Side-by-side · Research reference

5-Amino-1MQvsDermorphin

Side-by-side comparison across mechanism, dosage, evidence, side effects, administration, and stack synergies. Citations on every claim where available.

AAnimal-StrongAUTO-DRAFTED8/38 cited

BAnimal-StrongHUMAN-REVIEWED20/47 cited

5-Amino-1MQ

NNMT inhibitor · Methylation / SAM modulation

100–200 mgDaily dose (oral)Neelakantan 2018

AnimalEvidence levelNeelakantan 2018

HoursHalf-life (est)

Oral · Once daily fasted

Dermorphin

Opioid Peptide · μ-Receptor Agonist · Research Only

~30×Morphine potency

μ-selectiveReceptor typeNegri 1992

D-Ala²Unique featureAmiche 1998

Research only · ICV / SC (animal models)

01Mechanism of Action

Parameter

5-Amino-1MQ

Dermorphin

Primary target

Nicotinamide N-methyltransferase (NNMT)Neelakantan 2018

μ-opioid receptors (central and peripheral)Negri 1992 Steel 2014

Pathway

NNMT inhibition → preserved cellular SAM + NAD⁺ → restored methylation balance + ↑ thermogenic gene expressionNeelakantan 2018

μ-receptor activation → G-protein coupling → adenylyl cyclase inhibition → neuronal hyperpolarization

Downstream effect

Reversal of HFD-induced obesity in murine models; improved metabolic profileNeelakantan 2018

Potent analgesia, reduced nociceptive signaling, opioid-mediated CNS and peripheral effects

Feedback intact?

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N/A — exogenous opioid agonist

Origin

Selective small-molecule inhibitor designed in academic medicinal chemistry programsNeelakantan 2018

Phyllomedusa sauvagei and P. bicolor frog skin — gene-encoded with natural D-amino acid incorporationAmiche 1998 Mignogna 1992

Antibody development

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Site-directed antibodies produced for detection and purificationCucumel 1996

02Dosage Protocols

Parameter

5-Amino-1MQ

Dermorphin

Standard dose

100–200 mg / day oralNeelakantan 2018

Anecdotal community range; murine doses scaled.

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Frequency

Once daily, fasted

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Lower / starter dose

50 mg / day

—

Evidence basis

Animal-strong; no human RCT dataNeelakantan 2018

Animal studies · In vitro assays

Duration

8–12 weeks per cycle

—

Form

Oral capsule

—

Timing

Morning fasted preferred

—

Half-life

Hours (estimated; no human PK published)

—

Legal status

—

Controlled substance in many jurisdictions · Research only

Not approved for human use.

Animal research (ICV)

—

Low nanomolar to picomolar range

Intracerebroventricular administration in rodent models.

Detection limit (doping)

—

5 pg/mL in equine plasma/urineSteel 2014

High-throughput LC-MS/MS screen developed for racing industry.

Duration of action

—

10–120 minutes (dose-dependent, intrathecal)

Human toxicity

—

Kambô ritual (P. bicolor skin) — violent emesis, vasodilation, fluid shifts, ADH dysregulationTran 2025

04Side Effects & Safety

Parameter

5-Amino-1MQ

Dermorphin

GI symptoms

Mild nausea (anecdotal)

—

Methylation disruption

Theoretical risk if NNMT is over-inhibited (B vitamin metabolism)

—

Long-term safety

Unknown — no human trials

—

Cancer risk

Unclear — NNMT also studied in oncology contexts

—

Pregnancy / OB

Avoid

—

Drug interactions

Theoretical with niacin / B-vitamin supplements

—

Opioid effects

—

Respiratory depression, sedation, euphoria, tolerance, dependence risk

CNS effects

—

Analgesia (high-affinity sites), catalepsy (low-affinity sites)Negri 1992

Kambô ritual toxicity

—

Violent emesis, vasodilation, profound fluid shifts, hyponatremia, ADH dysregulation, brain death (case report)Tran 2025

Peripheral effects

—

GI motility inhibition (ileum > vas deferens in vitro)Negri 1992

Receptor selectivity caveat

—

Two μ-receptor subtypes — differential behavioral effects (analgesia vs. catalepsy)Negri 1992

Proteolytic stability

—

Tyr³-Pro⁶ bond relatively unstable; endogenous enzymes may produce tetrapeptide fragmentsCucumel 1996

Absolute Contraindications

5-Amino-1MQ

·Pregnancy / breastfeeding
·Active malignancy

Dermorphin

·Human use — not approved by any regulatory authority
·Controlled substance status — possession illegal in many jurisdictions
·Known opioid hypersensitivity or respiratory compromise

Relative Contraindications

5-Amino-1MQ

·Methylation-sensitive conditions (MTHFR mutation)
·Concurrent niacin / NAD+ precursor supplementation (theoretical interference)

Dermorphin

·Any context outside approved animal research protocols
·CNS depressant co-administration

05Administration Protocol

Parameter

5-Amino-1MQ

Dermorphin

1. Form

Oral capsule. No injection.

Dermorphin is a controlled substance in many jurisdictions and is not approved for human use. Possession, synthesis, or distribution may be illegal. Use is restricted to licensed research settings under institutional review.

2. Administration

Take with water, fasted preferred.

In rodent models, intracerebroventricular (ICV) or intrathecal injection is used at nanomolar to picomolar concentrations. Subcutaneous administration also documented. All protocols require IACUC approval.

3. Timing

Morning fasted.

High-throughput LC-MS/MS screens developed for anti-doping programs detect dermorphin and 17 related peptides in equine and human urine/plasma at limits as low as 5 pg/mL.Steel 2014

4. Storage

Room temp ≤25 °C, dry place.

Application of Phyllomedusa bicolor skin secretions to superficial burns. Not recommended — associated with severe toxicity including violent emesis, hyponatremia, and documented case of brain death.Tran 2025

5. Caveat

Monitor B-vitamin status with chronic use.

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