Tags

Type your tag names separated by a space and hit enter

The antiproliferative potency of histamine antagonists correlates with inhibition of binding of [3H]-histamine to novel intracellular receptors (HIC) in microsomal and nuclear fractions of rat liver.
Agents Actions Suppl. 1991; 33:325-42.AA

Abstract

Previously, we identified in rat liver microsomes, low (microM) affinity histamine receptors (HIC), associated with antiestrogen binding sites (AEBS). N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE), a potent AEBS ligand, is a specific HIC antagonist. Through binding HIC, newly-formed intracellular histamine mediates, and DPPE inhibits, human platelet aggregation. We now provide evidence that histamine, mobilized from cytoplasmic stores, is a mediator of the mitogenic response to concanavalin A in mouse spleen cells. DNA synthesis and intracellular histamine levels are decreased over time by the histidine decarboxylase inhibitor, alpha-fluoromethylhistidine. For DPPE, H1 and H2 antagonists, rank order of potency to inhibit [3H]-histamine binding to HIC in rat liver microsomes correlates with antiproliferative potency. DPPE also competes for [3H]-histamine binding at low and high affinity sites in rat liver nuclei (IC50 approximately 2 microM). Thus, histamine may mediate growth through two intracellular subtypes of HIC.

Authors+Show Affiliations

Brandes LJ
Department of Medicine, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
Davie JR
No affiliation info available
Paraskevas F
No affiliation info available
Sukhu B
No affiliation info available
Bogdanovic RP
No affiliation info available
LaBella FS
No affiliation info available

MeSH

AnimalsBinding SitesBinding, CompetitiveCell DivisionCell NucleusDNAEstrogen AntagonistsHistamineHistamine AntagonistsLiverMaleMiceMice, Inbred BALB CMicrosomes, LiverPhenyl EthersPlatelet AggregationPlatelet Aggregation InhibitorsRatsRats, Inbred StrainsReceptors, Histamine H1

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

2053513

Citation

Brandes, L J., et al. "The Antiproliferative Potency of Histamine Antagonists Correlates With Inhibition of Binding of [3H]-histamine to Novel Intracellular Receptors (HIC) in Microsomal and Nuclear Fractions of Rat Liver." Agents and Actions. Supplements, vol. 33, 1991, pp. 325-42.
Brandes LJ, Davie JR, Paraskevas F, et al. The antiproliferative potency of histamine antagonists correlates with inhibition of binding of [3H]-histamine to novel intracellular receptors (HIC) in microsomal and nuclear fractions of rat liver. Agents Actions Suppl. 1991;33:325-42.
Brandes, L. J., Davie, J. R., Paraskevas, F., Sukhu, B., Bogdanovic, R. P., & LaBella, F. S. (1991). The antiproliferative potency of histamine antagonists correlates with inhibition of binding of [3H]-histamine to novel intracellular receptors (HIC) in microsomal and nuclear fractions of rat liver. Agents and Actions. Supplements, 33, 325-42.
Brandes LJ, et al. The Antiproliferative Potency of Histamine Antagonists Correlates With Inhibition of Binding of [3H]-histamine to Novel Intracellular Receptors (HIC) in Microsomal and Nuclear Fractions of Rat Liver. Agents Actions Suppl. 1991;33:325-42. PubMed PMID: 2053513.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The antiproliferative potency of histamine antagonists correlates with inhibition of binding of [3H]-histamine to novel intracellular receptors (HIC) in microsomal and nuclear fractions of rat liver. AU - Brandes,L J, AU - Davie,J R, AU - Paraskevas,F, AU - Sukhu,B, AU - Bogdanovic,R P, AU - LaBella,F S, PY - 1991/1/1/pubmed PY - 1991/1/1/medline PY - 1991/1/1/entrez SP - 325 EP - 42 JF - Agents and actions. Supplements JO - Agents Actions Suppl VL - 33 N2 - Previously, we identified in rat liver microsomes, low (microM) affinity histamine receptors (HIC), associated with antiestrogen binding sites (AEBS). N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE), a potent AEBS ligand, is a specific HIC antagonist. Through binding HIC, newly-formed intracellular histamine mediates, and DPPE inhibits, human platelet aggregation. We now provide evidence that histamine, mobilized from cytoplasmic stores, is a mediator of the mitogenic response to concanavalin A in mouse spleen cells. DNA synthesis and intracellular histamine levels are decreased over time by the histidine decarboxylase inhibitor, alpha-fluoromethylhistidine. For DPPE, H1 and H2 antagonists, rank order of potency to inhibit [3H]-histamine binding to HIC in rat liver microsomes correlates with antiproliferative potency. DPPE also competes for [3H]-histamine binding at low and high affinity sites in rat liver nuclei (IC50 approximately 2 microM). Thus, histamine may mediate growth through two intracellular subtypes of HIC. SN - 0379-0363 UR - https://www.unboundmedicine.com/medline/citation/2053513/The_antiproliferative_potency_of_histamine_antagonists_correlates_with_inhibition_of_binding_of_[3H]_histamine_to_novel_intracellular_receptors__HIC__in_microsomal_and_nuclear_fractions_of_rat_liver_ DB - PRIME DP - Unbound Medicine ER -