New piperidinyl-and 1, 2, 3, 6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT 1A receptor agonists with highly potent anti-ischemic effects

…, R Katsuragi-Ogino, M Koyama, M Nakajima…

Index: Kamei, Katsuhide; Maeda, Noriko; Katsuragi-Ogino, Ryoko; Koyama, Makoto; Nakajima, Mika; Tatsuoka, Toshio; Ohno, Tomochika; Inoue, Teruyoshi Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 12 p. 2990 - 2993

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Citation Number: 29

Abstract

A series of new piperidinyl-and 1, 2, 3, 6-tetrahydropyridinyl-pyrimidine derivatives were synthesized. Among these compounds, 4-methyl-2-(1, 2, 3, 6-tetrahydropyridin-4-yl) pyrimidine derivative 23 (SUN N5147) exhibited sub-nanomolar affinity for 5-HT1A receptor with 1000-fold selectivity over both dopamine D2 and α1-adrenergic receptors and remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t- ...