
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| Synonyms |
SB223412; SB-223412; SB 223412; Talnetant
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~261.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00101985 | Completed | Drug: talnetant | Irritable Colon | GlaxoSmithKline | October 2004 | Phase 2 |
| NCT00103727 | Completed | Drug: Talnetant Other: placebo Other: risperidone |
Schizophrenia | GlaxoSmithKline | December 2004 | Phase 2 |
| NCT00300963 | Completed | Drug: Talnetant | Schizophrenia | GlaxoSmithKline | December 2004 | Phase 2 |
| NCT00049946 | Completed | Drug: talnetant Drug: risperidone |
Schizophrenia | GlaxoSmithKline | October 2002 | Phase 2 |
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