PMID- 2076478
OWN - NLM
STAT- MEDLINE
DCOM- 19910422
LR  - 20190510
IS  - 0007-1188 (Print)
IS  - 0007-1188 (Linking)
VI  - 101
IP  - 3
DP  - 1990 Nov
TI  - Alterations in histamine receptors of guinea-pig ileal smooth muscle produced 
      during agonist-induced desensitization.
PG  - 587-90
AB  - 1. The effects of prolonged treatment with histamine (10(-4) M, 30 min) on 
      desensitization at histamine H1-receptors of guinea-pig ileal longitudinal muscle 
      were investigated. 2. This treatment did not change either the maximum amount or 
      dissociation constant (Kd) of [3H]-mepyramine binding to membranes of guinea-pig 
      ileal muscle. 3. In contrast, this treatment shifted the histamine inhibition 
      curves of [3H]-mepyramine binding to the right both in the presence and absence 
      of 0.5 mM guanosine-5'-triphosphate (GTP). This rightward shift of the curves 
      occurred rapidly in the first 10 min of exposure to histamine. 4. The histamine 
      inhibition curves were analyzed with a two binding sites model. It was shown that 
      the histamine-induced affinity change of the receptor for the agonist occurred 
      with the high affinity binding component (which comprise about 80% of the total), 
      whereas no significant change occurred with the low affinity component. The 
      GTP-dependent decrease in the affinity of the receptor for the agonist also 
      occurred with the high affinity component both in control and histamine-treated 
      preparations. 5. These studies suggest that histamine-induced desensitization was 
      caused by alteration in the affinity of the receptor for the agonist rather than 
      reduction in the number of the receptors and that the interaction of the receptor 
      with a guanine nucleotide regulatory protein was retained in the desensitized 
      state.
FAU - Horio, S
AU  - Horio S
AD  - Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, 
      University of Tokushima, Japan.
FAU - Nakamura, S
AU  - Nakamura S
FAU - Ishida, Y
AU  - Ishida Y
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Br J Pharmacol
JT  - British journal of pharmacology
JID - 7502536
RN  - 0 (Receptors, Histamine H1)
RN  - 820484N8I3 (Histamine)
RN  - 86-01-1 (Guanosine Triphosphate)
RN  - HPE317O9TL (Pyrilamine)
SB  - IM
MH  - Animals
MH  - Female
MH  - Guanosine Triphosphate/pharmacology
MH  - Guinea Pigs
MH  - Histamine/pharmacology
MH  - Ileum/drug effects/*metabolism
MH  - In Vitro Techniques
MH  - Kinetics
MH  - Male
MH  - Muscle, Smooth/drug effects/*metabolism
MH  - Pyrilamine/metabolism
MH  - Receptors, Histamine H1/drug effects/*metabolism
PMC - PMC1917764
EDAT- 1990/11/01 00:00
MHDA- 1990/11/01 00:01
PMCR- 1991/11/01
CRDT- 1990/11/01 00:00
PHST- 1990/11/01 00:00 [pubmed]
PHST- 1990/11/01 00:01 [medline]
PHST- 1990/11/01 00:00 [entrez]
PHST- 1991/11/01 00:00 [pmc-release]
AID - 10.1111/j.1476-5381.1990.tb14125.x [doi]
PST - ppublish
SO  - Br J Pharmacol. 1990 Nov;101(3):587-90. doi: 10.1111/j.1476-5381.1990.tb14125.x.