High affinity histamine binding site is the H 3 receptor: Characterization and autoradiographic localization in rat brain

High affinity histamine binding site is the H 3 receptor: Characterization and autoradiographic... The binding of the histamine autoreceptor (H3) agonist (3H)‐Nα‐methyl‐histamine ((3H)‐N‐MeHA) was examined in 25 μm thick rat forebrain sections. The specific binding was saturable and of high affinity: Scatchard analysis indicated a Kd of 2 nM and a Bmax of 25 ± 3 fmol/section. Under similar conditions, (3H)‐histamine ((3H)‐HA) bound with a Kd of 8 nM and a Bmax of 20 ± 2 fmol/section. Competition studies indicated that both ligands bound an identical site which had the pharmacological characteristics of the H3 binding site. The high affinity binding of (3H)‐N‐MeHA was sensitive to the presence of 5′ ‐guanylyl‐imidodiphosphate, indicating that the binding site is likely coupled to a G‐protein. Autoradiographic studies indicated the (3H)‐N‐MeHA binding to be greatest in the nucleus accumbens, striatum, substantia nigra pars reticulata, and certain cortical areas. Striatal quinolinic acid lesions greatly reduced binding in both the striatum and ipsilateral substantia nigra, while 6‐hydroxydopamine lesions of the nigrostriatal dopamine system were without effect on binding. Therefore, most of the H3 binding sites in the basal ganglia are on striatonigral projection neurons. Cortical quinolinic acid lesions greatly reduced H3 binding in cortex, indicating that the binding in cortex, as in striatum, is largely on intrinsic neurons, rather than on afferents such as histamine nerve terminals. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Synapse Wiley

High affinity histamine binding site is the H 3 receptor: Characterization and autoradiographic localization in rat brain

Synapse, Volume 8 (2) – Jun 1, 1991

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Publisher
Wiley
Copyright
Copyright © 1991 Wiley‐Liss, Inc.
ISSN
0887-4476
eISSN
1098-2396
D.O.I.
10.1002/syn.890080208
Publisher site
See Article on Publisher Site

Abstract

The binding of the histamine autoreceptor (H3) agonist (3H)‐Nα‐methyl‐histamine ((3H)‐N‐MeHA) was examined in 25 μm thick rat forebrain sections. The specific binding was saturable and of high affinity: Scatchard analysis indicated a Kd of 2 nM and a Bmax of 25 ± 3 fmol/section. Under similar conditions, (3H)‐histamine ((3H)‐HA) bound with a Kd of 8 nM and a Bmax of 20 ± 2 fmol/section. Competition studies indicated that both ligands bound an identical site which had the pharmacological characteristics of the H3 binding site. The high affinity binding of (3H)‐N‐MeHA was sensitive to the presence of 5′ ‐guanylyl‐imidodiphosphate, indicating that the binding site is likely coupled to a G‐protein. Autoradiographic studies indicated the (3H)‐N‐MeHA binding to be greatest in the nucleus accumbens, striatum, substantia nigra pars reticulata, and certain cortical areas. Striatal quinolinic acid lesions greatly reduced binding in both the striatum and ipsilateral substantia nigra, while 6‐hydroxydopamine lesions of the nigrostriatal dopamine system were without effect on binding. Therefore, most of the H3 binding sites in the basal ganglia are on striatonigral projection neurons. Cortical quinolinic acid lesions greatly reduced H3 binding in cortex, indicating that the binding in cortex, as in striatum, is largely on intrinsic neurons, rather than on afferents such as histamine nerve terminals.

Journal

SynapseWiley

Published: Jun 1, 1991

References

  • Biphasic effects of intra‐accumbens histamine administration on spontaneous motor activity in the rat: a role for central histamine receptors
    Bristow, Bristow; Bennet, Bennet
  • Receptor activation and inositol lipid hydrolysis in neural tissue
    Fisher, Fisher; Agranoff, Agranoff
  • Histamine H 3 ‐receptor inhibit cholinergic neurotransmission in guinea‐pig airways
    Ichinose, Ichinose; Stretton, Stretton; Schwartz, Schwartz; Barnes, Barnes

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