Neuroleptic drug interactions with norepinephrine alpha receptor binding sites in rat brain

Peroutka, Stephen J.; U’Prichard, David C.; Greenberg, David A.; Snyder, Solomon H.

doi:10.1016/0028-3908(77)90023-5

Cited by 292 publications

(76 citation statements)

References 8 publications

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“…In addition, chlorpromazine strongly decreased the amount of ambulation at a dose of 10 mg/kg. (25,26). These adverse effects have severely limited the use of this medication.…”

Section: Effect On Thiopental-induced Sleep In Micementioning

confidence: 99%

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Omata

Yoshida

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-The antihistaminic effect of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy]benzoic acid maleate (ZCR-2060), a newly synthesized antiallergic agent, was investigated in both in vitro and in vivo studies. ZCR-2060 clearly antagonized histamine-induced contraction of isolated guinea pig ileum and trachea. In contrast, carbachol-, BaC12 and 5-hydroxytryptamine-induced contractions of isolated guinea pig ileum were slightly inhibited by higher concentrations of ZCR-2060. 3H-Mepyramine specific binding to membranes from guinea pig lung and brain were markedly inhibited by ZCR-2060 in a concentration-de pendent fashion. In the in vitro studies, the antihistaminic effect of ZCR-2060 was greater than those of cetirizine and terfenadine, but was less than that of ketotifen. In the in vivo studies, ZCR-2060 significantly inhibited the histamine-induced cutaneous reaction in rats, when administered orally 1 hr before the histamine injection. Moreover, ZCR-2060 has a long-lasting antihistaminic effect. In the in vivo studies, the antihistaminic effect of ZCR-2060 was found to be greater than that of cetirizine and terfenadine, and it was the same as that of ketotifen. Thiopental-induced sleep and spontaneous ambulatory activity in mice, however, were unaffected by ZCR-2060 at higher doses. These results indicate that ZCR-2060 has a potent, selective and long acting histamine H,-receptor antagonistic action without causing any unwanted CNS side effect.

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“…In addition, chlorpromazine strongly decreased the amount of ambulation at a dose of 10 mg/kg. (25,26). These adverse effects have severely limited the use of this medication.…”

Section: Effect On Thiopental-induced Sleep In Micementioning

confidence: 99%

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Omata

Yoshida

et al. 1994

Japanese Journal of Pharmacology

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“…The following radioactive ligands were used: [3H]morphine (79.2 Ci/mol, NEN) for the /z-opiate receptor [4] [2,3,10]. The assays were carried out as follows: Membranes (P2m) from rat striatum (300 pg protein in 100/Ll Tris buffer) were incubated with 300/zl supernatant from hybridoma cultures for 1 h at 25°C.…”

Section: Screening Assaymentioning

confidence: 99%

“…Binding assays were performed according to [2,3,9,10]. Protein concentration was determined colorimetrically [11].…”

Section: Receptor Assaymentioning

confidence: 99%

“…In v'~o binding studies and in vivo phar-/ macokinetics with various neurotransmitter agonists or antagonists [1][2][3] have indicated that, in general, neurotransmitters and their analogues are not strictly specific to a certain receptor. For example, serotonin acts on the Srserotonin receptors in nanomolar, but on the S2-serotonin receptors in micromolar concentrations, while spiperone shows nanomolar affinities for both the S2-serotonin and DJD4-dopamine receptors [2,3].…”

Section: Introductionmentioning

confidence: 99%

“…For example, serotonin acts on the Srserotonin receptors in nanomolar, but on the S2-serotonin receptors in micromolar concentrations, while spiperone shows nanomolar affinities for both the S2-serotonin and DJD4-dopamine receptors [2,3]. Similarly, opioids like etorphine and ketacocine recognize ~-,/z-and x-opiate receptors with comparable affinities [4].…”

Section: Introductionmentioning

confidence: 99%

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Monoclonal antibodies against the S₂‐serotonin receptor from rat brain that cross‐react with dopamine and opiate receptors

Deckmann

Shinitzky

1989

FEBS Letters

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Balb/c mice were immunized with rat striatal integral membrane proteins. After hybridization of splenocytes with myeloma cells, hybridoma lines secreting antibodies against serotonin, dopamine and opiate receptors were detected by inhibition of ligand binding to brain membrane preparations. Antibodies from two positive lines, Mab/a9 and Mab/a 18, were able to inhibit ligand binding to the S:serotonin (Kd range: 10-100 nM), the g-opiate (Ka range: 0.4-3 gM) and the ~-opiate receptors (Kd range: 0.7-I. 1 gM), while Mab/a9 was also found to inhibit ligand binding to the DJD4-dopamine receptor (Kd ~ 50 nM). An apparent molecular mass of 60 kDa could be ascribed to the c~-opiate receptor and apparent molecular masses of 29 and 36 kDa to the g-opiate receptor by ligand elution from immune-precipitates.

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Impaired Presynaptic Regulation of Norepinephrine in Schizophrenia

Sternberg¹

1982

Arch Gen Psychiatry

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Neuroleptic drug interactions with norepinephrine alpha receptor binding sites in rat brain

Cited by 292 publications

References 8 publications

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Monoclonal antibodies against the S₂‐serotonin receptor from rat brain that cross‐react with dopamine and opiate receptors

Impaired Presynaptic Regulation of Norepinephrine in Schizophrenia

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Neuroleptic drug interactions with norepinephrine alpha receptor binding sites in rat brain

Cited by 292 publications

References 8 publications

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Antiallergic Effect of ZCR-2060: Antihistaminic Action

Monoclonal antibodies against the S2‐serotonin receptor from rat brain that cross‐react with dopamine and opiate receptors

Impaired Presynaptic Regulation of Norepinephrine in Schizophrenia

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Product

Resources

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Monoclonal antibodies against the S₂‐serotonin receptor from rat brain that cross‐react with dopamine and opiate receptors