Cayman Agmatine (sulfate)

Agmatine is a metabolite formed during polyamine biosynthesis with diverse biological activities. Agmatine is released from and taken up by synaptosomes, demonstrating neurotransmitter-like activity. It binds to human adrenergic receptors (ARs) and imidazoline (I) receptors (K_is = 46.98, 164.4, 26.3, and 74.4 μM for α_2A-, α_2B-, and α_2c-ARs and I_2b, respectively). 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., 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 (K_ATP) in a concentration-dependent manner in mouse islets of Langerhans β-cells., Agmatine competitively inhibits neuronal, macrophage, endothelial, and inducible nitric oxide synthase (NOS; K_is = 660, 220, 7,500, and 260 μM, respectively) and irreversibly inactivates neuronal NOS in the presence of calmodulin (K_i = 29 μM). In vivo, agmatine (10 mg/kg) lowers the ED₅₀ value by 5.2- and 4.7-fold for morphine (Item No. ) and [D-Pen²,D-Pen⁵]enkephalin (DPDPE), respectively, in mice in a tail flick assay. 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-N^g-monomethyl arginine (L-NMMA; Item Nos. , ).

WARNING This product is not for human or veterinary use.