lobelane and piperidine

lobelane has been researched along with piperidine* in 1 studies

Other Studies

1 other study(ies) available for lobelane and piperidine

Article	Year
Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2. Bioorganic & medicinal chemistry letters, 2008, Dec-15, Volume: 18, Issue:24 A series of lobelane homologues has been synthesized and evaluated for their [(3)H]DTBZ binding affinity at the vesicular monoamine transporter-2 (VMAT2). The structure-activity relationships (SAR) indicate that for retention of binding affinity at VMAT2, the lengths of the methylene linkers should be no shorter than one methylene unit at C-6 of the piperidine ring, and no shorter than two methylene units at C-2 of the piperidine ring. These results indicate that the intramolecular distances between the piperidine ring and two phenyl rings in lobelane analogues are an important criterion for retention of high affinity at VMAT2. Topics: Animals; Binding Sites; Chemistry, Pharmaceutical; Drug Design; Humans; Kinetics; Lobeline; Models, Chemical; Oxygen; Piperidines; Rats; Structure-Activity Relationship; Vesicular Biogenic Amine Transport Proteins; Vesicular Monoamine Transport Proteins	2008

Article

Year

Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2.

Bioorganic & medicinal chemistry letters, 2008, Dec-15, Volume: 18, Issue:24

A series of lobelane homologues has been synthesized and evaluated for their [(3)H]DTBZ binding affinity at the vesicular monoamine transporter-2 (VMAT2). The structure-activity relationships (SAR) indicate that for retention of binding affinity at VMAT2, the lengths of the methylene linkers should be no shorter than one methylene unit at C-6 of the piperidine ring, and no shorter than two methylene units at C-2 of the piperidine ring. These results indicate that the intramolecular distances between the piperidine ring and two phenyl rings in lobelane analogues are an important criterion for retention of high affinity at VMAT2.

Topics: Animals; Binding Sites; Chemistry, Pharmaceutical; Drug Design; Humans; Kinetics; Lobeline; Models, Chemical; Oxygen; Piperidines; Rats; Structure-Activity Relationship; Vesicular Biogenic Amine Transport Proteins; Vesicular Monoamine Transport Proteins

2008