Description
Nasal Spray Format
This product is a liquid research preparation at a concentration of 1 mg/mL (10 mg total peptide in 10 mL), supplied with a metered nasal‑spray pump for research applications where intranasal administration is the study route. The intranasal route offers partial access to CNS tissue via the olfactory and trigeminal pathways, bypassing first‑pass hepatic metabolism.
Intranasal pharmacology varies substantially by molecule. Small, lipophilic peptides may achieve meaningful CNS concentrations; larger or highly hydrophilic peptides often do not. Peer‑reviewed data for intranasal PK is referenced below where available.
Parent Compound: PT-141 (Bremelanotide)
PT‑141 (bremelanotide, Vyleesi®) is a cyclic heptapeptide melanocortin‑receptor agonist centrally acting on MC4R. It is FDA‑approved (2019) as a subcutaneous autoinjector for hypoactive sexual desire disorder (HSDD) in premenopausal women.
Intranasal Research Context
- Diamond et al., Journal of Sexual Medicine (2004, 2012): early intranasal PT‑141 pilot studies in ED at 7.5–20 mg intranasal doses.
- The intranasal program was discontinued primarily due to dose‑dependent transient blood‑pressure increases that were more difficult to control vs. SC dosing.
- Final commercial product (Vyleesi®) is an SC autoinjector at 1.75 mg.
Preparation Details
- Total peptide: 10 mg PT‑141
- Volume: 10 mL
- Concentration: 1 mg/mL
- Format: Metered nasal‑spray pump
- Source: Solid‑phase synthesis; ≥98% HPLC, reconstituted in preservative‑containing sterile saline buffer
Known Side Effects — PT-141 Class
- Nausea (most common AE across programs)
- Flushing, headache
- Transient systolic BP increase (reason intranasal program was deprioritized for clinical development)
- Focal hyperpigmentation with repeated dosing (reversible)
- Contraindicated in uncontrolled hypertension or cardiovascular disease per Vyleesi® label
Storage & Handling
- Lyophilized (unreconstituted) vials: store at −20°C long‑term; short‑term 2–8°C acceptable.
- After reconstitution with bacteriostatic or sterile water: store at 2–8°C; use within 14–28 days per standard peptide stability guidance.
- Protect from light, heat, and repeated freeze‑thaw cycles. Handle in a sterile laboratory environment.
Certificate of Analysis
A Certificate of Analysis (COA) confirming identity and purity by HPLC / MS is available upon request. Contact Lonestar Peptides for lot‑specific documentation.
Summaries reference peer‑reviewed preclinical and clinical literature available as of early 2025. Newer findings may not be reflected. Researchers should consult current literature and conduct their own due diligence. Lonestar Peptides makes no claim of therapeutic benefit.
