Description

Product Description

Background

Contulakin G is an O-glycosylated invertebrate neurotensin peptide discovered in marine species. Unlike classical neurotensin, Contulakin G has reduced potency at the neurotensin receptor, making it a unique tool to study partial receptor agonism. Its antinociceptive effects have been demonstrated in multiple preclinical models, making it a valuable compound for pain research and neuropharmacology studies.

Chemical Nature and Structure

• Type: Glycosylated neuropeptide

• Sequence: Derived from invertebrate neurotensin homologs

• Modification: O-linked glycosylation

• Receptor Target: Neurotensin receptor (NTSR1)

The glycosylation increases stability and bioavailability in experimental models while reducing full receptor activation, allowing researchers to study receptor partial agonism in a controlled manner.

Research Significance

Contulakin G is essential for:

• Pain and Analgesia Research: Provides antinociceptive effects without full receptor overstimulation.

• Neurotensin Pathway Studies: Helps map receptor-ligand interactions and intracellular signaling.

• Neuroscience Models: Useful in exploring CNS modulation, nociceptive pathways, and behavioral pharmacology.

• Comparative Pharmacology: Allows comparison with mammalian neurotensin for translational studies.

Compared to other neurotensin peptides, Contulakin G provides enhanced selectivity, stability, and unique glycosylation-mediated receptor modulation, offering more nuanced preclinical insights.

Product Specifications

The combination of high purity, glycosylation modification, and GMP-grade manufacturing ensures reproducible and reliable results across multiple preclinical models.

Mechanism of Action & Research Applications

Mechanism of Action

Contulakin G binds to neurotensin receptors (NTSR1) with moderate affinity, acting as a partial agonist. The O-linked glycosylation enhances its resistance to enzymatic degradation, allowing stable receptor engagement.

• NTSR1 Binding: Activates intracellular G-protein signaling while avoiding full receptor overstimulation.

• Antinociceptive Pathway: Modulates neuronal calcium channels and neurotransmitter release, reducing pain perception.

• Neuroprotection: Provides protective effects in CNS neurons through anti-excitotoxic pathways.

Research Applications

1. Pain and Analgesia Studies:

   • Evaluates partial agonism effects on nociceptive signaling.

   • Used in rodent and invertebrate models of acute and chronic pain.

2. Neurotensin Signaling:

   • Helps map NTSR1-mediated pathways in neuronal cultures.

   • Facilitates understanding of receptor desensitization and downstream signaling.

3. Behavioral Pharmacology:

   • Assesses CNS responses to neuropeptide modulation.

   • Investigates changes in locomotion, anxiety, and sensory perception.

4. Comparative Peptide Studies:

   • Useful for cross-species pharmacological comparisons.

   • Supports translational research bridging invertebrate-derived peptides to mammalian systems.

Contulakin G’s unique structure allows the simultaneous study of analgesic efficacy, receptor pharmacology, and neuroprotective mechanisms, making it a versatile tool in neuroscience research.

Side Effects (For Reference in Research Models)

• CNS-related effects: Dose-dependent changes in locomotor activity in rodents.

• Transient receptor modulation: Partial agonism may lead to receptor desensitization over time.

• Solvent and formulation effects: Bioactivity can vary with buffer composition.

• Species variability: Observed effects differ between rodent and invertebrate models.

Proper experimental controls are necessary to ensure reproducibility and interpretability of data.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

Keywords

• Contulakin G CAS 229180-41-0

• O-glycosylated neurotensin peptide

• Antinociceptive neuropeptide research

• Neurotensin receptor partial agonist

• GMP peptide supplier Contulakin G

• Laboratory neuroscience peptide

• Pain modulation peptide

• Preclinical neuropharmacology research

• CNS neuropeptide research

• Contulakin G research use only