Selective activation of phosphoinositide hydrolysis by a rigid analogue of glutamate.
Ibotenate and trans-D,L-1-amino-1,3-cyclopentanedicarboxylic acid (trans-ACPD) are rigid analogues of glutamate. Ibotenate has been shown to activate phosphoinositide hydrolysis in rat brain slices. We now report that trans-ACPD also stimulates phosphoinositide hydrolysis but with much higher potency and efficacy than ibotenate. The pharmacological profiles, regional distributions, and developmental regulation of the responses to ibotenate and trans-ACPD are similar, suggesting that these agonists act at the same site. However, trans-ACPD is the first agonist described that is selective for this receptor relative to other excitatory amino acid receptor subtypes.
Desai
M A
MA
Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322.
Conn
P J
PJ
D000596:Amino Acids / Q000494:pharmacology*; D000818:Animals; D003515:Cycloleucine / Q000494:pharmacology*; D005971:Glutamates / Q000502:physiology*; D018698:Glutamic Acid; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism*; D007051:Ibotenic Acid / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D010716:Phosphatidylinositols / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D000596:Amino Acids; D005971:Glutamates; D010716:Phosphatidylinositols; D003515:Cycloleucine; D007051:Ibotenic Acid; D018698:Glutamic Acid