Quick Comparison

Agmatine SulfateForskolin
Half-Life2-3 hours4-6 hours
Typical DosageStandard: 500-2000 mg daily in 1-3 doses. For mood: 1000-2000 mg. For pain: 1000-2500 mg. Take on empty stomach. Agmatine sulfate is the most common supplement form. May enhance the effects of some nootropics and medications — research interactions.Standard: 250 mg Coleus forskohlii extract (standardized to 10% forskolin = 25 mg forskolin) twice daily. Higher forskolin concentrations (20%) available. Take with food. May cause blood pressure reduction — start low if hypotension-prone.
AdministrationOral (powder, capsules). Take on empty stomach for best absorption.Oral (capsules). Coleus forskohlii extract standardized to 10-20% forskolin.
Research Papers10 papers10 papers
Categories

Mechanism of Action

Agmatine Sulfate

Agmatine is a polyamine neuromodulator with multiple targets: (1) NMDA receptor antagonist at the polyamine binding site (GluN1/GluN2B) — reduces excitotoxicity, pain signaling, and blocks the receptor's open channel. (2) Imidazoline I1 and I2 receptor agonist — I1 in the rostral ventrolateral medulla reduces sympathetic tone; I2 modulates monoamine oxidase and provides anxiolytic/antidepressant effects. (3) Selective nNOS (neuronal nitric oxide synthase) inhibitor — reduces peroxynitrite formation and oxidative stress while preserving eNOS (endothelial) function for vascular health. (4) Alpha-2 adrenergic receptor agonist — reduces norepinephrine release from locus coeruleus, promoting calm. (5) Modulates opioid receptors — enhances mu-opioid analgesia, potentiates delta-opioid, and may reduce tolerance via nitric oxide and NMDA mechanisms.

Forskolin

Forskolin directly activates all nine isoforms of membrane-bound adenylate cyclase (AC1-9), the enzyme that converts ATP to cyclic AMP (cAMP), bypassing G-protein-coupled receptor activation. Elevated cAMP activates protein kinase A (PKA), which phosphorylates CREB (cAMP response element-binding protein) at Ser133 — a transcription factor essential for long-term memory formation that induces expression of BDNF, c-fos, and other plasticity-related genes. This is the same signaling cascade used by dopamine (D1), norepinephrine (beta-adrenergic), and serotonin (5-HT4/7) receptors, but forskolin activates it directly at the effector level. Elevated cAMP also increases neurotransmitter receptor sensitivity (e.g., beta-adrenergic receptor phosphorylation), enhances synaptic plasticity via PKA-mediated GluA1 phosphorylation, and potentiates L-type calcium channels. Forskolin may also activate TRPV channels.

Risks & Safety

Agmatine Sulfate

Common

Mild gastrointestinal discomfort, diarrhea at high doses.

Serious

May potentiate opioid medications (increased sedation risk). May lower blood pressure.

Rare

Headache, nausea.

Forskolin

Common

Diarrhea, low blood pressure, increased heart rate, headache.

Serious

Significant blood pressure reduction — avoid with hypotension or blood pressure medications.

Rare

Tremor, restlessness, bleeding risk.

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