(2S,3S,4S)-alpha-Carboxycyclopropylglycine (L-CCG I) and trans-1-amino-(1S,3R)-cyclopentanedicarboxylic acid ((1S,3R)-ACPD), partially constrained L-glutamate analogs known to be agonists at the metabotropic glutamate receptors (mGluRs) adenylyl cyclase coupled, have been submitted to conformational analysis and the data obtained utilized to define a pharmacophore which takes into account the location of hydrogen bonding donating sites of the receptor. This pharmacophore has been utilized to define the agonist mGluRs decreases cAMP bioactive conformation of L-Glu.
Definition of a Pharmacophore for the Metabotropic Glutamate Receptors Negatively Linked to Adenylyl Cyclase / Costantino, Gabriele; B., Natalini; R., Pellicciari; F., Moroni; G., Lombardi. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 1:(1993), pp. 259-264.
Definition of a Pharmacophore for the Metabotropic Glutamate Receptors Negatively Linked to Adenylyl Cyclase
COSTANTINO, Gabriele;
1993-01-01
Abstract
(2S,3S,4S)-alpha-Carboxycyclopropylglycine (L-CCG I) and trans-1-amino-(1S,3R)-cyclopentanedicarboxylic acid ((1S,3R)-ACPD), partially constrained L-glutamate analogs known to be agonists at the metabotropic glutamate receptors (mGluRs) adenylyl cyclase coupled, have been submitted to conformational analysis and the data obtained utilized to define a pharmacophore which takes into account the location of hydrogen bonding donating sites of the receptor. This pharmacophore has been utilized to define the agonist mGluRs decreases cAMP bioactive conformation of L-Glu.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.