The Experts below are selected from a list of 327 Experts worldwide ranked by ideXlab platform

Stevin H. Zorn - One of the best experts on this subject based on the ideXlab platform.

  • ziprasidone a novel Antipsychotic Agent with a unique human receptor binding profile
    European Journal of Pharmacology, 2001
    Co-Authors: Anne W. Schmidt, Harry R. Howard, Lorraine A Lebel, Stevin H. Zorn
    Abstract:

    Abstract Ziprasidone is a novel Antipsychotic Agent with a unique combination of pharmacological activities at human receptors. Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D 2 receptors. Ziprasidone is a 5-HT 1A receptor agonist and an antagonist at 5-HT 2A , 5-HT 2C and 5-HT 1B/1D receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. This unique pharmacological profile of ziprasidone may be related to its clinical effectiveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cognitive deficits and weight gain.

  • 3-Benzisothiazolylpiperazine derivatives as potential atypical Antipsychotic Agents
    Journal of Medicinal Chemistry, 1996
    Co-Authors: Harry R. Howard, John A. Lowe, Thomas Francis Seeger, Patricia A. Seymour, Stevin H. Zorn, Patrick Maloney, Frank E. Ewing, M. E. Newman, Anne W. Schmidt, Jerome S. Furman
    Abstract:

    A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical Antipsychotic Agent. The in vitro profile of 8e from this series is a combination of D2 receptor affinity comparable to the typical Antipsychotic Agent haloperidol and a 5-HT2A/D2 ratio comparable to the atypical Agent clozapine. In vivo 8e possesses activity consistent with an efficacious Antipsychotic Agent with less tendency to induce extrapyramidal side effects in man.

Anne W. Schmidt - One of the best experts on this subject based on the ideXlab platform.

  • ziprasidone a novel Antipsychotic Agent with a unique human receptor binding profile
    European Journal of Pharmacology, 2001
    Co-Authors: Anne W. Schmidt, Harry R. Howard, Lorraine A Lebel, Stevin H. Zorn
    Abstract:

    Abstract Ziprasidone is a novel Antipsychotic Agent with a unique combination of pharmacological activities at human receptors. Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D 2 receptors. Ziprasidone is a 5-HT 1A receptor agonist and an antagonist at 5-HT 2A , 5-HT 2C and 5-HT 1B/1D receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. This unique pharmacological profile of ziprasidone may be related to its clinical effectiveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cognitive deficits and weight gain.

  • 3-Benzisothiazolylpiperazine derivatives as potential atypical Antipsychotic Agents
    Journal of Medicinal Chemistry, 1996
    Co-Authors: Harry R. Howard, John A. Lowe, Thomas Francis Seeger, Patricia A. Seymour, Stevin H. Zorn, Patrick Maloney, Frank E. Ewing, M. E. Newman, Anne W. Schmidt, Jerome S. Furman
    Abstract:

    A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical Antipsychotic Agent. The in vitro profile of 8e from this series is a combination of D2 receptor affinity comparable to the typical Antipsychotic Agent haloperidol and a 5-HT2A/D2 ratio comparable to the atypical Agent clozapine. In vivo 8e possesses activity consistent with an efficacious Antipsychotic Agent with less tendency to induce extrapyramidal side effects in man.

  • 1-Naphthylpiperazine derivatives as potential atypical Antipsychotic Agents.
    Journal of Medicinal Chemistry, 1991
    Co-Authors: John A. Lowe, Harry R. Howard, Thomas Francis Seeger, Patricia A. Seymour, Frank E. Ewing, M. E. Newman, Arthur Adam Nagel, J. Heym, Anne W. Schmidt
    Abstract:

    The design and synthesis of a series of potential atypical Antipsychotic Agents based on the structure of 1-naphthylpiperazine are described. The incorporation of dopamine antagonist activity into the parent structure was achieved with heterocyclic surrogates for the catechol moiety of dopamine. Compound 4b from this series showed a biochemical profile that translated to behavioral activity in the rat predictive of an Antipsychotic Agent with a low propensity to cause extrapyramidal side effects in man.

Lars Slørdal - One of the best experts on this subject based on the ideXlab platform.

