PT-141 (Bremelanotide) overview:
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PT-141, also known by its chemical name Bremelanotide, is a synthetic peptide developed from the melanocortin-stimulating hormone (MSH) analog. It was initially studied for its potential in tanning and skin pigmentation due to its melanocortin receptor activity, but subsequent research revealed its unique effect on sexual arousal and erectile function, leading to its primary research focus on sexual dysfunction disorders. PT-141 has shown promise in stimulating sexual desire and improving sexual performance through central nervous system activation rather than direct vascular effects, distinguishing it from traditional treatments like PDE5 inhibitors (e.g., sildenafil).
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Molecular Structure and Properties
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Molecular Formula: C50H68N14O10
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Molecular Weight: 1025.2 g/mol
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Peptide Sequence: Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-OH
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CAS Number: 189691-06-3
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PT-141 is a cyclic heptapeptide lactam analog of α-MSH (alpha-melanocyte-stimulating hormone). The synthetic modification includes the substitution of certain amino acids, enhancing its stability and selectivity toward melanocortin receptors.
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Mechanism of Action
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PT-141 acts as a potent and selective agonist of the melanocortin receptors, particularly MC1R and MC4R, which are primarily expressed in the brain and play critical roles in sexual arousal and appetite regulation.
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1. Binding to Melanocortin Receptors:
PT-141 binds to MC4R receptors in the central nervous system (CNS), which are primarily located in the hypothalamus. The activation of these receptors triggers a cascade of intracellular signaling pathways.
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2. cAMP Pathway Activation:
Upon binding, PT-141 activates the adenylate cyclase enzyme, leading to an increase in intracellular cyclic adenosine monophosphate (cAMP). This elevation in cAMP stimulates the release of neurotransmitters involved in sexual arousal, such as dopamine and oxytocin.
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3. Enhanced Sexual Arousal and Performance:
The increased activity of MC4R and the subsequent release of neurotransmitters result in enhanced sexual desire and arousal. Unlike PDE5 inhibitors that act on vascular function to improve blood flow to erectile tissue, PT-141 works at the neurological level, making it effective for both male erectile dysfunction (ED) and female sexual arousal disorder (FSAD).
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Pharmacokinetics
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Administration: Typically administered via subcutaneous injection
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Onset of Action: Effects are typically observed within 30 to 60 minutes post-injection
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Duration of Action: Lasts between 6 to 12 hours, depending on dosage and individual response
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Metabolism: Primarily metabolized in the liver through proteolytic cleavage
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Excretion: Excreted primarily through renal pathways
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Potential Research Applications
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1. Male Sexual Dysfunction: PT-141 has shown efficacy in improving erectile function in cases of psychogenic, neurogenic, and vasculogenic erectile dysfunction.
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2. Female Sexual Dysfunction: PT-141 has been investigated for hypoactive sexual desire disorder (HSDD) and female sexual arousal disorder (FSAD).
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3. Appetite and Metabolism Regulation: MC4R is also involved in appetite control, making PT-141 a potential target for research into obesity and metabolic disorders.
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4. Neurological and Endocrine Disorders: PT-141’s interaction with melanocortin receptors presents possible avenues for studying its effects on mood regulation, stress response, and endocrine balance.
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Side Effects and Safety Profile
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While PT-141 has demonstrated effectiveness in sexual dysfunction research, some side effects have been reported, including:
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Nausea
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Flushing
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Headache
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Increased blood pressure
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Injection site reactions
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**For Research Use Only.
**Not for Human Consumption.
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PT-141 is intended solely for research purposes in a laboratory setting. It is not approved for human use, and any use outside of research environments is prohibited. The information provided here is for educational and informational purposes only and does not constitute medical advice or endorsement of any kind.