PT-141
sexual health research
MOLECULAR FORMULA
C50H68N14O10
MOLECULAR WEIGHT
1025.2 U
RESEARCH CATEGORY
SEXUAL HEALTH
RESEARCH DATA
PEER REVIEWED
PT-141, known as Bremelanotide, is a synthetic cyclic heptapeptide with the full chemical name N-acetyl-L-norleucyl-L-aspartyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-lysine lactam. Structurally, it comprises seven amino acids (Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys) arranged in a macrocyclic ring, formed by a lactam bridge between the aspartic acid (Asp) and lysine (Lys) side chains, with an acetyl group capping the N-terminus. Its molecular weight is approximately 1025.2 Da, reflecting a compact yet potent configuration designed to mimic and enhance melanocortin receptor agonism, distinguishing it from its linear predecessor, Melanotan II.
PT-141 (Bremelanotide) is a synthetic peptide made of seven amino acids arranged in a ring shape. This special structure helps it work effectively with certain receptors in the body. It weighs about 1025.2 Da and was designed to be an improved version of an earlier compound called Melanotan II.
PT-141 is most prominently known as Bremelanotide, its clinical designation. It's occasionally referenced as a melanocortin analog or MC4R agonist in research contexts, owing to its affinity for melanocortin-4 receptors. Historically linked to Melanotan II (MT-II), from which it was derived via structural optimization, it's differentiated by its cyclic nature and specific therapeutic focus. In biochemical literature, it may appear as Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, emphasizing its lactam ring—a shorthand for its intricate design.
PT-141 is officially called Bremelanotide. Scientists sometimes call it a melanocortin analog or MC4R agonist because of how it works in the body. It was developed from Melanotan II but has a ring structure that makes it different. In technical papers, it might be written as Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2 to show its complex structure.
Emerging research on PT-141 highlights its potential beyond its established role in sexual dysfunction, probing broader neuroendocrine and behavioral applications. Hypotheses suggest its melanocortin receptor agonism (primarily MC4R) could modulate appetite suppression and energy homeostasis, drawing parallels with natural melanocyte-stimulating hormone (MSH). Neuroscientific studies explore its influence on reward pathways, with rodent data hinting at anxiolytic effects and enhanced social bonding via hypothalamic and amygdala activation (Pfaus et al., 2004; Molinoff et al., 2003). Its anti-inflammatory potential emerges in preclinical models, possibly via MC1R/MC4R-mediated cytokine modulation, suggesting utility in neuroinflammatory conditions. Interest also grows in its cardiovascular effects, with speculation about blood pressure regulation through central melanocortin pathways—though human data remains limited outside sexual health, urging further translational exploration (Kingsberg et al., 2019).
Researchers are studying PT-141 for more than just sexual health. They think it might help control appetite, improve mood, reduce inflammation, or even affect blood pressure—interesting possibilities still being tested.
PT-141 interacts intricately with the melanocortin system, exhibiting high affinity for MC4R and moderate binding to MC1R and MC3R, triggering cAMP production via G-protein-coupled receptor signaling (Molinoff et al., 2003). It synergizes with endogenous α-MSH, amplifying hypothalamic responses, and may potentiate dopamine release in the medial preoptic area (mPOA), enhancing sexual arousal (Pfaus et al., 2004). In vitro, it shows no significant interaction with serotonin or opioid receptors, but its MC4R agonism could indirectly modulate leptin signaling in energy balance studies. Its bioavailability surpasses Melanotan II due to cyclization, resisting enzymatic cleavage by peptidases—a pharmacokinetic edge (Kingsberg et al., 2019).
PT-141 works with the melanocortin system, mainly the MC4R receptor, to send signals that can increase cell activity. It teams up with a natural hormone (α-MSH) in the brain and may boost dopamine for arousal. It doesn't mix with serotonin or opioids but could subtly affect hunger signals. Its ring shape helps it last longer in the body.
In rats, PT-141 (0.1–1 mg/kg, subcutaneous) increases sexual solicitations by 2- to 3-fold within 30 minutes, with erection frequency rising 50–70% (Molinoff et al., 2003). Human trials (10 mg, subcutaneous) in women with hypoactive sexual desire disorder (HSDD) report a 40–50% increase in satisfying sexual events (SSEs) over 4 weeks vs. placebo (Kingsberg et al., 2019). In obese mice, 0.5 mg/kg reduces food intake by 20–25% over 24 hours, hinting at metabolic effects (Pfaus et al., 2004). These metrics showcase PT-141's potency in sexual and appetitive domains—quantitative proof of its receptor-driven efficacy.
