PMID- 6094741
OWN - NLM
STAT- MEDLINE
DCOM- 19841227
LR  - 20191101
IS  - 0270-6474 (Print)
IS  - 1529-2401 (Electronic)
IS  - 0270-6474 (Linking)
VI  - 4
IP  - 11
DP  - 1984 Nov
TI  - Modification of guanine nucleotide-regulatory components in brain membranes. I. 
      Changes in guanosine 5'-triphosphate regulation of opiate receptor-binding sites.
PG  - 2755-63
AB  - Guanine nucleotides regulate binding of opiate agonists to membrane receptors by 
      increasing agonist dissociation rates. The current study demonstrates that the 
      ability of guanosine 5'-triphosphate (GTP) and its nonhydrolyzable analogue 
      guanylyl-5'-imidodiphosphate (Gpp(NH)p) to inhibit opiate agonist binding to rat 
      brain membranes can be altered by two methods: by preincubating with EDTA, and by 
      preincubating at pH 4.5. EDTA pretreatment increased the potency of Gpp(NH)p in 
      inhibiting [3H]morphine binding by 4-fold, with little apparent change in the 
      maximum effect of Gpp(NH)p or on levels of binding itself. The effect of EDTA 
      pretreatment was blocked by prior incubation of membranes with excess calcium or 
      manganese but could not be reversed by any divalent cation if the EDTA incubation 
      was longer than 10 min. EDTA pretreatment increased the effects of GTP on 
      dissociation rates of agonists. Pretreatment of membranes at pH 4.5 increased the 
      ability of guanine nucleotides to regulate agonist binding by increasing the 
      maximum effect of Gpp(NH)p from 50% to 80% inhibition of [3H]morphine binding 
      with minor increase in potency of Gpp(NH)p. The actions of EDTA and low pH 
      pretreatments were additive when both were conducted on the same membranes. These 
      results suggest that modification of brain membranes can alter the interaction of 
      receptors with guanine nucleotide-regulatory components which may lead to changes 
      in post-receptor membrane events.
FAU - Lambert, S M
AU  - Lambert SM
FAU - Childers, S R
AU  - Childers SR
LA  - eng
GR  - DA-02094/DA/NIDA NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - J Neurosci
JT  - The Journal of neuroscience : the official journal of the Society for 
      Neuroscience
JID - 8102140
RN  - 0 (Cations, Divalent)
RN  - 0 (Receptors, Opioid)
RN  - 34273-04-6 (Guanylyl Imidodiphosphate)
RN  - 42Z2K6ZL8P (Manganese)
RN  - 76I7G6D29C (Morphine)
RN  - 86-01-1 (Guanosine Triphosphate)
RN  - 9G34HU7RV0 (Edetic Acid)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Animals
MH  - Brain/*metabolism
MH  - Calcium/pharmacology
MH  - Cations, Divalent
MH  - Cell Membrane/metabolism
MH  - Edetic Acid/pharmacology
MH  - Guanosine Triphosphate/*pharmacology
MH  - Guanylyl Imidodiphosphate/pharmacology
MH  - Hydrogen-Ion Concentration
MH  - Kinetics
MH  - Male
MH  - Manganese/pharmacology
MH  - Morphine/metabolism
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Receptors, Opioid/drug effects/*metabolism
PMC - PMC6564730
EDAT- 1984/11/01 00:00
MHDA- 1984/11/01 00:01
PMCR- 1985/05/01
CRDT- 1984/11/01 00:00
PHST- 1984/11/01 00:00 [pubmed]
PHST- 1984/11/01 00:01 [medline]
PHST- 1984/11/01 00:00 [entrez]
PHST- 1985/05/01 00:00 [pmc-release]
AID - 10.1523/JNEUROSCI.04-11-02755.1984 [doi]
PST - ppublish
SO  - J Neurosci. 1984 Nov;4(11):2755-63. doi: 10.1523/JNEUROSCI.04-11-02755.1984.