Highly potent and selective ligands for histamine H3-receptors

Arrang, Jean‐Michel; Garbarg, M.; Lancelot, J.-C.; Lecomte, Jeanne‐Marie; Pollard, H.; Robba, M.; Schunack, Walter; Schwartz, Jean‐Charles

doi:10.1038/327117a0

Cited by 880 publications

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“…human when compared to rat brain slices, K i values being 16 nM (Arrang et al, 1988) and 4 nM (Arrang et al, 1987), respectively. Other functional or binding studies performed with various ligands led to even higher K i values for this compound at the hH 3 R, i.e., 85 ± 200 nM (Cheri® et al, 1992;West et al, 1999).…”

Section: Special Reportmentioning

confidence: 92%

“…In the same way the antagonist ciproxifan displayed signi®cantly higher potency at the rH 3 R when compared to the hH 3 R in fresh brain tissues using either functional or binding assays performed under parallel conditions (Ligneau et al, 1998 and X. Ligneau, unpublished observations). Interestingly, however, both histamine and (R)a-methylhistamine were found to be nearly equipotent at the native rH 3 R and hH 3 R in brain (Arrang et al, 1987(Arrang et al, , 1988West et al, 1999). …”

Section: Special Reportmentioning

confidence: 92%

“…Therefore, these two residues appear to be responsible for the distinct pharmacology of the H 3 R in the two species. British Journal of Pharmacology (2000) Introduction Whereas the histamine H 3 receptor (H 3 R) was initially identi®ed in the rat brain (Arrang et al, 1983;1987), its presence in the human brain was con®rmed a few years later (Arrang et al, 1988). In both cases a functional test, the inhibition of [ 3 H]-histamine release from depolarized brain slices, was used, but the pharmacological characterization of the human H 3 R has remained preliminary since the availability of fresh brain tissues obtained during neurosurgery is limited.…”

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confidence: 99%

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Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain

Ligneau

Morisset-Lopez

Tardivel-Lacombe

et al. 2000

British J Pharmacology

144

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Starting from the sequence of the human histamine H 3 receptor (hH 3 R) cDNA, we have cloned the corresponding rat cDNA. Whereas the two deduced proteins show 93.5% overall homology and di er only by ®ve amino acid residues at the level of the transmembrane domains (TMs), some ligands displayed distinct a nities. Thioperamide and ciproxifan were about 10 fold more potent at the rat than at the human receptor, whereas FUB 349 displayed a reverse preference. Histamine, (R)a-methylhistamine, proxyfan or clobenpropit were nearly equipotent at H 3 receptors of both species. The inverse discrimination patterns of ciproxifan and FUB 349 were partially changed by mutation of one amino acid (V122A), and fully abolished by mutation of two amino acids (A119T and V122A), in TM3 of the rH 3 R located in the vicinity of Asp 114 purported to salt-link the ammonium group of histamine. Therefore, these two residues appear to be responsible for the distinct pharmacology of the H 3 R in the two species. British Journal of Pharmacology (2000) Introduction Whereas the histamine H 3 receptor (H 3 R) was initially identi®ed in the rat brain (Arrang et al., 1983;1987), its presence in the human brain was con®rmed a few years later (Arrang et al., 1988). In both cases a functional test, the inhibition of [ 3 H]-histamine release from depolarized brain slices, was used, but the pharmacological characterization of the human H 3 R has remained preliminary since the availability of fresh brain tissues obtained during neurosurgery is limited. Nevertheless there were some indications that the pharmacology of the human and the rat H 3 R may slightly di er (Arrang et al., 1988; West et al., 1999 and X. Ligneau, unpublished observation).With the recent cloning of the human H 3 R (hH 3 R) (Lovenberg et al., 1999), it became feasible to determine with greater precision the apparent a nity of ligands at this receptor and assess the existence of species di erences. Namely, for this purpose we have cloned the rat H 3 R (rH 3 R) starting from the published sequence of the hH 3 R and established permanent cell lines expressing the hH 3 R or rH 3 R. This allowed us to identify ligands displaying distinct apparent a nities at the H 3 R of the two species. Then we tried to identify the amino acid residues responsible for such discrimination using site-directed mutagenesis of the rH 3 R.

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Section: Special Reportmentioning

confidence: 92%

Section: Special Reportmentioning

confidence: 92%

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confidence: 99%

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Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain

Ligneau

Morisset-Lopez

Tardivel-Lacombe

et al. 2000

British J Pharmacology

144

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“…In a previous study, we reported that the selective histamine H3 antagonist thioperamide (Arrang et al, 1987) can potentiate the subjective effects of methamphetamine in rats trained to discriminate a 1.0 mg/kg intraperitoneal (i.p.) dose of methamphetamine from an i.p.…”

Section: Introductionmentioning

confidence: 99%

Histamine H3 Receptor Antagonists Potentiate Methamphetamine Self-Administration and Methamphetamine-Induced Accumbal Dopamine Release

