2004
DOI: 10.1016/j.bmcl.2003.11.050
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Thiazoles and thiopyridines: novel series of high affinity h5HT7 ligands

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Cited by 32 publications
(10 citation statements)
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“…To date, the search for 5-HT 7 receptor antagonists has led to the discovery of LY215840 [3], SB-258719 [4], DR4004 [5], SB-269970 [6], and SB-656104-A [7]. Regarding 5-HT 7 receptor agonists, AS-19 [8, 9], MSD-5a [10], LP-44 [11], LP-211 [12], E-55888 [13], and E-57431 [14] have been developed. However, most of these agonists display rather modest selectivity because their affinity for the 5-HT 7 type is only 11-fold higher than for 5-HT 1D in case of AS-19 [13], 28.6-fold higher than for 5-HT 1A in case of MSD-5a [10], and 33-fold higher than for dopamine D2 receptor [15], and 5-14-fold higher than for 5-HT 1B , 5-HT 2B , 5-HT 2C , and 5-HT 5A in case of LP-211 [16].…”
Section: Introductionmentioning
confidence: 99%
See 1 more Smart Citation
“…To date, the search for 5-HT 7 receptor antagonists has led to the discovery of LY215840 [3], SB-258719 [4], DR4004 [5], SB-269970 [6], and SB-656104-A [7]. Regarding 5-HT 7 receptor agonists, AS-19 [8, 9], MSD-5a [10], LP-44 [11], LP-211 [12], E-55888 [13], and E-57431 [14] have been developed. However, most of these agonists display rather modest selectivity because their affinity for the 5-HT 7 type is only 11-fold higher than for 5-HT 1D in case of AS-19 [13], 28.6-fold higher than for 5-HT 1A in case of MSD-5a [10], and 33-fold higher than for dopamine D2 receptor [15], and 5-14-fold higher than for 5-HT 1B , 5-HT 2B , 5-HT 2C , and 5-HT 5A in case of LP-211 [16].…”
Section: Introductionmentioning
confidence: 99%
“…Regarding 5-HT 7 receptor agonists, AS-19 [8, 9], MSD-5a [10], LP-44 [11], LP-211 [12], E-55888 [13], and E-57431 [14] have been developed. However, most of these agonists display rather modest selectivity because their affinity for the 5-HT 7 type is only 11-fold higher than for 5-HT 1D in case of AS-19 [13], 28.6-fold higher than for 5-HT 1A in case of MSD-5a [10], and 33-fold higher than for dopamine D2 receptor [15], and 5-14-fold higher than for 5-HT 1B , 5-HT 2B , 5-HT 2C , and 5-HT 5A in case of LP-211 [16]. Indeed, among 5-HT 7 receptor agonists, only E-55888 and E-57431 seem to have a satisfactory selectivity with affinity for the 5-HT 7 receptor 280-fold higher than for 5-HT 1A and 112.7-fold higher than for 5-HT 1D , respectively [13] (see Table 1).…”
Section: Introductionmentioning
confidence: 99%
“…Recent thiazoles [18] were of a comparative affinity but here, the most promising antidepressants effects in mice support further development of our easily available ligands as new agents in the treatment of depression. …”
Section: Animal Studies In Micementioning
confidence: 92%
“…Merck Sharp & Dohme Ltd. presented the first descriptions of a programme that was only recently disclosed in a patent application, in which novel substituted carbocyclic sulfonamide derivatives (88) and methods of their use for treating conditions alleviated by 5-HT 7 receptor antagonism are claimed. The series explored the activity of structures that incorporated the phenylsulfonyl and 1-piperazinyl fragments employed by the GSK scientists in the discovery of the 5-HT 7 antagonists SB-269970 (18).…”
Section: Emerging 5-ht 7 Receptor Antagonistsmentioning
confidence: 99%
“…Pyridine derivative 93 still remains the compound with the highest affinity, and the most selective from the two series. This compound was therefore tested in a functional assay with a β-lactamase reporter gene assay (using Aurora 3, HEK293/cyclic AMP response element [CRE] β-lactamase reporter cells stably transfected with the h5-HT 7 receptor) and found to behave as a partial agonist, giving 80% of the response of the full agonist 5-CT in h5-HT 7 receptors [88]. A patent application assigned to Sigma-Tau Industries Farmaceutiche Riunite SpA claiming known non-selective 5-halotryptamine derivatives (96) and their use as 5-HT 6 and/or 5-HT 7 serotoninergic receptor ligands for the treatment of a variety of nervous system pathologies, including migraine, depression, psychosis, mood disorders, schizophrenia, motor disorders, cognitive disorders, Parkinson's disease, Alzheimer's disease or Huntington's disease, and for the treatment of systemic pathologies involving the cardiovascular system and the gastrointestinal tract, such as hypertension and irritable bowel disease.…”
Section: Emerging 5-ht 7 Receptor Antagonistsmentioning
confidence: 99%