Imidazoline Binding Site Ligands

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SML1703 2-BFI hydrochloride ≥98% (HPLC) 2-BFI is a high-affinity Imidzoline I2 receptor ligand (Ki = 9.8 nM) In an in vivo functional assay, 2-BFI induces hypothermia in rats.
A7127 Agmatine sulfate salt ≥97%, powder Putative endogenous neurotransmitter at imidazoline receptors; displaces clonidine at α2-adrenergic and at imidazoline receptors; blocks NMDA-activated ion channels in hippocampal neurons.
A9899 Antazoline hydrochloride Imidazoline agonist; more potent than efaroxan in inducing insulin release from β cells; H1 histamine receptor antagonist.
B154 BU224 hydrochloride solid I2 Imidazoline receptor antagonist.
C223 Cirazoline hydrochloride solid Selective α1-adrenoceptor agonist; non-selective imidazoline binding site ligand
C7897 Clonidine hydrochloride solid α2-adrenoceptor agonist; I1 imidazoline binding site ligand.
Clonidine hydrochloride is used for management of hypertension in pregnant women. In addition, it also acts as a therapeutic for neonatal abstinence syndrome. Clonidine hydrochloride binds to central α-adrenergic receptors and reduces the efferent sympathetic neuronal vasoconstrictor tone to the heart, kidneys and peripheral vasculature leading to vasodilatation and reduction in the blood pressure.
E3263 Efaroxan hydrochloride ≥98% (HPLC) (+)-Isomer is a selective α-adrenoceptor antagonist; (−)-isomer is an imidazoline ligand that induces insulin secretion, mediated by the blockade of ATP-sensitive potassium channels in pancreatic β cells; I1 imidazoline binding site antagonist.
I6138 Idazoxan hydrochloride α2-adrenoceptor antagonist; I2 imidazoline receptor agonist; I1 imidazoline receptor antagonist. Idazoxan can antagonize various behaviors generated by ethanol in a preclinical setting. It possesses neuroprotective activity against spinal cord injury, resulted due to experimental autoimmune encephalomyelitis (EAE) in mouse, an animal modal of multiple sclerosis (MS).
SML1019   Lofexidine hydrochloride ≥98% (HPLC) Lofexidine, a derivative of clonidine, is a very potent agonist of α2 adrenoceptors. Lofexidine is used as a treatment for withdrawl from heroin and other opiates, and as a short-activg anti-hypertensive agent.
M5685 Metrazoline solid Potent and selective imidazoline binding site ligand
SML0862   RX871024 ≥98% (HPLC) RX871024 is an imidazoline receptor antagonist that stimulates insulin secretion in β-cells and islets at lower concentrations than other imidazoline ligands. 0.1 μM RX871024 enhances glucose-induced insulin secretion under nonpolarizing conditions and at higher concentrations, it enhances secretion through a KATP channel-independent mechanism.
R134 Rilmenidine hemifumarate salt solid Selective I1 imidazoline receptor agonist.