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Bryan L. Roth - One of the best experts on this subject based on the ideXlab platform.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a common and potentially serious complication of some antipsychotic drug therapy, and may be accompanied by hyperlipidemia, hypertension and hyperglycemia and, in some extreme cases, diabetic ketoacidosis. The molecular mechanism(s) responsible for antipsychotic drug-induced weight gain are unknown, but have been hypothesized to be because of interactions of antipsychotic drugs with several neurotransmitter Receptors, including 5-HT(2A) and 5-HT(2C) serotonin Receptors, H(1)-Histamine Receptors, alpha(1)- and alpha(2)-adrenergic Receptors, and m3-muscarinic Receptors. To determine the Receptor(s) likely to be responsible for antipsychotic-drug-induced weight gain, we screened 17 typical and atypical antipsychotic drugs for binding to 12 neurotransmitter Receptors. H(1)-Histamine Receptor affinities for this group of typical and atypical antipsychotic drugs were significantly correlated with weight gain (Spearman rho=-0.72; p<0.01), as were affinities for alpha(1A) adrenergic (rho=-0.54; p<0.05), 5-HT(2C) (rho=-0.49; p<0.05) and 5-HT(6) Receptors (rho=-0.54; p<0.05), whereas eight other Receptors' affinities were not. A principal components analysis showed that affinities at the H(1), alpha(2A), alpha(2B), 5-HT(2A), 5-HT(2C), and 5-HT(6) Receptors were most highly correlated with the first principal component, and affinities for the D(2), 5-HT(1A), and 5-HT(7) Receptors were most highly correlated with the second principal component. A discriminant functions analysis showed that affinities for the H(1) and alpha(1A) Receptors were most highly correlated with the discriminant function axis. The discriminant function analysis, as well as the affinity for the H(1)-Histamine Receptor alone, correctly classified 15 of the 17 drugs into two groups; those that induce weight gain and those that do not. Because centrally acting H(1)-Histamine Receptor antagonists are known to induce weight gain with chronic use, and because H(1)-Histamine Receptor affinities are positively correlated with weight gain among typical and atypical antipsychotic drugs, it is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H(1)-Histamine Receptors.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

  • discovery of a novel member of the Histamine Receptor family
    Molecular Pharmacology, 2001
    Co-Authors: Tuan V Nguyen, David A Shapiro, Susan R George, Vincent Setola, Dennis Lee, Regina Cheng, Laura Rauser, Samuel P Lee, Kevin R Lynch, Bryan L. Roth
    Abstract:

    We report the discovery, tissue distribution and pharmacological characterization of a novel Receptor, which we have named H4. Like the three Histamine Receptors reported previously (H1, H2, and H3), the H4 Receptor is a G protein-coupled Receptor and is most closely related to the H3 Receptor, sharing 58% identity in the transmembrane regions. The gene encoding the H4 Receptor was discovered initially in a search of the GenBank databases as sequence fragments retrieved in a partially sequenced human genomic contig mapped to chromosome 18. These sequences were used to retrieve a partial cDNA clone and, in combination with genomic fragments, were used to determine the full-length open reading frame of 390 amino acids. Northern analysis revealed a 3.0-kb transcript in rat testis and intestine. Radioligand binding studies indicated that the H4 Receptor has a unique pharmacology and binds [ 3 H]Histamine ( K d = 44 nM) and [ 3 H]pyrilamine ( K d = 32 nM) and several psychoactive compounds (amitriptyline, chlorpromazine, cyproheptadine, mianserin) with moderate affinity ( K i range of 33–750 nM). Additionally, Histamine induced a rapid internalization of HA-tagged H4 Receptors in transfected human embryonic kidney 293 cells.

