Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist
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Synthesis of 1-arylsulfonyl pyrrolo[1,2-a]quinoxalines: Scope and limitation
2023, Tetrahedron LettersRoute to pyrrolo[1,2-a]quinoxalines via a furan ring opening-pyrrole ring closure sequence
2020, Tetrahedron LettersCitation Excerpt :Pyrrolo[1,2-a]quinoxalines and their (partially) hydrogenated analogues belong to an important family of heterocycles found in various natural compounds, including those possessing a broad diversity of biological activities. For example, quinoxaline I was recently isolated from Piper nigrum L. and Piper longum L. [1]; compound II is an arginine vasopressin antagonist with selectivity for the V2 receptor [2]; carboxylic acid III and related compounds possess anti-allergic activity [3]; PPQ-102 is an inhibitor of the cystic fibrosis transmembrane conductance regulator [4]; CGS 12066B is a potent and selective agonist for the 5-HT1B receptor [5]; quinoxaline IV is an inhibitor of PARP-1 [6]. The diverse biological activities of pyrrolo[1,2-a]quinoxalines open promising possibilities for drug discovery and development based on this heterocyclic motif (Fig. 1).
The role of peripheral 5-HT<inf>1A</inf>, 5-HT<inf>1B</inf>, 5-HT<inf>1D</inf>, 5-HT<inf>1E</inf> and 5-HT<inf>1F</inf> serotonergic receptors in the reduction of nociception in rats
2010, NeuroscienceCitation Excerpt :The serotonergic drugs tested were selected based on relevant receptor selectivity and efficacy (see Table 1). These included: (i) 5-HT1 receptor agonists such as R(+)-UH-301 (5-HT1A, Björk et al., 1992), CGS-12066A (5-HT1B, Neale et al., 1987), GR46611 (5-HT1B/1D, Barf et al., 1996; O'Neill and Sanger, 1999), BRL54443 (5-HT1E/5-HT1F, Brown et al., 1998) and LY344864 (5-HT1F, Phebus et al., 1997); and (ii) selective 5-HT1 receptor antagonists such as WAY-100635 (5-HT1A, Forster et al., 1995; Fletcher et al., 1996), GR55562 (5-HT1B/1D, Lamothe et al., 1997; Filip et al., 2001), SB224289 (5-HT1B, Selkirk et al., 1998; De Vries et al., 1998) and BRL15572 (5-HT1D antagonist, Price et al., 1997). Since currently there are no selective antagonists for 5-HT1E and 5-HT1F receptors, methiothepin was used based on its moderate affinity for these receptors (see Table 1; Adham et al., 1992; Zgombick et al., 1992).
5-HT<inf>1A</inf> receptor-mediated G protein activation assessed by [ <sup>35</sup>S]GTPγS binding in rat cerebral cortex
2005, European Journal of PharmacologyMechanisms of analgesic action of neurotropin on chronic pain in adjuvant-induced arthritic rat: Roles of descending noradrenergic and serotonergic systems
2005, Journal of Pharmacological Sciences