E-resources
Peer reviewed
-
Patrick, K S; Caldwell, R W; Ferris, R M; Breese, G R
The Journal of pharmacology and experimental therapeutics, 04/1987, Volume: 241, Issue: 1Journal Article
The pharmacology of the enantiomers of threo-methylphenidate (MPH) was evaluated in the rat to assess the relative contribution of each isomer to central and peripheral actions of the racemic drug. Fractional recrystallization of binaphthyl phosphate salts of dl-threo-MPH allowed resolution of d-threo-MPH and 92% enrichment of l-threo-MPH. The enantiomeric disposition was monitored using gas chromatographic separation of trifluoroacetylprolyl diastereomeric derivatives. The activity of the d-isomer was greater than the l-isomer in the induction of locomotor activity and the inhibition of tritiated dopamine and l-norepinephrine uptake into striatal and hypothalamic synaptosomes, respectively. Neither isomer produced a significant change in the spontaneous release of tritiated catecholamines from synaptosomes. Destruction of catecholaminergic neurons by 6-hydroxydopamine pretreatment attenuated the locomotor response to d-threo-MPH, indicating the involvement of catecholaminergic neural pathways in the locomotor response. Only the d-enantiomer significantly potentiated the pressor responses to i.v. l-norepinephrine. Receptor site stereoselectively for threo- vs. erythro-MPH is discussed in terms of isomer conformational preferences. These results suggest that synaptic inhibition of catecholamine uptake by d-threo-MPH may be involved fundamentally in behavioral and pressor effects of the racemic drug.
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|
Source: Personal bibliographies
and: SICRIS
The material is available in full text. If you wish to order the material anyway, click the Continue button.