DSIP: Safety Profile & Research Summary
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Preclinical Research Summary
Key Preclinical Studies
| Study | Model | Key Findings | Ref |
|---|---|---|---|
| Mu et al. (2024) | Mice β PCPA-induced insomnia; DSIP-CBBBP fusion peptide, not native DSIP | Modulated 5-HT, glutamate, dopamine and melatonin levels; fusion construct outperformed unmodified DSIP on neurotransmitter restoration | [22] |
| Monnier/Polc (1977β78) | Rabbits/Cats β EEG/sleep | 39β54% increase in delta activity (rabbits); enhanced REM in cats | [17] |
| Tukhovskaya et al. (2021) | SD rats β MCAO stroke, 120 Β΅g/kg intranasal | Significant motor recovery (Rotarod p<0.01); infarct size not significantly reduced | [7] |
| Tukhovskaya et al. (2021) | SD rats β MI reperfusion, 150 Β΅g/kg IP | IA/AAR reduced to 28.7% vs 42.1% control (p=0.01); β οΈ 100% mortality during occlusion | [8] |
| Popovich et al. (2003) | SHR mice β 2.5 Β΅g/mouse SC monthly | Max lifespan +24.1% (917 vs 739 d); tumors β2.6-fold; chromosomal aberrations β22.6% | [10] |
| HrnΔiΔ et al. (2006) | Wistar rats β metaphit audiogenic seizure model, DSIP 1.0 mg/kg IP Β± valproate 50 mg/kg | DSIP or valproate alone had no significant effect on seizure latency; the combination significantly prolonged latency over 6 h without motor impairment. Neither abolished EEG epileptiform activity | [16] |
| Scherschlicht/Tissot (Patent) | Mice β morphine withdrawal (naloxone-precipitated) | Dose-dependent withdrawal inhibition: 0.3 mg/kg SC reduced jumping to 54% of control | [13] |
| Nakamura et al. (1988) | Mice/Rats β pain tests (tail-pinch, hot plate) | Potent dose-dependent antinociception via ICV; blocked by naloxone (opioid-mediated) | [11] |
Clinical / Human Studies
| Trial | Population | Key Results | Outcome | Ref |
|---|---|---|---|---|
| Acute Effects in Normals | n=6 healthy adults | 59% median increase in total sleep time; β SWS and REM | Success | [3] |
| 7-Night Insomnia Treatment | n=14 chronic insomniacs | Normalized sleep efficiency and daytime alertness to levels of healthy controls | Success | [4] |
| Double-Blind Insomnia Study | n=16 chronic insomniacs | Higher sleep efficiency and shorter sleep latency vs placebo, but the authors judged the effects weak and partly attributable to change in the placebo group; subjective sleep quality was unchanged | Negative / equivocal | [23] |
| Withdrawal Syndromes | n=107 (47 alcoholics, 60 opiate addicts) | Opiate: 97% improved; Alcohol: 87% improved; DTs terminated in 6/8 | Success | [2] |
| Chronic Pain Pilot | n=7 (migraine, tinnitus, psychogenic pain) | Pain reduced in 6/7 subjects; simultaneous reduction in depression | Success | [5] |
| Double-Blind Insomnia | n=16 chronic insomniacs | Effects described as "weak"; authors concluded "not likely to be of major therapeutic benefit" | Failure | [23] |
Safety Summary
| Parameter | Finding |
|---|---|
| FDA Category 2 Warning | "Significant safety risks" β potential immunogenicity; "lacks sufficient information"; not approved for compounding |
| Acute Toxicity (Animals) | Oral LD50 in rats >5,000 mg/kg; MTD in dogs >2,000 mg/kg β high safety margin |
| Historical Human Trials | Mild adverse events: headache, nausea, vertigo; described as "incredibly safe" in 70+ subjects |
| β οΈ CRITICAL TIMING | 100% mortality when given during active ischemic occlusion (MI or stroke); protective ONLY during reperfusion |
| Pharmacokinetics | Half-life ~15 min; degraded by aminopeptidases (N-terminal Trp cleavage); crosses BBB partly |
| Drug Interactions | Antagonizes morphine; reversed by naloxone; reverses amphetamine hyperthermia; incompatible with peptidase inhibitors (captopril) |
In Vitro / Preclinical Disclaimer: The research findings described above were observed in laboratory (in vitro) and/or animal model studies. These results may not translate to human outcomes. No claims are made regarding human therapeutic applications.
Educational Use Only: This content is provided for informational and educational purposes only. It is not intended as medical advice and should not be used to diagnose, treat, cure, or prevent any disease or medical condition. Always consult qualified healthcare professionals for medical decisions.
Editorial Research Note
βPreclinical Research Summary Key Preclinical Studies StudyModelKey FindingsRef Mu et al.β
References
- Kovalzon VM, Strekalova TV. Delta sleep-inducing peptide (DSIP): A still unresolved riddle. J Neurochem. 2006;97(2):303-309.
