PMID- 2985852
OWN - NLM
STAT- MEDLINE
DCOM- 19850528
LR  - 20190725
IS  - 0021-5198 (Print)
IS  - 0021-5198 (Linking)
VI  - 37
IP  - 1
DP  - 1985 Jan
TI  - Effects of calcium hopantenate on neurotransmitter receptors in the rat brain.
PG  - 45-50
AB  - Effects of calcium hopantenate (HOPA) on neurotransmitter and neuropeptide 
      receptors in the central nervous system (CNS) were investigated. In the 
      radioreceptor assay (RRA), HOPA inhibited the [3H]-gamma-aminobutylic acid (GABA) 
      receptor binding in a dose-dependent manner with a cross-reactive potency of 
      0.2%. On the other hand, radiolabeled ligand binding to CNS receptors in the 
      benzodiazepine (BDZ)-, muscarinic cholinergic (mACh)-, methionine-enkephalin 
      (ENK)- and thyrotropin releasing hormone (TRH)-RRA systems was not inhibited even 
      by the addition of HOPA up to 100 microM. Repeated injection of HOPA (250 
      mg/kg/day for 7 consecutive days) increased GABA receptor binding by 53% in the 
      cerebral cortex, while GABA binding in the rest of the forebrain did not change. 
      The increased GABA receptor binding in the cerebral cortex of HOPA treated rats 
      was due to the increased affinity of the binding sites. BDZ-, mACh-, ENK- and 
      TRH-receptor bindings were not affected in either the cerebral cortex or the rest 
      of the forebrain by repeated injection of HOPA. These results suggest that at 
      least a part of the therapeutic efficacy of HOPA is due to sensitization of the 
      GABA receptor in the cerebral cortex.
FAU - Ogawa, N
AU  - Ogawa N
FAU - Nukina, I
AU  - Nukina I
FAU - Hirose, Y
AU  - Hirose Y
FAU - Fukushima, M
AU  - Fukushima M
FAU - Mori, A
AU  - Mori A
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Japan
TA  - Jpn J Pharmacol
JT  - Japanese journal of pharmacology
JID - 2983305R
RN  - 0 (Receptors, Cell Surface)
RN  - 0 (Receptors, GABA-A)
RN  - 0 (Receptors, Muscarinic)
RN  - 0 (Receptors, Neurotransmitter)
RN  - 0 (Receptors, Opioid)
RN  - 0 (Receptors, Thyrotropin-Releasing Hormone)
RN  - 1977-33-9 (pantogab)
RN  - 19F5HK2737 (Pantothenic Acid)
RN  - 56-12-2 (gamma-Aminobutyric Acid)
RN  - M4I0D6VV5M (Calcium Chloride)
SB  - IM
MH  - Animals
MH  - Brain Chemistry/*drug effects
MH  - Calcium Chloride/pharmacology
MH  - In Vitro Techniques
MH  - Kinetics
MH  - Male
MH  - Pantothenic Acid/*analogs & derivatives/pharmacology
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Receptors, Cell Surface/drug effects
MH  - Receptors, GABA-A/drug effects
MH  - Receptors, Muscarinic/drug effects
MH  - Receptors, Neurotransmitter/*drug effects
MH  - Receptors, Opioid/drug effects
MH  - Receptors, Thyrotropin-Releasing Hormone
MH  - Synaptic Membranes/metabolism
MH  - gamma-Aminobutyric Acid/*analogs & derivatives/pharmacology
EDAT- 1985/01/01 00:00
MHDA- 1985/01/01 00:01
CRDT- 1985/01/01 00:00
PHST- 1985/01/01 00:00 [pubmed]
PHST- 1985/01/01 00:01 [medline]
PHST- 1985/01/01 00:00 [entrez]
AID - 10.1254/jjp.37.45 [doi]
PST - ppublish
SO  - Jpn J Pharmacol. 1985 Jan;37(1):45-50. doi: 10.1254/jjp.37.45.