1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors.
Amino acid derivatives of 1,2,5-thiadiazol-3-yl-piperazine related to (+)-WAY-100135 and WAY-100635 are potent 5-HT1A receptor agonists and antagonists, which have selective affinity for 5-HT1A receptors versus alpha1 and dopamine (D2, D3, and D4) receptors.
Sabb
A L
AL
Medicinal Chemistry, Chemical Sciences, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. sabba@war.wyeth.com
Vogel
R L
RL
Kelly
M G
MG
Palmer
Y
Y
Smith
D L
DL
Andree
T H
TH
Schechter
L E
LE
D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D010879:Piperazines / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects; D011954:Receptors, Dopamine / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D013830:Thiadiazoles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*
D000596:Amino Acids; D010879:Piperazines; D011725:Pyridines; D018340:Receptors, Adrenergic, alpha-1; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D013830:Thiadiazoles; C081293:WAY 100135; C090413:N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide