Imidazoline Receptors
Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. There are three classes of imidazoline receptors: I1 receptor – mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure, (NISCH or IRAS, imidazoline receptor antisera selected), I2 receptor - an allosteric binding site of monoamine oxidase and is involved in pain modulation and neuroprotection, I3 receptor - regulates insulin secretion from pancreatic beta cells. Activated I1-imidazoline receptors trigger the hydrolysis of phosphatidylcholine into DAG. Elevated DAG levels in turn trigger the synthesis of second messengers arachidonic acid and downstreameicosanoids. In addition, the sodium-hydrogen antiporter is inhibited, and enzymes of catecholamine synthesis are induced. The I1-imidazoline receptor may belong to the neurocytokine receptorfamily, since its signaling pathways are similar to those of interleukins.
Products for Imidazoline Receptors
- Cat.No. Product Name Information
-
GC11588
2-BFI hydrochloride
I2 ligand
-
GC16831
Agmatine sulfate
NIH 11035
α2-adrenergic receptor ligand -
GC14934
AGN 192403 hydrochloride
I1 imidazoline receptor
-
GN10492
Allantoin
(±)-Allantoin, NSC 7606, SD 101, 5-Ureidohydantoin
-
GC74240
Allantoin-13C2,15N4
5-Ureidohydantoin-13C2,15N4
Allantoin-13C2,15N4 is the 13C and 15N labeled Allantoin. -
GC15700
BU 224 hydrochloride
Antagonist of I2 Imidazoline receptor,potent and selective
-
GC15202
BU 226 hydrochloride
Ligand at I2 imidazoline sites,high affinity and selectivity
-
GC11580
BU 239 hydrochloride
Imidazoline receptors-selective antagonist
-
GC31094
CR4056
-
GC15384
Harmane
1-Methyl-β-Carboline, NSC 54439
endogenous ligand for imidazoline binding sites -
GC69206
Harmane-d
Harmane-d is the deuterated form of Harmane. Harmane, a beta-carboline alkaloid, is an effective neurotoxin that can cause severe motor tremors and psychiatric symptoms. Harmane has a 1000-fold selectivity for I1-imidazoline receptors (IC50=30 nM) over alpha-2 adrenergic receptors (IC50=18 μM). It is also an effective and selective monoamine oxidase inhibitor with IC50 values of 0.5 μM and 5 μM for MAO A/B, respectively.
-
GC63754
Harmane-d1
Harmane-d1 is the deuterium labeled Harmane.
-
GC38192
Idazoxan hydrochloride
-
GC12629
Moxonidine
LY326869
An imidazoline I1 and α2A-adrenergic receptor agonist -
GC11198
Moxonidine hydrochloride
Mixed I1 imidazoline receptor and α2-adrenergic agonist
-
GC60325
Rilmenidine
Oxaminozoline, NSC 664312
An antihypertensive agent -
GC13017
Rilmenidine Phosphate
antihypertensive drug targets the imidazoline receptor
-
GC14958
RS 45041-190 hydrochloride
Highly selective I2 imidazoline receptor ligand