Serotonin Antagonist

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Steven K Salzman - One of the best experts on this subject based on the ideXlab platform.

  • the Serotonin Antagonist mianserin improves functional recovery following experimental spinal trauma
    Annals of Neurology, 1991
    Co-Authors: Steven K Salzman, Michael A Puniak, Zhongjun Liu, Richard P Maitlandheriot, Gina M Freeman, Cynthia A Agresta
    Abstract:

    The ability of the Serotonin Antagonist mianserin to improve neurological recovery after graded impact trauma to the thoracic region of the spinal cord was compared to that of cyproheptadine and ketanserin in pentobarbital-anesthetized rats. Spinal cord injury was produced at T-10 by the weight-drop method and confirmed by the disappearance of the somatosensory-evoked response during the subsequent 15 minutes. In all experiments, drug or vehicle treatments were randomly administered as a single intravenous bolus 15 minutes after injury. Functional outcome was blindly assessed for 2 weeks after injury using a modified Tarlov scale, and in some cases, the Rivlin-Tator angleboard test. The survival of descending raphe-spinal axons was determined by the measurement of Serotonin in postmortem spinal tissues located above and below the site of injury. In separate acute experiments, the physiological and hemodynamic correlates of a 50 gm cm injury and either mianserin or vehicle injection were examined, as were the effects on Serotonin content and metabolism in spinal tissues harvested 30 minutes after injury. All doses of mainserin were associated with some index of improved recovery following a 50 gm cm injury, with a 1-mg/kg dose being clearly superior. Both ketanserin (0.1 mg/kg) and cyproheptadine (2 mg/kg) displayed marginal therapeutic actions for 50 gm cm injuries. In acute studies, mianserin at 1 mg/kg was associated with the preservation of posttraumatic spinal cord blood flow at T-12 as well as a pronounced alteration in postmortem spinal Serotonin content and metabolism, in contrast to vehicle control treatments. These data lend further support to a serotonergic hypothesis of secondary spinal cord injury and suggest the potential use of mianserin for the acute treatment of spinal cord injury.

  • Comparison of a Serotonin Antagonist, opioid Antagonist, and TRH analog for the acute treatment of experimental spinal trauma.
    Journal of neurotrauma, 1991
    Co-Authors: Michael A Puniak, Gina M Freeman, Cynthia A Agresta, Laura Van Newkirk, Carol A. Barone, Steven K Salzman
    Abstract:

    ABSTRACT The therapeutic efficacies of a Serotonin Antagonist (mianserin), an opioid Antagonist (nalmefene), and a TRH analog (YM-14673) were compared in a well-characterized model of experimental ...

Cynthia A Agresta - One of the best experts on this subject based on the ideXlab platform.

  • the Serotonin Antagonist mianserin improves functional recovery following experimental spinal trauma
    Annals of Neurology, 1991
    Co-Authors: Steven K Salzman, Michael A Puniak, Zhongjun Liu, Richard P Maitlandheriot, Gina M Freeman, Cynthia A Agresta
    Abstract:

    The ability of the Serotonin Antagonist mianserin to improve neurological recovery after graded impact trauma to the thoracic region of the spinal cord was compared to that of cyproheptadine and ketanserin in pentobarbital-anesthetized rats. Spinal cord injury was produced at T-10 by the weight-drop method and confirmed by the disappearance of the somatosensory-evoked response during the subsequent 15 minutes. In all experiments, drug or vehicle treatments were randomly administered as a single intravenous bolus 15 minutes after injury. Functional outcome was blindly assessed for 2 weeks after injury using a modified Tarlov scale, and in some cases, the Rivlin-Tator angleboard test. The survival of descending raphe-spinal axons was determined by the measurement of Serotonin in postmortem spinal tissues located above and below the site of injury. In separate acute experiments, the physiological and hemodynamic correlates of a 50 gm cm injury and either mianserin or vehicle injection were examined, as were the effects on Serotonin content and metabolism in spinal tissues harvested 30 minutes after injury. All doses of mainserin were associated with some index of improved recovery following a 50 gm cm injury, with a 1-mg/kg dose being clearly superior. Both ketanserin (0.1 mg/kg) and cyproheptadine (2 mg/kg) displayed marginal therapeutic actions for 50 gm cm injuries. In acute studies, mianserin at 1 mg/kg was associated with the preservation of posttraumatic spinal cord blood flow at T-12 as well as a pronounced alteration in postmortem spinal Serotonin content and metabolism, in contrast to vehicle control treatments. These data lend further support to a serotonergic hypothesis of secondary spinal cord injury and suggest the potential use of mianserin for the acute treatment of spinal cord injury.