Javier Gonzalezmaeso - One of the best experts on this subject based on the ideXlab platform.

  • revised pharmacophore model for 5 ht2a receptor antagonists derived from the atypical Antipsychotic Agent risperidone
    ACS Chemical Neuroscience, 2019
    Co-Authors: Urjita H Shah, Richard A. Glennon, Supriya A. Gaitonde, José L. Moreno, Małgorzata Dukat, Javier Gonzalezmaeso
    Abstract:

    Pharmacophore models for 5-HT2A receptor antagonists consist of two aromatic/hydrophobic regions at a given distance from a basic amine. We have previously shown that both aromatic/hydrophobic moieties are unnecessary for binding or antagonist action. Here, we deconstructed the 5-HT2A receptor antagonist/serotonin-dopamine Antipsychotic Agent risperidone into smaller structural segments that were tested for 5-HT2A receptor affinity and function. We show, again, that the entire risperidone structure is unnecessary for retention of affinity or antagonist action. Replacement of the 6-fluoro-3-(4-piperidinyl)-1,2-benz[ d]isoxazole moiety by isosteric tryptamines resulted in retention of affinity and antagonist action. Additionally, 3-(4-piperidinyl)-1,2-benz[ d]isoxazole (10), which represents less than half the structural features of risperidone, retains both affinity and antagonist actions. 5-HT2A receptor homology modeling/docking studies suggest that 10 binds in a manner similar to risperidone and that there is a large cavity to accept various N4-substituted analogues of 10 such as risperidone and related Agents. Alterations of this "extended" moiety improve receptor binding and functional potency. We propose a new risperidone-based pharmacophore for 5-HT2A receptor antagonist action.

Harry R. Howard - One of the best experts on this subject based on the ideXlab platform.

  • ziprasidone a novel Antipsychotic Agent with a unique human receptor binding profile
    European Journal of Pharmacology, 2001
    Co-Authors: Anne W. Schmidt, Harry R. Howard, Lorraine A Lebel, Stevin H. Zorn
    Abstract:

    Abstract Ziprasidone is a novel Antipsychotic Agent with a unique combination of pharmacological activities at human receptors. Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D 2 receptors. Ziprasidone is a 5-HT 1A receptor agonist and an antagonist at 5-HT 2A , 5-HT 2C and 5-HT 1B/1D receptors. Additionally, ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. This unique pharmacological profile of ziprasidone may be related to its clinical effectiveness as a treatment for the positive, negative and affective symptoms of schizophrenia with a low propensity for extrapyramidal side effects, cognitive deficits and weight gain.

  • 3-Benzisothiazolylpiperazine derivatives as potential atypical Antipsychotic Agents
    Journal of Medicinal Chemistry, 1996
    Co-Authors: Harry R. Howard, John A. Lowe, Thomas Francis Seeger, Patricia A. Seymour, Stevin H. Zorn, Patrick Maloney, Frank E. Ewing, M. E. Newman, Anne W. Schmidt, Jerome S. Furman
    Abstract:

    A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical Antipsychotic Agent. The in vitro profile of 8e from this series is a combination of D2 receptor affinity comparable to the typical Antipsychotic Agent haloperidol and a 5-HT2A/D2 ratio comparable to the atypical Agent clozapine. In vivo 8e possesses activity consistent with an efficacious Antipsychotic Agent with less tendency to induce extrapyramidal side effects in man.

  • 1-Naphthylpiperazine derivatives as potential atypical Antipsychotic Agents.
    Journal of Medicinal Chemistry, 1991
    Co-Authors: John A. Lowe, Harry R. Howard, Thomas Francis Seeger, Patricia A. Seymour, Frank E. Ewing, M. E. Newman, Arthur Adam Nagel, J. Heym, Anne W. Schmidt
    Abstract:

    The design and synthesis of a series of potential atypical Antipsychotic Agents based on the structure of 1-naphthylpiperazine are described. The incorporation of dopamine antagonist activity into the parent structure was achieved with heterocyclic surrogates for the catechol moiety of dopamine. Compound 4b from this series showed a biochemical profile that translated to behavioral activity in the rat predictive of an Antipsychotic Agent with a low propensity to cause extrapyramidal side effects in man.