Wesley K Kroeze - One of the best experts on this subject based on the ideXlab platform.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a common and potentially serious complication of some antipsychotic drug therapy, and may be accompanied by hyperlipidemia, hypertension and hyperglycemia and, in some extreme cases, diabetic ketoacidosis. The molecular mechanism(s) responsible for antipsychotic drug-induced weight gain are unknown, but have been hypothesized to be because of interactions of antipsychotic drugs with several neurotransmitter Receptors, including 5-HT(2A) and 5-HT(2C) serotonin Receptors, H(1)-Histamine Receptors, alpha(1)- and alpha(2)-adrenergic Receptors, and m3-muscarinic Receptors. To determine the Receptor(s) likely to be responsible for antipsychotic-drug-induced weight gain, we screened 17 typical and atypical antipsychotic drugs for binding to 12 neurotransmitter Receptors. H(1)-Histamine Receptor affinities for this group of typical and atypical antipsychotic drugs were significantly correlated with weight gain (Spearman rho=-0.72; p<0.01), as were affinities for alpha(1A) adrenergic (rho=-0.54; p<0.05), 5-HT(2C) (rho=-0.49; p<0.05) and 5-HT(6) Receptors (rho=-0.54; p<0.05), whereas eight other Receptors' affinities were not. A principal components analysis showed that affinities at the H(1), alpha(2A), alpha(2B), 5-HT(2A), 5-HT(2C), and 5-HT(6) Receptors were most highly correlated with the first principal component, and affinities for the D(2), 5-HT(1A), and 5-HT(7) Receptors were most highly correlated with the second principal component. A discriminant functions analysis showed that affinities for the H(1) and alpha(1A) Receptors were most highly correlated with the discriminant function axis. The discriminant function analysis, as well as the affinity for the H(1)-Histamine Receptor alone, correctly classified 15 of the 17 drugs into two groups; those that induce weight gain and those that do not. Because centrally acting H(1)-Histamine Receptor antagonists are known to induce weight gain with chronic use, and because H(1)-Histamine Receptor affinities are positively correlated with weight gain among typical and atypical antipsychotic drugs, it is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H(1)-Histamine Receptors.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

Paul Ernsberger - One of the best experts on this subject based on the ideXlab platform.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a common and potentially serious complication of some antipsychotic drug therapy, and may be accompanied by hyperlipidemia, hypertension and hyperglycemia and, in some extreme cases, diabetic ketoacidosis. The molecular mechanism(s) responsible for antipsychotic drug-induced weight gain are unknown, but have been hypothesized to be because of interactions of antipsychotic drugs with several neurotransmitter Receptors, including 5-HT(2A) and 5-HT(2C) serotonin Receptors, H(1)-Histamine Receptors, alpha(1)- and alpha(2)-adrenergic Receptors, and m3-muscarinic Receptors. To determine the Receptor(s) likely to be responsible for antipsychotic-drug-induced weight gain, we screened 17 typical and atypical antipsychotic drugs for binding to 12 neurotransmitter Receptors. H(1)-Histamine Receptor affinities for this group of typical and atypical antipsychotic drugs were significantly correlated with weight gain (Spearman rho=-0.72; p<0.01), as were affinities for alpha(1A) adrenergic (rho=-0.54; p<0.05), 5-HT(2C) (rho=-0.49; p<0.05) and 5-HT(6) Receptors (rho=-0.54; p<0.05), whereas eight other Receptors' affinities were not. A principal components analysis showed that affinities at the H(1), alpha(2A), alpha(2B), 5-HT(2A), 5-HT(2C), and 5-HT(6) Receptors were most highly correlated with the first principal component, and affinities for the D(2), 5-HT(1A), and 5-HT(7) Receptors were most highly correlated with the second principal component. A discriminant functions analysis showed that affinities for the H(1) and alpha(1A) Receptors were most highly correlated with the discriminant function axis. The discriminant function analysis, as well as the affinity for the H(1)-Histamine Receptor alone, correctly classified 15 of the 17 drugs into two groups; those that induce weight gain and those that do not. Because centrally acting H(1)-Histamine Receptor antagonists are known to induce weight gain with chronic use, and because H(1)-Histamine Receptor affinities are positively correlated with weight gain among typical and atypical antipsychotic drugs, it is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H(1)-Histamine Receptors.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