  • Comparison of a Serotonin Antagonist, opioid Antagonist, and TRH analog for the acute treatment of experimental spinal trauma.
    Journal of neurotrauma, 1991
    Co-Authors: Michael A Puniak, Gina M Freeman, Cynthia A Agresta, Laura Van Newkirk, Carol A. Barone, Steven K Salzman
    Abstract:

    ABSTRACT The therapeutic efficacies of a Serotonin Antagonist (mianserin), an opioid Antagonist (nalmefene), and a TRH analog (YM-14673) were compared in a well-characterized model of experimental ...

Abdel-galil E. Amr - One of the best experts on this subject based on the ideXlab platform.

  • antiarrhythmic Serotonin Antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2 amino 4 5 6 7 tetrahydro n phenylbenzo b thiophene 3 carboxamide
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Abdel-galil E. Amr, Mohamed H Sherif, M G Assy, Mohamed A Alomar, Islam Ragab
    Abstract:

    A series of novel thiophene derivatives 3-17 were synthesized by initial reactions of 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide 1 and 2-amino-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carbonitrile 7 with different organic reagents. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, MS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. All the compounds were screened for their antiarrhythmic, Serotonin Antagonist and antianexiety activities and they showed high activity compared with procaine amide, lidocaine, diazepam and buspirone as positive controls. The detailed synthesis, spectroscopic data, LD50 and pharmacological activities of the synthesized compounds were reported.

  • Synthesis and Serotonin Antagonist and antianexity activities of pyrrolidine derivatives from 4-hydrazinyl-1-p-substituted phenyl-2,5-dihydro-1H-pyrrole-3-carbonitriles
    Monatshefte für Chemie - Chemical Monthly, 2008
    Co-Authors: Mohamed M. Abdalla, Bakr F. Abdel-wahab, Abdel-galil E. Amr
    Abstract:

    N -( p -substituted phenyl)-4-cyanopyrrolidin-3-ones and their corresponding hydrazines were prepared and used as starting materials to synthesize heterocyclic candidates as Serotonin Antagonist and antianexity agents. Condensation of hydrazines with selected aromatic aldehydes afforded the corresponding Schiff bases. The hydrazines were treated with phenyl isothiocyanate to afford the corresponding thiosemicarbazides, which were cyclized with ethyl bromoacetate to N -phenylthiazolidinones. The hydrazine was reacted with 1,2,4,5-tetrachlorophthalic anhydride to give the tetrachloroimide derivative. It was reacted with benzoyl acetonitrile, 2-(bismethylsulfanyl-methylene)malononitrile, 2-ethoxymethylenemalononitrile, or 2-cyano-3-ethoxyacrylic acid ethyl ester to afford the corresponding pyrazoline derivatives. Schiff bases were obtained by simple condensation of the hydrazine with different carbonyl compounds. All the compounds were screened for their Serotonin Antagonistic and antianexity activities, and they showed high activities compared to buspirone and diazepam as controls. Graphical abstract

Michael A Puniak - One of the best experts on this subject based on the ideXlab platform.

  • the Serotonin Antagonist mianserin improves functional recovery following experimental spinal trauma
    Annals of Neurology, 1991
    Co-Authors: Steven K Salzman, Michael A Puniak, Zhongjun Liu, Richard P Maitlandheriot, Gina M Freeman, Cynthia A Agresta
    Abstract:

