Research compounds
Nociceptin
Orphanin FQ, N/OFQ
Nociceptin is a 17-amino-acid peptide and the endogenous ligand for the opioid receptor-like 1 receptor, the fourth member of the opioid receptor family. Its effects on pain are famously context-dependent.
Also known as: orphanin FQ, N/OFQ, PNOC
- Status
- Nociceptin is a research compound and not approved by the FDA for human use.
- Evidence
- Preclinical. Evidence comes from animal or lab studies; effects in people are not established.
- Half-life
- Short; degraded rapidly in plasma.
- How it's taken
- Not used therapeutically; research administration only
- Mechanism
- Other
How Nociceptin works
Nociceptin binds the NOP receptor, which is structurally similar to the classical opioid receptors but does not respond to naloxone. Given supraspinally it produces hyperalgesia and reverses opioid analgesia; given spinally it is analgesic. It also has anxiolytic effects, modulates reward, and is being explored for substance use disorder.
What research has looked at
- NOP receptor pharmacology produced a genuinely novel analgesic mechanism: cebranopadol, a mixed NOP and mu agonist, has advanced in trials with the aim of analgesia with reduced respiratory depression and abuse liability.
- NOP agonists reduce drug-seeking behaviour in animal models, making the system a target for substance use disorder.
- Its anxiolytic effects occur without the sedation and dependence of benzodiazepines in animal models.
Evidence level: Preclinical. Evidence comes from animal or lab studies; effects in people are not established. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Its effects reverse depending on site of administration — supraspinal hyperalgesia versus spinal analgesia — which makes systemic administration of the native peptide unpredictable and is the central obstacle to its use. No regulator has approved it, the human evidence base is limited, and material sold under this name is research chemical supply with unverified identity, purity, sterility and dose accuracy.
- Nociceptin is not blocked by naloxone, so opioid reversal agents do not counter its effects.
- No nociceptin-based product has been approved; the NOP-targeting drugs remain investigational.
- It does not meaningfully cross the blood-brain barrier, so peripheral administration cannot reproduce the central effects that make it interesting.
Sources
- PubMed research on nociceptin orphanin FQ NOP cebranopadol · NIH · National Library of Medicine
- DrugBank record for nociceptin · DrugBank
- Active clinical trials for nociceptin · U.S. National Library of Medicine
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Related compounds
Nociceptin FAQ
What is Nociceptin?
Nociceptin is a 17-amino-acid peptide and the endogenous ligand for the opioid receptor-like 1 receptor, the fourth member of the opioid receptor family. Its effects on pain are famously context-dependent.
How does Nociceptin work?
Nociceptin binds the NOP receptor, which is structurally similar to the classical opioid receptors but does not respond to naloxone. Given supraspinally it produces hyperalgesia and reverses opioid analgesia; given spinally it is analgesic. It also has anxiolytic effects, modulates reward, and is being explored for substance use disorder.
Is Nociceptin FDA approved?
No. Nociceptin is a research compound and not approved by the FDA for human use. Evidence level: preclinical. Evidence comes from animal or lab studies; effects in people are not established.
What is the half-life of Nociceptin?
Reported half-life: Short; degraded rapidly in plasma.
How is Nociceptin taken?
Not used therapeutically; research administration only.
What side effects have been reported with Nociceptin?
Reported in the sources: Its effects reverse depending on site of administration — supraspinal hyperalgesia versus spinal analgesia — which makes systemic administration of the native peptide unpredictable and is the central obstacle to its use. No regulator has approved it, the human evidence base is limited, and material sold under this name is research chemical supply with unverified identity, purity, sterility and dose accuracy; Nociceptin is not blocked by naloxone, so opioid reversal agents do not counter its effects; No nociceptin-based product has been approved; the NOP-targeting drugs remain investigational; It does not meaningfully cross the blood-brain barrier, so peripheral administration cannot reproduce the central effects that make it interesting.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.