- Centrally acting 6,7,8,9-tetrahydro-3H-benz(E)indole heterocyclics
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A compound of Formula I STR1 or pharmaceutically acceptable salts of Formula I, where R1 is H, C1 -C3 alkyl, --(CH2)n CONH2 where n is 2 to 6, (CH2)n -1-(4,4-dimethylpiperidine-2
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- Synthesis of (R)- and (S)-1-formyl-6,7,8,9-tetrahydro-N,N-(dipropyl)-3H- benz[e]indol-8-amines: Potent and orally active 5-HT(1A) receptor agonists
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An efficient synthesis of the potent and orally active 5-HT(1A) agonists, (R)-(+)- and (S)-(-)-l-formyl-6,7,8,9-tetrahydro-N,N-dipropyl-3H- benz[e]indol-8-amines 1a and 1b, is described. This synthesis was accomplished in twelve steps from commercially av
- Lin,Ennis,Hoffman,Phillips,Haadsma-Svensson,Ghazal,Chidester
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p. 129 - 139
(2007/10/02)
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- Centrally acting 6,7,8,9-tetrahydro-3H-benz(e)indole heterocyclics
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A compound of Formula I STR1 or pharmaceutically acceptable salts of Formula I, where R 1 is H, C 1 -C 3 alkyl, --(CH 2) n CONH 2 where n is 2 to 6, (CH2) n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R 2 is hydrogen, C 1 -C 8 alkyl, C
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- (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: A new class of orally active 5-HT(1A)-receptor agonists
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The enantiomers of 6,7,8,9-tetrahydro-N,N-di-n-propyl-3H-benz[e]indol-8- amine (S-(-)-2b and R-(+)-2b) and their corresponding 1-formyl analogs (S-(- )-6 and R-(+)-6 were prepared and evaluated pharmacologically for serotonergic and dopaminergic activity. The introduction of a formyl group in the 1-position shifted the pharmacological profile of 2b from a mixed D2/5- HT(1A) agonists to a selective 5-HT(1A) agonist (6). The enantiomers of 6 were agonists with full intrinsic activity and had an affinity comparable to that of 8-hydroxy-2-(di-n-propylamino)tetrahydronaphthalene (8-OH-DPAT). In contrast to 8-OH-DPAT, the enantiomers of compound 6 were found to have good oral availability.
- Stjernlof,Gullme,Elebring,Andersson,Wikstrom,Lagerquist,Svensson,Ekman,Carlsson,Sundell
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p. 2059 - 2065
(2007/10/02)
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