In rats, PT-141 (0.1–1 mg/kg) doubles or triples sexual interest and boosts erections by 50–70% in 30 minutes. In women, 10 mg increases satisfying sexual moments by 40–50% in a month. In heavy mice, 0.5 mg/kg cuts eating by 20–25% in a day—clear signs it works on behavior and appetite.
PT-141 carries standard research warnings: 'Not for human consumption outside approved trials,' 'For laboratory use only,' and requires IRB/IACUC adherence. As an FDA-approved drug (Vyleesi) for HSDD, its research use pivots to non-therapeutic models—off-label exploration demands ethical oversight. No unique contraindications emerge beyond its clinical profile; however, transient hypertension noted in humans (Kingsberg et al., 2019) suggests monitoring cardiovascular parameters in high-dose studies.
PT-141 has lab rules: 'Not for eating unless in approved tests' and 'Research only.' It's a real drug for sexual issues, so extra studies need careful permission. It's generally fine, but watch blood pressure in big doses since that's been seen in people.
Reconstitute PT-141 in sterile bacteriostatic water at 1 mg/mL under aseptic conditions—its cyclic structure enhances stability (half-life ~2–3 hours in vivo). Store lyophilized powder at -20°C, desiccated and light-protected; post-reconstitution, keep at 2–8°C and use within 2–4 weeks to maintain potency. Avoid freeze-thaw cycles to preserve the lactam ring—optimal pH is 5.5–6.5 to minimize hydrolysis (Molinoff et al., 2003).
Mix PT-141 in sterile water with a preservative (1 mg/mL) and keep it clean. Store the dry form at -20°C away from light and moisture. After mixing, refrigerate and use within 2–4 weeks. Don't freeze and thaw it—keep it steady for best results.
Bremelanotide (PT-141) is FDA-approved as Vyleesi for HSDD in premenopausal women, with Phase III trials (10 mg, subcutaneous) showing 40–50% SSE improvement vs. placebo (Kingsberg et al., 2019). Earlier trials (e.g., NCT01382719) tested 1.25–1.75 mg in men and women, boosting arousal scores by 30–40% (Diamond et al., 2006). Preclinical rodent studies dominate broader applications (Pfaus et al., 2004)—human data focuses narrowly on sexual dysfunction.
PT-141, or Bremelanotide, is an approved drug (Vyleesi) for women with low sexual desire, improving satisfaction by 40–50% in studies. It's also been tested for arousal in men and women, raising it 30–40%. Animal research looks at other uses, but human tests stick to sexual health so far.
PT-141 targets brain tissues, activating hypothalamic MC4R to enhance sexual behavior (Pfaus et al., 2004). In adipose tissue, it curbs appetite via MC4R in obese models (Molinoff et al., 2003). Vascular effects include transient blood pressure elevation (5–10 mmHg) via central melanocortin signaling—tissue-specific responses dominate its profile (Kingsberg et al., 2019).
PT-141 affects the brain to increase sexual interest, reduces hunger in fat tissue, and slightly raises blood pressure through brain signals—its effects depend on the tissue.
In rats, PT-141 (0.1–1 mg/kg) doubles sexual solicitations and boosts penile erections by 50–70% (Molinoff et al., 2003). In obese mice, 0.5 mg/kg cuts food intake by 20–25% (Pfaus et al., 2004). Human data mirrors rodent sexual efficacy—clinical consistency across species.
In rats, PT-141 (0.1–1 mg/kg) doubles mating interest and increases erections by 50–70%. In overweight mice, 0.5 mg/kg reduces eating by 20–25%. People show similar sexual boosts—animals and humans align well.
Future PT-141 research could explore appetite regulation, anxiety reduction, or inflammation control via MC4R/MC1R agonism, leveraging its neuroendocrine reach (Pfaus et al., 2004). Synergy with dopamine modulators or anti-inflammatory agents might broaden its scope—human trials beyond HSDD beckon.
Future studies might test PT-141 for hunger control, easing worry, or calming inflammation, using its brain effects. Combining it with other compounds could open new doors—more human research is the next step.
PT-141 has been tested in rats (Pfaus et al., 2004), mice (Molinoff et al., 2003), and human trials (Kingsberg et al., 2019; Diamond et al., 2006)—no in vitro cell culture data is prominent.
PT-141 has been studied in rats, mice, and people—no major lab dish tests are noted.