    The ability of the Serotonin Antagonist mianserin to improve neurological recovery after graded impact trauma to the thoracic region of the spinal cord was compared to that of cyproheptadine and ketanserin in pentobarbital-anesthetized rats. Spinal cord injury was produced at T-10 by the weight-drop method and confirmed by the disappearance of the somatosensory-evoked response during the subsequent 15 minutes. In all experiments, drug or vehicle treatments were randomly administered as a single intravenous bolus 15 minutes after injury. Functional outcome was blindly assessed for 2 weeks after injury using a modified Tarlov scale, and in some cases, the Rivlin-Tator angleboard test. The survival of descending raphe-spinal axons was determined by the measurement of Serotonin in postmortem spinal tissues located above and below the site of injury. In separate acute experiments, the physiological and hemodynamic correlates of a 50 gm cm injury and either mianserin or vehicle injection were examined, as were the effects on Serotonin content and metabolism in spinal tissues harvested 30 minutes after injury. All doses of mainserin were associated with some index of improved recovery following a 50 gm cm injury, with a 1-mg/kg dose being clearly superior. Both ketanserin (0.1 mg/kg) and cyproheptadine (2 mg/kg) displayed marginal therapeutic actions for 50 gm cm injuries. In acute studies, mianserin at 1 mg/kg was associated with the preservation of posttraumatic spinal cord blood flow at T-12 as well as a pronounced alteration in postmortem spinal Serotonin content and metabolism, in contrast to vehicle control treatments. These data lend further support to a serotonergic hypothesis of secondary spinal cord injury and suggest the potential use of mianserin for the acute treatment of spinal cord injury.

  • Comparison of a Serotonin Antagonist, opioid Antagonist, and TRH analog for the acute treatment of experimental spinal trauma.
    Journal of neurotrauma, 1991
    Co-Authors: Michael A Puniak, Gina M Freeman, Cynthia A Agresta, Laura Van Newkirk, Carol A. Barone, Steven K Salzman
    Abstract:

    ABSTRACT The therapeutic efficacies of a Serotonin Antagonist (mianserin), an opioid Antagonist (nalmefene), and a TRH analog (YM-14673) were compared in a well-characterized model of experimental ...

Gina M Freeman - One of the best experts on this subject based on the ideXlab platform.

  • the Serotonin Antagonist mianserin improves functional recovery following experimental spinal trauma
    Annals of Neurology, 1991
    Co-Authors: Steven K Salzman, Michael A Puniak, Zhongjun Liu, Richard P Maitlandheriot, Gina M Freeman, Cynthia A Agresta
    Abstract:

    The ability of the Serotonin Antagonist mianserin to improve neurological recovery after graded impact trauma to the thoracic region of the spinal cord was compared to that of cyproheptadine and ketanserin in pentobarbital-anesthetized rats. Spinal cord injury was produced at T-10 by the weight-drop method and confirmed by the disappearance of the somatosensory-evoked response during the subsequent 15 minutes. In all experiments, drug or vehicle treatments were randomly administered as a single intravenous bolus 15 minutes after injury. Functional outcome was blindly assessed for 2 weeks after injury using a modified Tarlov scale, and in some cases, the Rivlin-Tator angleboard test. The survival of descending raphe-spinal axons was determined by the measurement of Serotonin in postmortem spinal tissues located above and below the site of injury. In separate acute experiments, the physiological and hemodynamic correlates of a 50 gm cm injury and either mianserin or vehicle injection were examined, as were the effects on Serotonin content and metabolism in spinal tissues harvested 30 minutes after injury. All doses of mainserin were associated with some index of improved recovery following a 50 gm cm injury, with a 1-mg/kg dose being clearly superior. Both ketanserin (0.1 mg/kg) and cyproheptadine (2 mg/kg) displayed marginal therapeutic actions for 50 gm cm injuries. In acute studies, mianserin at 1 mg/kg was associated with the preservation of posttraumatic spinal cord blood flow at T-12 as well as a pronounced alteration in postmortem spinal Serotonin content and metabolism, in contrast to vehicle control treatments. These data lend further support to a serotonergic hypothesis of secondary spinal cord injury and suggest the potential use of mianserin for the acute treatment of spinal cord injury.

  • Comparison of a Serotonin Antagonist, opioid Antagonist, and TRH analog for the acute treatment of experimental spinal trauma.
    Journal of neurotrauma, 1991
    Co-Authors: Michael A Puniak, Gina M Freeman, Cynthia A Agresta, Laura Van Newkirk, Carol A. Barone, Steven K Salzman
    Abstract:

    ABSTRACT The therapeutic efficacies of a Serotonin Antagonist (mianserin), an opioid Antagonist (nalmefene), and a TRH analog (YM-14673) were compared in a well-characterized model of experimental ...