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Cat. No.: HY-WAA0304

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Agmatine

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Agmatine is an orally active analgesic that can cross the blood-brain barrier. Agmatine targets the 5-HT_2A receptor, 5-HT₃ receptor, α₂-adrenergic receptor, and I1 imidazoline receptor. Agmatine produces dose-dependent analgesic effects in various pain models. Agmatine can be used in research related to visceral pain, neuropathic pain, and inflammatory pain.

For research use only. We do not sell to patients.

CAS No.: 306-60-5
Formula: C₅H₁₄N₄
Molecular Weight:130.19

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Agmatine Chemical Structure

CAS No.: 306-60-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

5-HT_2A Receptor

5-HT₃ Receptor

α2-adrenergic receptor

All 5-HT Receptor Isoforms :

All Adrenergic Receptor Isoforms :

In Vivo

Agmatine (1-30 mg/kg; i.p.; 30 min pre-acetic acid, 0.5-6 hours pre-acetic acid; 10-300 mg/kg; p.o.; 60 min pre-acetic acid) produces dose-dependent, long-lasting antinociception against acetic acid-induced visceral pain in Mus musculus, with 26-fold greater potency via i.p. (ID₅₀ 5.6 mg/kg) than oral (ID₅₀ 147.3 mg/kg) administration, acting through nitrergic, opioid, α₂-adrenoceptor, imidazoline I₁, and serotonergic (5-HT_2A, 5-HT₃) pathways^[2].
Agmatine (10-100 mg/kg; i.p.; 30 min pre-glutamate) dose-dependently inhibits glutamate-induced paw nociception in mice with an ID₅₀ of 19.5 mg/kg (i.p.)^[2].
Agmatine (3-100 mg/kg; i.p.; 30 min pre-capsaicin) dose-dependently inhibits Capsaicin (HY-10448)-induced paw nociception in mice with an ID₅₀ of 43.7 mg/kg (i.p.)^[2].
Agmatine (1-100 mg/kg; i.p.; 30 min pre-formalin; 10 mg/kg; i.p.; 10 min pre-formalin; 10 mg/kg; i.p.; 5 min post-formalin) dose-dependently inhibits both neurogenic and inflammatory phases of formalin-induced paw nociception in mice, with greater potency against the inflammatory phase (ID₅₀ 5.6 mg/kg i.p.) than the neurogenic phase (ID₅₀ 13.7 mg/kg i.p.)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Swiss mice (both sexes, 25-35 g)^[2]
Dosage:

1-30 mg/kg (i.p.); 10-300 mg/kg (p.o.)
Administration:

i.p. (30 min pre-acetic acid; 0.5, 1, 2, 4, or 6 hours pre-acetic acid); p.o. (60 min pre-acetic acid)
Result:

Produced dose-dependent inhibition of acetic acid-induced abdominal constrictions, with an ID₅₀ of 5.6 mg/kg (i.p.) and 147.3 mg/kg (p.o.), achieving maximum inhibitions of 83% and 57%, respectively.
Produced significant antinociception starting at 30 minutes post-administration with 10 mg/kg i.p., which persisted for up to 4 hours.
Had its antinociceptive effect completely reversed by pre-treatment with L-arginine (600 mg/kg i.p.), naloxone (1 mg/kg i.p.), yohimbine (0.15 mg/kg i.p.), ketanserin (0.3 mg/kg i.p.), ondansetron (0.5 mg/kg i.p.), or efaroxan (1 mg/kg i.p.), but not by D-arginine (600 mg/kg i.p.), pindolol (1 mg/kg i.p.), idazoxan (3 mg/kg i.p.), or neonatal capsaicin treatment.
Had its antinociceptive effect significantly reversed by pre-treatment with p-chlorophenylalanine methyl ester (100 mg/kg i.p. once daily for 4 days).

Animal Model:

Swiss mice (both sexes, 25-35 g)^[2]
Dosage:

10-100 mg/kg
Administration:

i.p. (30 min pre-glutamate)
Result:

Produced dose-dependent inhibition of glutamate-induced paw licking, with an ID₅₀ of 19.5 mg/kg and a maximum inhibition of 76%.

Animal Model:

Swiss mice (both sexes, 25-35 g)^[2]
Dosage:

3-100 mg/kg
Administration:

i.p. (30 min pre-capsaicin)
Result:

Produced dose-dependent inhibition of capsaicin-induced paw licking, with an ID₅₀ of 43.7 mg/kg and a maximum inhibition of 55%.

Animal Model:

Swiss mice (both sexes, 25-35 g)^[2]
Dosage:

1-100 mg/kg (30 min pre-formalin); 10 mg/kg (10 min pre-formalin); 10 mg/kg (5 min post-formalin)
Administration:

i.p. (30 min pre-formalin; 10 min pre-formalin; 5 min post-formalin)
Result:

Produced dose-dependent inhibition of both formalin-induced pain phases, with ID₅₀ values of 13.7 mg/kg (neurogenic phase, maximum inhibition 65%) and 5.6 mg/kg (inflammatory phase, maximum inhibition 76%).
Inhibited the neurogenic phase significantly when administered 10 mg/kg i.p. 10 minutes pre-formalin.
Inhibited the inflammatory phase by 42% when administered 10 mg/kg i.p. 5 minutes post-formalin.
Inhibited the inflammatory phase by 56% when administered 10 mg/kg i.p. 30 minutes pre-formalin.

Chemical Information

CAS No. 306-60-5
Appearance Solid
Molecular Weight 130.19
Formula C₅H₁₄N₄
Color White to off-white
SMILES

NC(NCCCCN)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Psychopharmacology (Berl)

Agmatine ameliorates morphine-induced behavioral sensitization through blood-brain barrier protection and anti-neuroinflammatory effects in the nucleus accumbens. [Abstract]

2025 Oct 24. PMID: 41134339

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Nudelman N. Aromatic nucleophilic substitution in aprotic solvents using hydrogen-bonded biological amines. Kinetic studies and quantum chemical calculations[J]. Journal of Physical Organic Chemistry, 2015.

[2]. Santos AR, et al. Mechanisms involved in the antinociception caused by agmatine in mice. Neuropharmacology. 2005;48(7):1021-1034. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References

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Agmatine

Publications Citing Use of MedChemExpress (MCE) Agmatine

All 5-HT Receptor Isoforms

All Adrenergic Receptor Isoforms