Senktide is a NK3 tachykinin receptor agonist. It was shown to induce bronchoconstriction in guinea pig lungs.
- Product Specifications
| Item | Description |
|---|---|
| Catalog No. | 123592 |
| Product Name | Neurokinin-3 (NK3) Receptor Agonist: [Succinyl-Asp6, NMePhe8]-Substance P (6-11), Senktide |
| Synonyms | [Succinyl-Asp6, NMePhe8]-Substance P (6-11), Senktide |
| English Name | [Succinyl-Asp6, NMePhe8]-Substance P (6-11), Senktide |
| English Synonyms | [Suc-Asp6, Me-Phe8] Substance P |
| CAS No. | 106128-89-6 |
| Sequence (One-letter Code) | Suc-DF-(NMe)F-GLM-CONH₂ |
| Sequence (Three-letter Code) | Suc-Asp-Phe-(NMe)Phe-Gly-Leu-Met-CONH₂ |
| Number of Amino Acids | 6 |
| Molecular Formula | C₄₀H₅₅O₁₁N₇S₁ |
| Average Molecular Weight | 841.97 |
| Exact Molecular Weight | 841.37 |
| Isoelectric Point (pI) | – |
| Net Charge at pH 7.0 | –1 |
| Average Hydrophobicity | –1.02 |
| Hydrophobicity Index | 1.23 |
| Appearance | White powder, solid |
| Solubility | – |
| Source | Synthetic; for scientific research use only, not for human use |
| Purity | 95%, 98% |
| Salt Form | TFA, Acetate, HCl, or others upon request |
| Delivery Time | 2–3 weeks |
| Storage Conditions | –20 °C to –80 °C |
Senktide is an NK3 tachykinin receptor agonist. It has been shown to induce bronchoconstriction in guinea pig lungs.
The tachykinin receptor family has recently attracted considerable attention due to the potential of tachykinin NK3 receptor antagonism in the treatment of schizophrenia. However, critical differences in tachykinin NK3 receptors among rats, mice, and humans make rodents suboptimal models for testing the antagonistic effects on this receptor. This situation has led researchers to shift toward gerbils and guinea pigs for testing tachykinin NK3 receptor activity. Since these species are much less commonly used experimental animals compared with rodents, there is currently a relative lack of in vivo models for tachykinin NK3 receptor activation. The present study systematically characterizes the locomotor activity induced by the tachykinin NK3 receptor agonist Senktide.
Experimental results showed that intracerebroventricular administration of Senktide produced dose-dependent hyperlocomotion in the range of 0.06 nmol to the highest tested dose of 0.6 nmol. The locomotor effect induced by 0.1 nmol Senktide could be blocked by the following antagonists: the tachykinin NK3 receptor antagonists SB222200 (intraperitoneal, 10 and 30 mg/kg) and Talnetant (SB223412; intraperitoneal, 10 and 30 mg/kg), as well as Osanetant (SR142801; intraperitoneal, 10 and 30 mg/kg) formulated with vitamin E and Glycofurol. Senktide-induced activity could also be reversed by the antipsychotic drugs haloperidol (oral, 0.3 and 1 mg/kg) and risperidone (oral, 1 mg/kg), but not by the serotonin 5HT2a/c receptor antagonist MDL100907 (oral, 0.1, 0.3, and 1 mg/kg). Interestingly, when the tachykinin NK1 receptor antagonist aprepitant (oral, 1, 3, and 10 mg/kg) was co-administered, locomotor hyperactivity induced by 0.03 nmol Senktide was enhanced.
The study demonstrates that Senktide-induced hyperlocomotion in gerbils is a specific NK3 receptor–mediated behavior. This model is suitable for evaluating the activity of novel compounds on tachykinin NK3 receptors.
Senktide is a potent and selective neurokinin-3 (NK3) receptor agonist (EC₅₀ = 0.5–3 nM). It shows much weaker activity on NK1 receptors (EC₅₀ = 35 μM). Senktide holds promise for use in research on neurological disorders.
In Vitro Studies
The selective NK3 receptor agonist Senktide excited 24 out of 31 dopaminergic neurons in the substantia nigra pars compacta in a concentration-dependent manner. The effective concentration range was 3–3000 nM. The average EC₅₀ was 41.2 ± 9 nM (n = 5).
In Vivo Studies
The selective NK3 receptor agonist Senktide excited 24 out of 31 dopaminergic neurons in the substantia nigra pars compacta in a concentration-dependent manner. The effective concentration range was 3–3000 nM. The average EC₅₀ was 41.2 ± 9 nM (n = 5).
Methylated Peptides
Also known as methyl-labeled peptides, methylation modification is one of the most prominent post-translational modifications (PTMs) in terms of biological and physicochemical properties. Methylation is involved in nearly all cellular processes and plays important regulatory roles. It is a covalent process in which methyltransferases catalyze the transfer of a methyl group to specific amino acid residues of proteins. Methylation is a reversible modification, with demethylases catalyzing demethylation. It can occur on at least nine of the 20 common amino acids (Met, Cys, Lys, Arg, His, Gln, Asn, Glu, and Asp), but is most commonly found on the side chains of lysine (Lys) and arginine (Arg). Methylation is widely involved in regulating cellular processes such as transcription, cell division, and differentiation.
Histone lysine methylation carries diverse biological functions, including stem cell maintenance and differentiation, X-chromosome inactivation, transcriptional regulation, and DNA damage responses, mainly by influencing chromatin compaction and repressing gene expression. Histone arginine methylation plays an important role in transcriptional regulation and affects multiple physiological processes, including DNA repair, signal transduction, cell development, and carcinogenesis. Therefore, [Company name] has developed methylation-modified peptide technology to support scientists in PTM research.
Methylation Modifications (Me1, Me2, Me3)
Using high-quality raw materials such as Fmoc-Lys(Me,Boc)-OH, Fmoc-Lys(Me2)-OH, Fmoc-Lys(Me3)-OH·HCl, Fmoc-Arg(Me,Pbf)-OH, Fmoc-Arg(Me)2-OH·HCl (asymmetrical), and Fmoc-Arg(Me)2-OH·HCl (symmetrical), peptides with Lys and Arg methylation modifications are synthesized via Fmoc solid-phase synthesis. The products are purified by HPLC. Final products are supplied with mass spectra and HPLC chromatograms for purity analysis.
Samples and further technical data can be provided upon request.
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