PMID- 23886690
OWN - NLM
STAT- MEDLINE
DCOM- 20140415
LR  - 20130809
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 23
IP  - 17
DP  - 2013 Sep 1
TI  - 3,4-Dihydroxy- and 3,4-methylenedioxy- phenanthrene-type alkaloids with high 
      selectivity for D2 dopamine receptor.
PG  - 4824-7
LID - S0960-894X(13)00811-1 [pii]
LID - 10.1016/j.bmcl.2013.06.078 [doi]
AB  - Dopamine-mediated neurotransmission plays an important role in relevant 
      psychiatric and neurological disorders. Nowadays, there is an enormous interest 
      in the development of new drugs acting at the dopamine receptors (DR) as 
      potential new targets for the treatment of schizophrenia or Parkinson's disease. 
      Previous studies have revealed that isoquinoline compounds such as 
      tetrahydroisoquinolines (THIQs) can behave as selective D2 dopaminergic 
      alkaloids. In the present study we have synthesized five aporphine compounds and 
      five phenanthrene alkaloids and evaluated their potential dopaminergic activity. 
      Binding studies on rat striatal membranes were used to evaluate their affinity 
      and selectivity towards D1 and D2 DR. Phenanthrene type alkaloids, in particular 
      the 3,4-dihydroxy- and 3,4-methylenedioxy derivatives, displayed high selectivity 
      towards D2 DR. Therefore, they are potential candidates to be used in the 
      treatment of schizophrenia (antagonists) or Parkinson's disease (agonists) due to 
      their scarce D1 DR-associated side effects.
CI  - Copyright (c) 2013 Elsevier Ltd. All rights reserved.
FAU - Moreno, Laura
AU  - Moreno L
AD  - Departamento de Farmacologia, Laboratorio de Farmacoquimica, Facultad de 
      Farmacia, Universidad de Valencia, Burjassot, 46100 Valencia, Spain.
FAU - Cabedo, Nuria
AU  - Cabedo N
FAU - Ivorra, Maria Dolores
AU  - Ivorra MD
FAU - Sanz, Maria-Jesus
AU  - Sanz MJ
FAU - Castel, Arturo Lopez
AU  - Castel AL
FAU - Carmen Alvarez, M
AU  - Carmen Alvarez M
FAU - Cortes, Diego
AU  - Cortes D
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20130704
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Alkaloids)
RN  - 0 (Phenanthrenes)
RN  - 0 (Receptors, Dopamine D2)
RN  - 448J8E5BST (phenanthrene)
SB  - IM
MH  - Alkaloids/*chemistry/*pharmacology
MH  - Animals
MH  - Corpus Striatum/drug effects/metabolism
MH  - Humans
MH  - Parkinson Disease/drug therapy
MH  - Phenanthrenes/*chemistry/*pharmacology
MH  - Rats
MH  - Receptors, Dopamine D2/*metabolism
MH  - Schizophrenia/drug therapy
OTO - NOTNLM
OT  - Aporphines
OT  - Dopamine receptors
OT  - Phenanthrene alkaloids
OT  - Structure-activity relationships
EDAT- 2013/07/28 06:00
MHDA- 2014/04/16 06:00
CRDT- 2013/07/27 06:00
PHST- 2013/05/30 00:00 [received]
PHST- 2013/06/24 00:00 [revised]
PHST- 2013/06/27 00:00 [accepted]
PHST- 2013/07/27 06:00 [entrez]
PHST- 2013/07/28 06:00 [pubmed]
PHST- 2014/04/16 06:00 [medline]
AID - S0960-894X(13)00811-1 [pii]
AID - 10.1016/j.bmcl.2013.06.078 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2013 Sep 1;23(17):4824-7. doi: 10.1016/j.bmcl.2013.06.078. 
      Epub 2013 Jul 4.