[Pantogam and pantogam active: qualitative and quantitative features of the interaction with neurotransmitter receptors in vitro].
We conducted a comparative study on the effect of active compounds of pantogam and pantogam active (calcium D(R)-homopantothenate and calcium DL(RS)-homopantothenate) and its L(S)-isomer on the receptors of main brain neuromediators in rats using in vitro radioligand binding analysis. All three compounds interact with binding sites of specific GABA-A and, in particular, GABA-B receptor ligands. Racemate and S-enantiomer, but not its R-form, competed to a moderate degree for D2-receptor binding sites. In all cases, degrees of interaction with receptors were ranged as follows: S-isomer>racemate>R-isomer. These qualitative and quantitative differences are assumed to contribute to pharmacological activity of both drugs.
G I
GI
Kovalev
Iu Iu
IuIu
Firstova
D A
DA
Abaimov
N A
NA
Starikova
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D010205:Pantothenic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D018080:Receptors, GABA-B / Q000378:metabolism*; D013237:Stereoisomerism; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D017448:Receptors, Dopamine D2; D011963:Receptors, GABA-A; D018080:Receptors, GABA-B; C016030:pantogab; D010205:Pantothenic Acid; D005680:gamma-Aminobutyric Acid