ArticleBritish journal of pharmacology2007
Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers, 1 of them a synthesis that pooled it.
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42 citing papers in PubMed, 1 synthesis or guideline pooled it, 95 citations in OpenAlex.
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- Centrally Acting Skeletal Muscle Relaxants Sharing Molecular Targets with Drugs for Neuropathic Pain Management.Brain sciences · 2025Review
- Preclinical evaluation of new C-11 labeled benzo-1,4-dioxane PET radiotracers for brain α2C adrenergic receptors.European journal of medicinal chemistry · 2022Article
- The affinity and selectivity of α-adrenoceptor antagonists, antidepressants and antipsychotics for the human α2A, α2B, and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors.Pharmacology research & perspectives · 2022Article
- The differentialFrontiers in pharmacology · 2022Article
- Classification models and SAR analysis on CysLT1 receptor antagonists using machine learning algorithms.Molecular diversity · 2021Article
- Ligands of Adrenergic Receptors: A Structural Point of View.Biomolecules · 2021Review
- Role of α2-Adrenoceptor Subtypes in Suppression of L-Type CaInternational journal of molecular sciences · 2021Article
- Application of the PET ligand [EJNMMI research · 2020Article
- PET Radiotracers for CNS-Adrenergic Receptors: Developments and Perspectives.Molecules (Basel, Switzerland) · 2020Review
- Spinal αBritish journal of pharmacology · 2019Review
- Selective adrenergic alpha2C receptor antagonist ameliorates acute phencyclidine-induced schizophrenia-like social interaction deficits in rats.Psychopharmacology · 2019Article
- Effects of 2-bromoterguride, a dopamine DPsychopharmacology · 2018Article
- The role of αThe journal of headache and pain · 2017Article
- Therapeutic Potential of Selectively Targeting the αFrontiers in psychiatry · 2017Review
- Tolerability of ORM-12741 and effects on episodic memory in patients with Alzheimer's disease.Alzheimer's & dementia (New York, N. Y.) · 2017Article
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposePharmacological validation of novel functions for the alpha2A-, alpha2B-, and alpha2C-adrenoceptor (AR) subtypes has been hampered by the limited specificity and subtype-selectivity of available ligands. The current study describes a novel highly selective alpha2C-adrenoceptor antagonist, JP-1302 (acridin-9-yl-[4-(4-methylpiperazin-1-yl)-phenyl]amine). EXPERIMENTAL APPROACH: Standard in vitro binding and antagonism assays were employed to demonstrate the alpha2C-AR specificity of JP-1302. In addition, JP-1302 was tested in the forced swimming test (FST) and the prepulse-inhibition of startle reflex (PPI) model because mice with genetically altered alpha2C-adrenoceptors have previously been shown to exhibit different reactivity in these tests when compared to wild-type controls. KEY
resultsJP-1302 displayed antagonism potencies (KB values) of 1,500, 2,200 and 16 nM at the human alpha2A-, alpha2B-, and alpha2C-adrenoceptor subtypes, respectively. JP-1302 produced antidepressant and antipsychotic-like effects, i.e. it effectively reduced immobility in the FST and reversed the phencyclidine-induced PPI deficit. Unlike the alpha2-subtype non-selective antagonist atipamezole, JP-1302 was not able to antagonize alpha2-agonist-induced sedation (measured as inhibition of spontaneous locomotor activity), hypothermia, alpha2-agonist-induced mydriasis or inhibition of vas deferens contractions, effects that have been generally attributed to the alpha2A-adrenoceptor subtype. In contrast to JP-1302, atipamezole did not antagonize the PCP-induced prepulse-inhibition deficit. CONCLUSIONS AND IMPLICATIONS: The results provide further support for the hypothesis that specific antagonism of the alpha2C-adrenoceptor may have therapeutic potential as a novel mechanism for the treatment of neuropsychiatric disorders.
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