2,7-diazabicyclo[3.3.0]octanes as novel h5-HT receptor agonists.
The conformational restriction of a (benzylamino)methyl substituted pyrrolidine to form 2,7-diazabicyclo[3.3.0]octanes has led to a series of compounds with high affinity at the h5-HT1D receptor as well as dramatically increased concentrations in the hepatic portal vein following oral administration.
Russell
M G
MG
Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK. michael_russell@merck.com
Beer
M S
MS
Stanton
J A
JA
Sohal
B
B
Mortishire-Smith
R J
RJ
Castro
J L
JL
D000284:Administration, Oral; D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000187:drug effects*; D011994:Recombinant Proteins / Q000187:drug effects; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
D019086:Bridged Bicyclo Compounds, Heterocyclic; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D011994:Recombinant Proteins; D017366:Serotonin Receptor Agonists