Munzar

Justinová²,

Goldberg³

2004

Neuropsychopharmacol

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Methamphetamine administration increases brain levels of histamine and neuronal histamine attenuates several of methamphetamine's behavioral effects. The role of different subtypes of histamine receptors in this negative feedback, however, remains unclear. There is some evidence on possible involvement of histamine H3 receptors in these actions of methamphetamine. The aim of the present study was to evaluate the effects of two histamine H3 receptor antagonists, clobenpropit and thioperamide, on rewarding and neurochemical effects of methamphetamine utilizing three in vivo methodologies, drug self-administration, drug discrimination, and microdialysis in Sprague-Dawley rats. In rats self-administering methamphetamine intravenously under a fixed-ratio schedule, presession treatment with thioperamide (1.0-3.0 mg/kg, subcutaneous, s.c.) or clobenpropit (1.0-3.0 mg/kg, s.c.) potentiated the reinforcing effects of methamphetamine, as indicated by a dose-dependent increase in responding for a low 0.03 mg/kg dose of methamphetamine, that by itself failed to maintain responding above saline substitution levels, and a decrease in responding for a higher 0.06 mg/kg training dose of methamphetamine. In contrast, neither thioperamide nor clobenpropit treatment increased responding during saline substitution. In other rats trained to discriminate intraperitoneal (i.p.) injection of 1.0 mg/kg methamphetamine from i.p. injection of saline, both thioperamide and clobenpropit (0.3-3.0 mg/kg, s.c.) dose dependently increased methamphetamine-appropriate responding when administered with a low 0.3 mg/kg i.p. dose of methamphetamine, which by itself produced predominantly saline-appropriate responding. However, thioperamide and clobenpropit produced only saline-appropriate responding when administered with saline vehicle. Finally, thioperamide and clobenpropit potentiated methamphetamine-induced elevations in extracellular dopamine levels in the shell of the nucleus accumbens, but did not increase brain dopamine levels when given alone. These findings point to histamine H3 receptors as a new and important receptor system modulating the reinforcing, subjective, and neurochemical actions of methamphetamine.

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“…Histamine receptors are classified into H1-, H2-and H3-receptors according to the potency order of histaminergic agonists and antagonists (Ash and Schild 1966;Black et al 1972;Durant et al 1978;Arrang et al 1983Arrang et al , 1987Schwartz et al 1986;Buschauer et al 1989). Occupancy of HI-and H2-receptors by agonists leads to the activation of phospholipase C and adenylyl cyclase, respectively (Schwartz et al 1986;Buschauer et al 1989).…”

Section: Introductionmentioning

confidence: 99%

Histamine inhibits activation of human neutrophils and HL-60 leukemic cells via H2-receptors

Burde

Seifert

Buschauer

et al. 1989

Naunyn-Schmiedeberg's Arch. Pharmacol.

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Summary. The effects of prostaglandin E 1 (PGE 1) and histamine on activation of superoxide (O ~-) formation, exocytosis of fi-glucuronidase and aggregation in human neutrophils and HL-60 leukemic cells were studied. PGEb histamine and impromidine, a potent Hz-agonist, inhibited O2 formation in neutrophils induced by the chemotactic peptide, N-formyl-L-methionyl-L-leucyl-L-phenylalanine (tMet-Leu-Phe) with ICso values of 0.5 gM, 8 ~tM and 2 gM, respectively. The full Hl-agonist and weak partial Hzagonist, betahistine, was much less potent and effective than histamine. Dibutyryl cyclic AMP and forskolin mimicked the effects of histamine and PGE1 on O~ formation. The Hz-antagonist, famotidine, competitively reversed histamine-induced inhibition of O2 formation with a pA2 value of 7.5. Histamine inhibited O2 formation when added prior to or after fMet-Leu-Phe, fMet-Leu-Phe-induced aggregation and release of fl-glucuronidase in neutrophils were less sensitive to inhibition by PGE1, histamine, dibutyryl cyclic AMP and forskolin than O~-formation. The inhibitor of cyclic AMP-specific phosphodiesterase, rac-4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone (Ro 20-1724), additively enhanced the inhibitory effects of histamine and PGE1 on the above cell functions. In HL-60 cells differentiated by dimethyl sulfoxide or dibutyryl cyclic AMP, histamine, impromidine and PGE1 but not betahistine inhibited fMet-Leu-Phe-induced O~ formation as well. Our data suggest that histamine inhibits activation of neutrophils and HL-60 cells via Hz-receptors through activation of adenylyl cyclase and increased formation of cyclic AMP. As stimulated basophils and mast cells release high quantities of histamine, this intercellular signal molecule may play an inhibitory role in the activation of cytotoxic functions of myeloid cells.

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Highly potent and selective ligands for histamine H3-receptors

Cited by 880 publications

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Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain

Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain

Histamine H3 Receptor Antagonists Potentiate Methamphetamine Self-Administration and Methamphetamine-Induced Accumbal Dopamine Release

Histamine inhibits activation of human neutrophils and HL-60 leukemic cells via H2-receptors

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Highly potent and selective ligands for histamine H3-receptors

Cited by 880 publications

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Distinct pharmacology of rat and human histamine H3 receptors: role of two amino acids in the third transmembrane domain

Distinct pharmacology of rat and human histamine H3 receptors: role of two amino acids in the third transmembrane domain

Histamine H3 Receptor Antagonists Potentiate Methamphetamine Self-Administration and Methamphetamine-Induced Accumbal Dopamine Release

Histamine inhibits activation of human neutrophils and HL-60 leukemic cells via H2-receptors

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Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain

Distinct pharmacology of rat and human histamine H₃ receptors: role of two amino acids in the third transmembrane domain