Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.4.16.2 (
PCP
)
3,761
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The following monohydroxy derivatives of 1-(1-phenylcyclohexyl)piperidine (phencyclidine,
PCP
) were synthesized: o-, m-, and p-phenols of
PCP
,
1-(1-phenylcyclohexyl)-4-piperidinol
, and two stereoisomeric pairs of 3-phenyl-3-(1-piperidinyl)cyclohexanol and 4-phenyl-4-(1-piperidinyl)cyclohexanol. Inhibition of specific binding of tritiated
PCP
, morphine, or quinuclidinyl benzylate (QNB) in rat brain homogenates was measured for these compounds. Inhibition of
PCP
binding for selected compounds correlated with mouse rotarod assay activity. The most characteristic effects of hydroxylation of
PCP
on the cyclohexyl, piperidine, or phenyl moieties are the following: (i) it generally decreases its activity in inhibiting [3H]
PCP
binding by a factor of 10 to 80; (ii) it does not produce a large variation in the affinity for the morphine receptor; (iii) it produces a considerable decrease of the affinity for the muscarinic receptor. An important exception to these general observations was the metaphenolic derivative of
PCP
. This
PCP
derivative has an affinity for the [3H]
PCP
binding sites that is 8 times higher than that of
PCP
itself; its affinity for the muscarinic receptor is only twice lower than that of
PCP
, but its affinity for the morphine receptor is 430 times higher than that of
PCP
and only one order of magnitude lower than that of morphine itself.
...
PMID:Chemical synthesis and molecular pharmacology of hydroxylated 1-(1-phenylcyclohexyl-piperidine derivatives. 627 47