- Dick P, Costa C, Fayolle K, et al. DSIP in the treatment of withdrawal syndromes from alcohol and opiates. Eur Neurol. 1984;23(5):364-371.
- Schneider-Helmert D, Gnirss F, Monnier M, Schenker J, Schoenenberger GA. Acute and delayed effects of DSIP (delta sleep-inducing peptide) on human sleep behavior. Int J Clin Pharmacol Ther Toxicol. 1981;19(8):341-345.
- Schneider-Helmert D. Effects of delta-sleep-inducing peptide on 24-hour sleep-wake behaviour in severe chronic insomnia. Eur Neurol. 1987;27(2):120-129.
- Larbig W, Gerber WD, Kluck M, Schoenenberger GA. Therapeutic effects of delta-sleep-inducing peptide (DSIP) in patients with chronic, pronounced pain episodes. Eur Neurol. 1984;23(5):372-385.
- Kaeser HE. A clinical trial with DSIP. Eur Neurol. 1984;23(5):386-388.
- Tukhovskaya EA, Ismailova AM, Shaykhutdinova ER, et al. Delta Sleep-Inducing Peptide Recovers Motor Function in SD Rats after Focal Stroke. Molecules. 2021;26(17):5173.
- Tukhovskaya EA, Shaykhutdinova ER, Ismailova AM, et al. DSIP-Like KND Peptide Reduces Brain Infarction in C57Bl/6 and Reduces Myocardial Infarction in SD Rats When Administered during Reperfusion. Biomedicines. 2021;9(4):407.
- Graf MV, Kastin AJ. Delta-sleep-inducing peptide (DSIP): a review. Neurosci Biobehav Rev. 1984;8(1):83-93.
- Popovich IG, Voitenkov BO, Anisimov VN, et al. Effect of delta-sleep inducing peptide-containing preparation Deltaran on biomarkers of aging, life span and spontaneous tumor incidence in female SHR mice. Mech Ageing Dev. 2003;124(6):721-731.
- Nakamura A, Nakashima M, Sugao T, et al. Potent antinociceptive effect of centrally administered delta-sleep-inducing peptide (DSIP). Eur J Pharmacol. 1988;155(3):247-253.
- Dick P, Grandjean ME, Tissot R. Successful treatment of withdrawal symptoms with delta sleep-inducing peptide. Neuropsychobiology. 1983;10(4):205-208.
- Scherschlicht RR, Tissot R. Nonapeptide for treating addictive drug withdrawal conditions. US Patent 4,444,758. 1984.
- Food and Drug Administration. Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks. FDA Website. Updated July 2025.
- Schoenenberger GA. Characterization, properties and multivariate functions of delta-sleep-inducing peptide (DSIP). Eur Neurol. 1984;23(5):321-345.
- HrnΔiΔ D, StanojloviΔ O, Ε½ivanoviΔ D, Ε uΕ‘iΔ V. Delta-sleep-inducing peptide potentiates anticonvulsive activity of valproate against metaphit-provoked audiogenic seizure in rats. Pharmacology. 2006;77(2):78-84.
- Monnier M, Dudler L, Gaechter R, et al. The delta sleep inducing peptide (DSIP). Comparative properties of the original and synthetic nonapeptide. Experientia. 1977;33(4):548-552.
- Sudakov KV, Ivanov VT, Koplik EV, et al. Delta-sleep-inducing peptide (DSIP) as a factor facilitating animals' resistance to acute emotional stress. Pavlov J Biol Sci. 1983;18(1):1-5.
- Graf M, Baumann JB, Girard J, et al. DSIP-induced changes of daily concentrations of brain neurotransmitters and plasma proteins in rats. Pharmacol Biochem Behav. 1982;17(3):511-517.
- Shandra AA, Godlevskii RS, Vast'yanov AI, et al. Effect of intranigral dosage with delta-sleep-inducing peptide and its analogs on movement and convulsive activity in rats. Neurosci Behav Physiol. 1996;26(6):567-571.
- Salieva RM, Koplik EV, Kamenov ZA, Poletaev AB. Effects of beta endorphin and delta-sleep inducing peptide on resistance to emotional stress. Biull Eksp Biol Med. 1989;108(10):464-466.
- Mu X, Qu L, Yin L, Wang L, Liu X, Liu D. Pichia pastoris secreted peptides crossing the blood-brain barrier and DSIP fusion peptide efficacy in PCPA-induced insomnia mouse models. Front Pharmacol. 2024;15:1439536.
- Bes F, Hofman W, Schuur J, Van Boxtel C. Effects of delta sleep-inducing peptide on sleep of chronic insomniac patients. A double-blind study. Neuropsychobiology. 1992;26(4):193-197.
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