Octreotide pamoate | CAS No. 135467-16-2

Description

Product Description

Octreotide pamoate (CAS No. 135467-16-2) is a synthetic octapeptide derivative of somatostatin, formulated as the pamoate salt to improve stability and pharmacological properties. Somatostatin is a naturally occurring peptide hormone that regulates endocrine and exocrine secretions, but its short half-life has limited its therapeutic use. Octreotide, as a long-acting analogue, overcomes this challenge and provides a valuable tool for research in endocrinology, oncology, and metabolic disorders.

Background and Discovery

Somatostatin plays a crucial role in inhibiting hormone secretion, including growth hormone (GH), insulin, glucagon, and gastrointestinal peptides. However, its half-life of less than 3 minutes made it unsuitable for practical therapeutic use. Octreotide, designed as a stable analogue, retains the inhibitory functions of natural somatostatin but with enhanced half-life, receptor selectivity, and potency. The pamoate formulation further enhances its pharmacokinetics, allowing for controlled release and extended biological activity in vivo, making it a critical compound in long-term disease models.

Structural Features

Octreotide pamoate maintains the core cyclic structure of somatostatin, but substitutions confer:

• Increased resistance to enzymatic degradation

• High binding affinity to somatostatin receptors SSTR2, SSTR3, and SSTR5

• Improved half-life compared to endogenous somatostatin

The pamoate salt contributes to low solubility and sustained release, enabling its use in extended-release depot formulations for experimental studies.

Research Significance

Octreotide pamoate is extensively applied in studies of hormone-dependent diseases, cancer biology, apoptosis mechanisms, and metabolic regulation. Research shows that it can:

• Suppress growth hormone secretion, making it vital in acromegaly models

• Inhibit tumor growth by promoting apoptosis in receptor-positive cancer cells

• Reduce insulin and glucagon release, enabling research on diabetes and metabolic syndrome

• Modulate gastrointestinal activity, relevant in digestive disease models

Applications in Disease Research

1. Acromegaly Research

   • Octreotide pamoate serves as a model for studying GH hypersecretion and endocrine regulation.

   • Used in long-term models of pituitary adenomas and hormone-dependent disorders.

2. Oncology

   • Demonstrates direct antitumor effects by inducing apoptosis in somatostatin receptor-expressing tumors.

   • Applied in models of neuroendocrine tumors, pancreatic cancer, and gastrointestinal malignancies.

3. Apoptosis and Cell Signaling

   • Promotes caspase activation and mitochondrial pathway apoptosis.

   • Provides insights into peptide-mediated regulation of tumor cell death.

4. Endocrine Disorders

   • Used to model the suppression of insulin, glucagon, gastrin, and vasoactive intestinal peptide (VIP).

   • Supports exploration of diabetes and hormonal dysregulation mechanisms.

5. Neuroendocrinology

   • Helps understand the role of somatostatin analogues in regulating neurotransmitter secretion and neuronal activity.

Through its diverse applications, Octreotide pamoate has become a cornerstone tool in endocrine and oncology research.

Product Specifications

Extended Notes

• Pamoate salt formulation ensures sustained release properties.

• Useful in animal models requiring long-term exposure.

• Suitable for combination therapy research with chemotherapy or radiotherapy.

Mechanism of Action

Octreotide pamoate is a somatostatin receptor agonist that selectively binds to SSTR2, SSTR3, and SSTR5.

Receptor Binding and Signal Transduction

• Activation of Gi proteins reduces intracellular adenylate cyclase activity, leading to decreased cAMP levels.

• This cascade results in inhibition of hormone secretion from endocrine cells.

• In tumor cells, signaling induces apoptosis and antiproliferative responses.

Hormonal Suppression

• Growth Hormone (GH): Octreotide strongly inhibits GH release, relevant in acromegaly.

• Insulin and Glucagon: Reduces secretion, altering glucose metabolism.

• Gastrointestinal Hormones: Inhibits gastrin, secretin, and VIP, modulating GI activity.

Antitumor Effects

• Induces apoptosis via mitochondrial and caspase-dependent pathways.

• Inhibits angiogenesis by reducing VEGF and other pro-angiogenic signals.

• Blocks tumor cell proliferation in receptor-positive malignancies.

Pharmacokinetic Role of Pamoate

• Provides low solubility, ensuring slow absorption and extended half-life.

• Suitable for depot administration in research requiring long-term peptide exposure.

Role in Combination Research

• Enhances efficacy of chemotherapeutic agents through synergistic apoptosis induction.

• Used with radiotherapy in tumor models to improve outcomes.

  

Side Effects

While Octreotide pamoate is a research compound, studies reveal potential side effects in preclinical models:

Endocrine and Metabolic Effects

• Hypoglycemia or hyperglycemia due to insulin and glucagon modulation.

• Altered lipid metabolism in long-term studies.

Gastrointestinal Effects

• Nausea, diarrhea, abdominal discomfort reported in experimental animals.

• Reduced gastric motility and altered gut microbiota composition.

Cardiovascular Effects

• Possible bradycardia and arrhythmias observed in sensitive models.

• Reduction in splanchnic blood flow.

Tumor-Specific Responses

• Not all tumors respond; resistance may develop with prolonged exposure.

• Some receptor-negative tumors show negligible response.

Laboratory Safety Considerations

• Strict handling protocols required for peptide research compounds.

• Store under recommended conditions to preserve stability.

Disclaimer

Octreotide pamoate is provided strictly for research use only. It is not intended for human therapeutic use, diagnosis, or clinical application.

Keywords

Octreotide pamoate, CAS 135467-16-2, somatostatin analogue, SMS 201-995 pamoate, acromegaly research, endocrine peptide, SSTR agonist, antitumor peptide, apoptosis inducer, cAMP inhibitor.

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