Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.

Authors :: Austin NE
Avenell KY
Boyfield I
Branch CL
Hadley MS
Jeffrey P
Johnson CN
Macdonald GJ
Nash DJ
Riley GJ
Smith AB
Stemp G
Thewlis KM
Vong AK
Wood M
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2000 Nov 20; Vol. 10 (22), pp. 2553-5.
Publication Year :: 2000
Abstract: Starting from the dopamine D3 receptor antagonist SB-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinity for the dopamine D3 receptor and selectivity over the D2 receptor. The 3-acetamido-2-fluorocinnamide derivative 20 gave high D3 receptor affinity (pKi 8.4) with 130-fold selectivity over the 2, receptor.

Subjects :: Animals
Nitriles chemistry
Quinolines chemistry
Rats
Receptors, Dopamine D3
Nitriles pharmacology
Quinolines pharmacology
Receptors, Dopamine D2 drug effects
Tetrahydroisoquinolines

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