ArticleBrain research2009
Identification of an imidazoline binding protein: creatine kinase and an imidazoline-2 binding site.
Article in Brain research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 34 citations in OpenAlex.
- Pharmacology, Medicinal Chemistry, and Therapeutic Potential of Imidazoline Receptor Ligands.ChemMedChem · 2026Review
- Targeting Creatine and Creatine Kinase in Cancer: Exploring Potential Therapeutic Strategies.Current drug targets · 2025Review
- Creatine Kinase Is Decreased in Childhood Asthma.American journal of respiratory and critical care medicine · 2023Article
- Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.International journal of molecular sciences · 2022Review
- Increased monoamine oxidase activity and imidazoline binding sites in insulin-resistant adipocytes from obese Zucker rats.World journal of biological chemistry · 2022Article
- Imaging of Reactive Astrogliosis by Positron Emission Tomography.Frontiers in neuroscience · 2022Review
- Improved efficacy, tolerance, safety, and abuse liability profile of the combination of CR4056 and morphine over morphine alone in rodent models.British journal of pharmacology · 2020Article
- CR4056, a powerful analgesic imidazoline-2 receptor ligand, inhibits the inflammation-induced PKCε phosphorylation and membrane translocation in sensory neurons.British journal of pharmacology · 2020Article
- Effects of imidazoline I2 receptor agonists on reserpine-induced hyperalgesia and depressive-like behavior in rats.Behavioural pharmacology · 2019Article
- Neuroanatomical characterization of imidazoline IThe European journal of neuroscience · 2018Article
- Mechanisms of imidazoline IBritish journal of pharmacology · 2018Article
- Morphine Binds Creatine Kinase B and Inhibits Its Activity.Frontiers in cellular neuroscience · 2018Article
- Role of intracellular CaPsychopharmacology · 2017Article
- Imidazoline IPharmacology & therapeutics · 2017Review
- Antinociceptive effects of imidazoline I2 receptor agonists in the formalin test in rats.Behavioural pharmacology · 2016Article
- Discriminative stimulus effects of the imidazoline I2 receptor ligands BU224 and phenyzoline in rats.European journal of pharmacology · 2015Article
- Discriminative stimulus effects of the novel imidazoline I₂ receptor ligand CR4056 in rats.Scientific reports · 2014Article
- Behavioral effects of the imidazoline I(2) receptor ligand BU99006 in rats.Behavioural pharmacology · 2014Article
- Analgesic efficacy of CR4056, a novel imidazoline-2 receptor ligand, in rat models of inflammatory and neuropathic pain.Journal of pain research · 2011Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
Abstract
Drugs that bind to imidazoline binding proteins have major physiological actions. To date, three subtypes of such proteins, I(1), I(2) and I(3), have been proposed, although characterisations of these binding proteins are lacking. I(2) binding sites are found throughout the brain, particularly dense in the arcuate nucleus of the hypothalamus. Selective I(2) ligands demonstrate antidepressant-like activity and the identity of the proteins that respond to such ligands remained unknown until now. Here we report the isolation of a approximately 45 kDa imidazoline binding protein from rabbit and rat brain using a high affinity ligand for the I(2) subtype, 2-BFI, to generate an affinity column. Following protein sequencing of the isolated approximately 45 kDa imidazoline binding protein, we identified it to be brain creatine kinase (B-CK). B-CK shows high binding capacity to selective I(2) ligands; [(3)H]-2-BFI (5 nM) specifically bound to B-CK (2330+/-815 fmol mg protein(-1)). We predicted an I(2) binding pocket near the active site of B-CK using molecular modelling. Furthermore, B-CK activity was inhibited by a selective I(2) irreversible ligand, where 20 microM BU99006 reduced the enzyme activity by 16%, confirming the interaction between B-CK and the I(2) ligand. In summary, we have identified B-CK to be the approximately 45 kDa imidazoline binding protein and we have demonstrated the existence of an I(2) binding site within this enzyme. The importance of B-CK in regulating neuronal activity and neurotransmitter release may well explain the various actions of I(2) ligands in brain and the alterations in densities of I(2) binding sites in psychiatric disorders.
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Registered trials
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