PMID- 10633171
OWN - NLM
STAT- MEDLINE
DCOM- 20000225
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 387
IP  - 1
DP  - 2000 Jan 3
TI  - Constitutive activity of the histamine H(1) receptor reveals inverse agonism of 
      histamine H(1) receptor antagonists.
PG  - R5-7
AB  - Transient expression of the wild-type human histamine H(1) receptor in 
      SV40-immortalised African green monkey kidney cells resulted in an 
      agonist-independent elevation of the basal levels of the second messenger 
      inositoltrisphospate. Several histamine H(1) receptor antagonists, including the 
      therapeutically used anti-allergics cetirizine, loratadine and epinastine reduced 
      this constitutive histamine H(1) receptor activity. Inverse agonism, i.e., 
      stabilisation of an inactive conformation of the human histamine H(1) receptor, 
      may therefore be a key component of the anti-allergic mechanism of action of 
      clinically used antihistamines.
FAU - Bakker, R A
AU  - Bakker RA
AD  - Department of Pharmacochemistry, Division of Medicinal Chemistry, 
      Leiden/Amsterdam Center for Drug Research, Vrije Universiteit Amsterdam, De 
      Boelelaan 1083, 1081 HV, Amsterdam, Netherlands.
FAU - Wieland, K
AU  - Wieland K
FAU - Timmerman, H
AU  - Timmerman H
FAU - Leurs, R
AU  - Leurs R
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Histamine Agonists)
RN  - 0 (Histamine H1 Antagonists)
RN  - 0 (Inositol Phosphates)
RN  - 0 (Methylhistidines)
RN  - 0 (Receptors, Histamine H1)
RN  - 0 (Recombinant Fusion Proteins)
RN  - 70050-43-0 (alpha-fluoromethylhistidine)
RN  - 820484N8I3 (Histamine)
RN  - HPE317O9TL (Pyrilamine)
SB  - IM
MH  - Animals
MH  - Binding, Competitive
MH  - COS Cells
MH  - Cell Line, Transformed
MH  - Histamine/pharmacology
MH  - Histamine Agonists/metabolism/*pharmacology
MH  - Histamine H1 Antagonists/metabolism/*pharmacology
MH  - Humans
MH  - Inositol Phosphates/metabolism
MH  - Methylhistidines/pharmacology
MH  - Pyrilamine/metabolism/pharmacology
MH  - Radioligand Assay
MH  - Receptors, Histamine H1/*drug effects/genetics/metabolism
MH  - Recombinant Fusion Proteins/drug effects/genetics/metabolism
EDAT- 2000/01/14 09:00
MHDA- 2000/03/04 09:00
CRDT- 2000/01/14 09:00
PHST- 2000/01/14 09:00 [pubmed]
PHST- 2000/03/04 09:00 [medline]
PHST- 2000/01/14 09:00 [entrez]
AID - S0014-2999(99)00803-1 [pii]
AID - 10.1016/s0014-2999(99)00803-1 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2000 Jan 3;387(1):R5-7. doi: 10.1016/s0014-2999(99)00803-1.