STRUCTURE-ACTIVITY STUDIES ON THE INHIBITION OF GABA BINDING TO RAT BRAIN MEMBRANES BY MUSCIMOL AND RELATED COMPOUNDS

1978 ◽  
Vol 30 (6) ◽  
pp. 1377-1382 ◽  
Author(s):  
P. Krogsgaard-Larsen ◽  
G. A. R. Johnston
Keyword(s):  
Rat Brain ◽  
Brain Membranes ◽  
Structure Activity ◽  
Rat Brain Membranes ◽  
Gaba Binding ◽  
Related Compounds

β-Carboline-3-carboxylic Acid (9H-Pyrido[3,4-b]indole-3-carboxylic Acid) and Related Compounds

1989 ◽  
Vol 42 (6) ◽  
pp. 813 ◽  
Author(s):  
JA Maclaren
Keyword(s):  
Carboxylic Acid ◽  
Rat Brain ◽  
High Yield ◽  
Brain Membranes ◽  
Novel Synthesis ◽  
Rat Brain Membranes ◽  
Related Compounds ◽  
Relative Inhibition

The synthesis of β-carboline-3-carboxylic acid and its esters (4) by oxidation of the corresponding 1,2,3,4-tetrahydro derivatives (2) or of the 3,4-dihydro derivatives (3) has been studied. A novel synthesis of the esters (3) [and hence of (4)] has been achieved in high yield by cyclization and elimination from the enamine (5). The relative inhibition of binding of a benzodiazepine to rat brain membranes by the esters (2)-(4) has been determined.

Synthesis of analogues of GABA. IX. 5-(Aminomethyl)-3-hydroxyfuran-2(5H)-one

1983 ◽  
Vol 36 (5) ◽  
pp. 977 ◽  
Author(s):  
RD Allan ◽  
GAR Johnston ◽  
R Kazlauskas ◽  
H Tran
Keyword(s):  
Singlet Oxygen ◽  
Rat Brain ◽  
Keto Group ◽  
Gaba Agonist ◽  
Mild Conditions ◽  
Brain Membranes ◽  
Rat Brain Membranes ◽  
Gaba Binding

5-(Aminomethyl)-3-hydroxyfuran-2(5H)-one (4) has been synthesized as a GABA analogue in five steps from hex-3-enedioic acid, the enolic α-keto group being introduced under mild conditions by means of a singlet oxygen cleavage of an enamino lactone. The compound showed negligible activity as a GABA agonist with respect to inhibition of [3H]GABA binding, uptake and trans amination in rat brain membranes

Diazepam enhancement of low affinity GABA binding to rat brain membranes

1982 ◽  
Vol 29 (1) ◽  
pp. 63-66 ◽  
Author(s):  
John H. Skerritt ◽  
Max Willow ◽  
Graham A.R. Johnston
Keyword(s):  
Rat Brain ◽  
Brain Membranes ◽  
Rat Brain Membranes ◽  
Gaba Binding

Modulation of GABA binding to rat brain membranes by alkyl β-carboline-3-carboxylate esters

1982 ◽  
Vol 86 (2) ◽  
pp. 299-301 ◽  
Author(s):  
John H. Skerritt ◽  
Graham A.R. Johnston ◽  
Claus Braestrup
Keyword(s):  
Rat Brain ◽  
Brain Membranes ◽  
Rat Brain Membranes ◽  
Gaba Binding

Synthesis of analogues of GABA. X. The bicyclic β-diketone Octahydro-1H-2-pyrindine-5,7-dione

1983 ◽  
Vol 36 (6) ◽  
pp. 1221 ◽  
Author(s):  
RD Allan ◽  
J Fong
Keyword(s):  
Rat Brain ◽  
Carboxyl Group ◽  
Gaba Agonists ◽  
Brain Membranes ◽  
Rat Brain Membranes ◽  
Gaba Binding ◽  
Weak Activity

The synthesis is described of octahydro-1H-2-pyrindine-5,7-dione (4) and its 6-diazo and 6-bromo derivatives. These are analogues of GABA in which the carboxyl group is replaced by an enolic β-diketone. The compounds showed negligible or very weak activity as GABA agonists with respect to inhibition of [3H] GABA binding, uptake and transamination in rat brain membranes.

scholarly journals Dimeric Dermorphin Analogues as µ-Receptor Probes on Rat Brain Membranes

1989 ◽  
Vol 264 (1) ◽  
pp. 354-362
Author(s):  
L H Lazarus ◽  
A Guglietta ◽  
W E Wilson ◽  
B J Irons ◽  
R de Castiglione
Keyword(s):  
Rat Brain ◽  
Brain Membranes ◽  
Rat Brain Membranes ◽  
Dermorphin Analogues
Sign in / Sign up

Export Citation Format

Share Document