A polyamine metabolite; binds to human α2A-

Agmatine (sulfate) – 10 g

Brand:
Cayman
CAS:
2482-00-0
Storage:
4
UN-No:
Non-Hazardous - /

Agmatine is a metabolite formed during polyamine biosynthesis with diverse biological activities.{37373} Agmatine is released from and taken up by synaptosomes, demonstrating neurotransmitter-like activity. It binds to human adrenergic receptors (ARs) and imidazoline (I) receptors (Kis = 46.98, 164.4, 26.3, and 74.4 μM for α2A-, α2B-, and α2c-ARs and I2b, respectively).{37374} Agmatine acts as an antagonist of the NMDA receptor (NMDAR) in a voltage- and concentration-dependent manner in primary rat hippocampal neurons and antagonizes nicotinic acetylcholine receptors (nAChRs) in intact chick retina at 1 mM.{37375},{37376} It is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 in mouse N1E-115 neuroblastoma cells (IC50 = 141 μM) and blocks ATP-sensitive potassium channels (KATP) in a concentration-dependent manner in mouse islets of Langerhans β-cells.{37377},{37378} Agmatine competitively inhibits neuronal, macrophage, endothelial, and inducible nitric oxide synthase (NOS; Kis = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (Ki = 29 μM).{37379} In vivo, agmatine (10 mg/kg) lowers the ED50 value by 5.2- and 4.7-fold for morphine (Item No. ISO60147) and [D-Pen2,D-Pen5]enkephalin (DPDPE), respectively, in mice in a tail flick assay.{37380} It increases the nephron filtration rate when microperfused into the urinary space of rats, an effect that is reversed by the non-selective NOS inhibitor L-NG-monomethyl arginine (L-NMMA; Item Nos. 80200, 10005031).{37381}  

 

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Description

A polyamine metabolite; binds to human α2A-, α2B-, and α2c-ARs and I2b (Kis = 46.98, 164.4, 26.3, and 74.4 μM, respectively); inhibits NMDAR in a voltage- and concentration-dependent manner in primary rat hippocampal neurons and antagonizes nAChR in intact chick retina at 1 mM; competitively inhibits neuronal, macrophage, endothelial, and inducible NOS (Kis = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (Ki = 29 μM); lowers the ED50 value by 5.2- and 4.7-fold for morphine and DPDPE, respectively, in mice in a tail flick assay (10 mg/kg); increases the nephron filtration rate when microperfused into the urinary space in rats

Formal name: N-(4-aminobutyl)-guanidine, monosulfate

Synonyms:  NIH 11035

Molecular weight: 228.3

CAS: 2482-00-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology||Research Area|Neuroscience|Pain Research

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