ArticleBritish journal of pharmacology2012
Characterization of the hypothermic effects of imidazoline I₂ receptor agonists in rats.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 38 citations in OpenAlex.
- Pharmacology, Medicinal Chemistry, and Therapeutic Potential of Imidazoline Receptor Ligands.ChemMedChem · 2026Review
- Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2Journal of medicinal chemistry · 2025Article
- The imidazoline IPsychopharmacology · 2024Article
- Evaluating the effects of 2-BFI and tracizoline, two potent INaunyn-Schmiedeberg's archives of pharmacology · 2021Article
- Behavioral and Cognitive Improvement Induced by Novel Imidazoline INeurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2019Article
- Mechanisms of imidazoline IBritish journal of pharmacology · 2018Article
- Neuroanatomical characterization of imidazoline IThe European journal of neuroscience · 2018Article
- Role of intracellular CaPsychopharmacology · 2017Article
- Imidazoline IPharmacology & therapeutics · 2017Review
- Agmatine attenuates the discriminative stimulus and hyperthermic effects of methamphetamine in male rats.Behavioural pharmacology · 2016Article
- Antinociceptive effects of imidazoline I2 receptor agonists in the formalin test in rats.Behavioural pharmacology · 2016Article
- Effects of the imidazoline I2 receptor agonist 2-BFI on the development of tolerance to and behavioural/physical dependence on morphine in rats.British journal of pharmacology · 2016Article
- Anti-hyperalgesic effects of imidazoline I2 receptor ligands in a rat model of inflammatory pain: interactions with oxycodone.Psychopharmacology · 2015Article
- Discriminative stimulus effects of the imidazoline I2 receptor ligands BU224 and phenyzoline in rats.European journal of pharmacology · 2015Article
- Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats.Pharmacology research & perspectives · 2014Article
- Discriminative stimulus effects of the novel imidazoline I₂ receptor ligand CR4056 in rats.Scientific reports · 2014Article
- Modulation of imidazoline I2 binding sites by CR4056 relieves postoperative hyperalgesia in male and female rats.British journal of pharmacology · 2014Article
- The trace amine associated receptor 1 agonist RO5263397 attenuates the induction of cocaine behavioral sensitization in rats.Neuroscience letters · 2014Article
- Behavioral effects of the imidazoline I(2) receptor ligand BU99006 in rats.Behavioural pharmacology · 2014Article
- Antihyperalgesic effects of imidazoline I(2) receptor ligands in rat models of inflammatory and neuropathic pain.British journal of pharmacology · 2014Article
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Authors and funding
5 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND PURPOSE Imidazoline I(2) receptors have been implicated in several CNS disorders. Although several I(2) receptor agonists have been described, no simple and sensitive in vivo bioassay is available for studying I(2) receptor ligands. This study examined I(2) receptor agonist-induced hypothermia as a functional in vivo assay of I(2) receptor agonism. EXPERIMENTAL APPROACH Different groups of rats were used to examine the effects of I(2) receptor agonists on the rectal temperature and locomotion. The pharmacological mechanisms were investigated by combining I(2) receptor ligands and different antagonists. KEY RESULTS All the selective I(2) receptor agonists examined (2-BFI, diphenyzoline, phenyzoline, CR4056, tracizoline, BU224 and S22687, 3.2-56 mg·kg(-1) , i.p.) dose-dependently and markedly decreased the rectal temperature (hypothermia) in rats, with varied duration of action. Pharmacological mechanism of the observed hypothermia was studied by combining the I(2) receptor agonists (2-BFI, BU224, tracizoline and diphenyzoline) with imidazoline I(2 ) receptor/ α(2) adrenoceptor antagonist idazoxan, selective I(1) receptor antagonist efaroxan, α(2) adrenoceptor antagonist/5-HT(1A) receptor agonist yohimbine. Idazoxan but not yohimbine or efaroxan attenuated the hypothermic effects of 2-BFI, BU224, tracizoline and diphenyzoline, supporting the I(2) receptor mechanism. In contrast, both idazoxan and yohimbine attenuated hypothermia induced by the α(2) adrenoceptor agonist clonidine. Among all the I(2) receptor agonists studied, only S22687 markedly increased the locomotor activity in rats. CONCLUSIONS AND IMPLICATIONS Imidazoline I(2) receptor agonists can produce hypothermic effects, which are primarily mediated by I(2) receptors. These data suggest that I(2) receptor agonist-induced hypothermia is a simple and sensitive in vivo assay for studying I(2) receptor ligands.
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