Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist
In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H3 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is iden...
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| Veröffentlicht in: | Journal of medicinal chemistry 2004-05, Vol.47 (10), p.2414-2417 |
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| container_end_page | 2417 |
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| container_issue | 10 |
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| container_title | Journal of medicinal chemistry |
| container_volume | 47 |
| creator | Kitbunnadaj, Ruengwit Zuiderveld, Obbe P Christophe, Bernard Hulscher, Saskia Menge, Wiro M. P. B Gelens, Edith Snip, Erwin Bakker, Remko A Celanire, Sylvain Gillard, Michel Talaga, Patrice Timmerman, Henk Leurs, Rob |
| description | In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H3 receptor. Particularly, the 4-pyridinyl analogue of immepip (1c, immethridine) is identified as a novel potent and highly selective histamine H3 receptor agonist (pK i = 9.07, pEC50 = 9.74) with a 300-fold selectivity over the closely related H4 receptor. |
| doi_str_mv | 10.1021/jm049932u |
| format | Article |
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| issn | 0022-2623 1520-4804 |
| language | eng |
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| source | ACS Publications |
| subjects | Biological and medical sciences Medical sciences Miscellaneous Pharmacology. Drug treatments |
| title | Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist |
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