Title : The role of physicochemical properties of entacapone and tolcapone on their efficacy during local intrastriatal administration.

Pub. Date : 2005 Apr

PMID : 15784340






6 Functional Relationships(s)
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1 Aqueous solubility, apparent partition coefficient (logPapp) and catechol-O-methyltransferase (COMT, EC 2.1.1.6) inhibiting potency of entacapone and tolcapone were compared in vitro. entacapone catechol-O-methyltransferase Rattus norvegicus
2 Aqueous solubility, apparent partition coefficient (logPapp) and catechol-O-methyltransferase (COMT, EC 2.1.1.6) inhibiting potency of entacapone and tolcapone were compared in vitro. entacapone catechol-O-methyltransferase Rattus norvegicus
3 Entacapone and tolcapone inhibited equally rat striatal COMT in vitro with Ki values of 1.86 and 2.50 nM, respectively. entacapone catechol-O-methyltransferase Rattus norvegicus
4 In conclusion, entacapone and tolcapone are equally potent COMT inhibitors against rat striatal COMT in vitro. entacapone catechol-O-methyltransferase Rattus norvegicus
5 In conclusion, entacapone and tolcapone are equally potent COMT inhibitors against rat striatal COMT in vitro. entacapone catechol-O-methyltransferase Rattus norvegicus
6 After local intrastriatal administration, entacapone appeared to inhibit COMT faster and more effectively than the more lipophilic tolcapone. entacapone catechol-O-methyltransferase Rattus norvegicus