Sandra J Hufeisen - One of the best experts on this subject based on the ideXlab platform.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a common and potentially serious complication of some antipsychotic drug therapy, and may be accompanied by hyperlipidemia, hypertension and hyperglycemia and, in some extreme cases, diabetic ketoacidosis. The molecular mechanism(s) responsible for antipsychotic drug-induced weight gain are unknown, but have been hypothesized to be because of interactions of antipsychotic drugs with several neurotransmitter Receptors, including 5-HT(2A) and 5-HT(2C) serotonin Receptors, H(1)-Histamine Receptors, alpha(1)- and alpha(2)-adrenergic Receptors, and m3-muscarinic Receptors. To determine the Receptor(s) likely to be responsible for antipsychotic-drug-induced weight gain, we screened 17 typical and atypical antipsychotic drugs for binding to 12 neurotransmitter Receptors. H(1)-Histamine Receptor affinities for this group of typical and atypical antipsychotic drugs were significantly correlated with weight gain (Spearman rho=-0.72; p<0.01), as were affinities for alpha(1A) adrenergic (rho=-0.54; p<0.05), 5-HT(2C) (rho=-0.49; p<0.05) and 5-HT(6) Receptors (rho=-0.54; p<0.05), whereas eight other Receptors' affinities were not. A principal components analysis showed that affinities at the H(1), alpha(2A), alpha(2B), 5-HT(2A), 5-HT(2C), and 5-HT(6) Receptors were most highly correlated with the first principal component, and affinities for the D(2), 5-HT(1A), and 5-HT(7) Receptors were most highly correlated with the second principal component. A discriminant functions analysis showed that affinities for the H(1) and alpha(1A) Receptors were most highly correlated with the discriminant function axis. The discriminant function analysis, as well as the affinity for the H(1)-Histamine Receptor alone, correctly classified 15 of the 17 drugs into two groups; those that induce weight gain and those that do not. Because centrally acting H(1)-Histamine Receptor antagonists are known to induce weight gain with chronic use, and because H(1)-Histamine Receptor affinities are positively correlated with weight gain among typical and atypical antipsychotic drugs, it is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H(1)-Histamine Receptors.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

Herbert Y Meltzer - One of the best experts on this subject based on the ideXlab platform.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a common and potentially serious complication of some antipsychotic drug therapy, and may be accompanied by hyperlipidemia, hypertension and hyperglycemia and, in some extreme cases, diabetic ketoacidosis. The molecular mechanism(s) responsible for antipsychotic drug-induced weight gain are unknown, but have been hypothesized to be because of interactions of antipsychotic drugs with several neurotransmitter Receptors, including 5-HT(2A) and 5-HT(2C) serotonin Receptors, H(1)-Histamine Receptors, alpha(1)- and alpha(2)-adrenergic Receptors, and m3-muscarinic Receptors. To determine the Receptor(s) likely to be responsible for antipsychotic-drug-induced weight gain, we screened 17 typical and atypical antipsychotic drugs for binding to 12 neurotransmitter Receptors. H(1)-Histamine Receptor affinities for this group of typical and atypical antipsychotic drugs were significantly correlated with weight gain (Spearman rho=-0.72; p<0.01), as were affinities for alpha(1A) adrenergic (rho=-0.54; p<0.05), 5-HT(2C) (rho=-0.49; p<0.05) and 5-HT(6) Receptors (rho=-0.54; p<0.05), whereas eight other Receptors' affinities were not. A principal components analysis showed that affinities at the H(1), alpha(2A), alpha(2B), 5-HT(2A), 5-HT(2C), and 5-HT(6) Receptors were most highly correlated with the first principal component, and affinities for the D(2), 5-HT(1A), and 5-HT(7) Receptors were most highly correlated with the second principal component. A discriminant functions analysis showed that affinities for the H(1) and alpha(1A) Receptors were most highly correlated with the discriminant function axis. The discriminant function analysis, as well as the affinity for the H(1)-Histamine Receptor alone, correctly classified 15 of the 17 drugs into two groups; those that induce weight gain and those that do not. Because centrally acting H(1)-Histamine Receptor antagonists are known to induce weight gain with chronic use, and because H(1)-Histamine Receptor affinities are positively correlated with weight gain among typical and atypical antipsychotic drugs, it is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H(1)-Histamine Receptors.

  • h1 Histamine Receptor affinity predicts short term weight gain for typical and atypical antipsychotic drugs
    Neuropsychopharmacology, 2003
    Co-Authors: Wesley K Kroeze, Sandra J Hufeisen, Beth Popadak, Sean Michael Renock, Seanna Steinberg, Paul Ernsberger, Karu Jayathilake, Herbert Y Meltzer, Bryan L. Roth
    Abstract:

    H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs