title: New L-dopa codrugs as potential antiparkinson agents.
abstract: This paper reports the synthesis and preliminary evaluation of new L-dopa (LD) conjugates (1 and 2) obtained by joining LD with two different natural antioxidants, caffeic acid and carnosine, respectively. The antioxidant efficacy of compounds 1 and 2 was assessed by evaluating plasmatic activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx) in the rat. Rat striatal concentration of LD and dopamine (DA), and central nervous effects were evaluated after oral administration of the codrugs 1 and 2. The results suggest that, though our codrugs are devoid of significant antioxidant activity, they are able to induce sustained delivery of DA in rat striatum and can improve LD and DA release in the brain.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università G D'Annunzio, Chieti, Italy.
authors.forename: Piera
authors.initials: P
authors.lastname: Sozio
authors.forename: Antonio
authors.initials: A
authors.lastname: Iannitelli
authors.forename: Laura Serafina
authors.initials: LS
authors.lastname: Cerasa
authors.forename: Ivana
authors.initials: I
authors.lastname: Cacciatore
authors.forename: Catia
authors.initials: C
authors.lastname: Cornacchia
authors.forename: Gianfabio
authors.initials: G
authors.lastname: Giorgioni
authors.forename: Massimo
authors.initials: M
authors.lastname: Ricciutelli
authors.forename: Cinzia
authors.initials: C
authors.lastname: Nasuti
authors.forename: Franco
authors.initials: F
authors.lastname: Cantalamessa
authors.forename: Antonio
authors.initials: A
authors.lastname: Di Stefano
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000978:Antiparkinson Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002109:Caffeic Acids / Q000737:chemistry / Q000494:pharmacology; D002336:Carnosine / Q000737:chemistry / Q000494:pharmacology; D003342:Corpus Striatum / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D005979:Glutathione Peroxidase / Q000378:metabolism; D007980:Levodopa / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D010300:Parkinson Disease / Q000188:drug therapy*; D051381:Rats; D013482:Superoxide Dismutase / Q000378:metabolism
chemical_list: D000975:Antioxidants; D000978:Antiparkinson Agents; D002109:Caffeic Acids; D007980:Levodopa; D002336:Carnosine; D005979:Glutathione Peroxidase; D013482:Superoxide Dismutase; C040048:caffeic acid; D004298:Dopamine