Cloning and regulation g-protein coupled receptorEvaluation of the α2C-adrenoceptor as a neuropsychiatric drug target: Studies in transgenic mouse models
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2,3-Dihydrobenzo-dioxine piperidine derivatives as potent and selective α2c antagonists
2022, Bioorganic and Medicinal Chemistry LettersAntinociceptive activity of methanol extract of Chlorophytum alismifolium tubers in murine model of pain: Possible involvement of α<inf>2</inf>-adrenergic receptor and K<inf>ATP</inf> channels
2020, Journal of Traditional and Complementary MedicineCitation Excerpt :The administration of α2-adrenoceptor agonists produce anti-nociception in rodents by inhibiting synaptic transmission in the dorsal horn of the spinal cord and there is an evidence that stimulation of the descending noradrenergic system results in the activation of spinal α2-adrenoceptor and antinociception.33,34 All the three α2-adrenoceptor subtypes have also been reported to act as presynaptic inhibitory feedback receptors to control the release of catecholamines from adrenergic neurons and are linked to antinociceptive process.35,36,37 In this study, pre-treatment of mice with yohimbine (a presynaptic α2-adrenergic receptor antagonist) significantly attenuated the antinociceptive activity of C. alismifolium extract.
Tolerability of ORM-12741 and effects on episodic memory in patients with Alzheimer's disease
2017, Alzheimer's and Dementia: Translational Research and Clinical InterventionsCitation Excerpt :These effects seem to be especially prominent under stressful conditions [6]. At the behavioral level, alpha-2C ARs modulate the performance of experimental animals in tests predicting antidepressant and antipsychotic efficacy as well as learning and memory functions [6]. Consistent with this, specific and subtype-selective alpha-2C AR antagonists have shown positive effects in various nonclinical models predicting efficacy on cognition as well as symptoms of schizophrenia and depression [7,8].
Function of brain α<inf>2B</inf>-adrenergic receptor characterized with subtype-selective α<inf>2B</inf> antagonist and KO mice
2016, NeuroscienceCitation Excerpt :Loss of the α2A receptor is associated with robust alterations in many functions, including sedation, hypothermia, sympathetic regulation, analgesia, blood pressure, anxiety, diurnal rhythms, and behavioral responses to psychostimulants (Scheinin et al., 2001; Tan et al., 2002; Lähdesmäki et al., 2002, 2004; Juhila et al., 2005). Knock out of α2C receptors has been associated with increased psychostimulant-induced locomotion, increased startle reactivity, increased aggression and decreased depressive behaviors and altered sensorimotor integration (Sallinen et al., 1998, 1999; Scheinin et al., 2001; Gilsbach et al., 2006). Findings with mice overexpressing the α2C receptor further support these KO findings and strongly suggest that the α2C receptor is involved in inhibiting sensory information processing (Sallinen et al., 1998, 1999; Scheinin et al., 2001).