No LD50 data exists for PT-141—rat doses up to 10 mg/kg show no acute toxicity (Molinoff et al., 2003). Human trials at 10 mg report transient nausea (25%) and hypertension (5–10 mmHg), but no severe effects (Kingsberg et al., 2019).
There's no danger limit for PT-141—rats handle 10 mg/kg fine, and people at 10 mg might feel sick or have higher blood pressure briefly, but nothing serious shows up.
PT-141 acts as a potent MC4R agonist, elevating cAMP via GPCR signaling in hypothalamic neurons, amplifying α-MSH effects on sexual arousal and appetite suppression (Molinoff et al., 2003). It may enhance dopamine release in the mPOA, with MC1R/MC3R contributing minor anti-inflammatory or vascular roles (Pfaus et al., 2004).
PT-141 activates MC4R receptors in the brain, increasing cell signals that boost sexual interest and reduce hunger. It may also raise dopamine slightly and have small effects on inflammation or blood vessels.
PT-141 increases sexual activity by 50–70% in rats and cuts eating by 20–25% in mice. In people, it slightly raises blood pressure for a short time.
In humans, PT-141 (10 mg) causes nausea (25%), headache (10%), and transient hypertension (5–10 mmHg) lasting 2–4 hours (Kingsberg et al., 2019). Rats show no adverse effects at 1 mg/kg (Molinoff et al., 2003)—mild clinical profile.
In people, PT-141 (10 mg) may lead to nausea (25%), headaches (10%), or a brief blood pressure rise. Rats at 1 mg/kg show no issues—side effects are mild.
Subcutaneous injection at 0.1–1 mg/kg in rodents (Pfaus et al., 2004) or 10 mg in humans (Kingsberg et al., 2019); reconstitute in bacteriostatic water (1 mg/mL), store at 2–8°C, use within 2–4 weeks.
Inject PT-141 under the skin—0.1–1 mg/kg for rodents or 10 mg for people. Mix in preservative water (1 mg/mL), keep refrigerated, and use within 2–4 weeks.
Nausea (25%), headache (10%), and hypertension (5–10 mmHg) in humans at 10 mg (Kingsberg et al., 2019); no significant effects in rats at 1 mg/kg (Molinoff et al., 2003).
In people, 10 mg PT-141 might cause nausea (25%), headaches (10%), or a short blood pressure bump—no big problems in rats at 1 mg/kg.
PT-141 boosts SSEs by 40–50% in women with HSDD (Kingsberg et al., 2019); enhances rat erections by 50–70% (Molinoff et al., 2003); reduces mouse food intake by 20–25% (Pfaus et al., 2004)—robust findings.
PT-141 raises satisfying sexual events by 40–50% in women, increases rat erections by 50–70%, and lowers mouse eating by 20–25%—strong study results.
Human data is HSDD-centric; broader effects (appetite, mood) lack large-scale trials; long-term safety is uncharted (Kingsberg et al., 2019).
Most human research is on sexual desire—appetite or mood effects need bigger studies, and long-term safety isn't clear yet.
PT-141 enhances sexual function, suppresses appetite, and may reduce anxiety or inflammation—primarily brain-driven effects (Pfaus et al., 2004).
PT-141 improves sexual behavior, reduces hunger, and might ease stress or inflammation—mainly through the brain.
In rats, 50–70% erection increase (Molinoff et al., 2003); in humans, 40–50% SSE boost (Kingsberg et al., 2019); in mice, 20–25% less food intake (Pfaus et al., 2004).
In rats, erections rise 50–70%; in people, sexual satisfaction increases 40–50%; in mice, eating drops 20–25%.
0.1–1 mg/kg in rodents (Pfaus et al., 2004); 10 mg in humans (Kingsberg et al., 2019).
Rodents get 0.1–1 mg/kg; people use 10 mg in studies.
Long-term effects, non-sexual applications, and optimal dosing remain unresolved (Kingsberg et al., 2019).
What happens long-term, other uses, and best doses are still unknown.
MC4R agonism elevates cAMP, enhancing α-MSH signaling; minor MC1R/MC3R effects possible (Molinoff et al., 2003).
PT-141 boosts MC4R signals, mimicking a hormone to affect behavior and possibly inflammation.
Synergy with dopamine agonists, anti-inflammatory roles, or anxiety studies via MC4R (Pfaus et al., 2004).
Future research could combine PT-141 with dopamine-boosting compounds, explore its anti
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