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Sergio Mantegani - One of the best experts on this subject based on the ideXlab platform.
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d1 agonist and or d2 antagonist dopamine receptor properties of a series of ergoline derivatives a structure activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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Serotonergic ergoline derivatives
Bioorganic & medicinal chemistry letters, 1998Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Robert A Mcarthur, M. G. Fornaretto, Gabriele Damiani, Mario VarasiAbstract:Novel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT1A or 5-HT2 affinity and selectivity respectively.
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synthesis and antihypertensive activity of 2 4 dioxoimidazolidin 1 yl and perhydro 2 4 dioxopyrimidin 1 yl ergoline derivatives
Farmaco, 1998Co-Authors: Sergio Mantegani, E Lamberti, Enrico Di Salle, Enzo Brambilla, Carla Caccia, Laura Chiodini, Daniela Ruggieri, Patricia SalvatiAbstract:The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the Δ9,10 double bond for conferring high potency within these compounds.
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Synthesis and in vitro structure-activity relationship of 13-tert-butyl-ergoline derivatives as 5-HT1A receptor ligands
European Journal of Medicinal Chemistry, 1997Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, M. G. Fornaretto, R. A. Mc Arthur, Mario VarasiAbstract:Summary A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT1A receptors versus α1, α2, D1, D2, and 5-HT2 appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT1A affinity and hundred-fold selectivity versus the other receptors considered.
Carla Caccia - One of the best experts on this subject based on the ideXlab platform.
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d1 agonist and or d2 antagonist dopamine receptor properties of a series of ergoline derivatives a structure activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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Serotonergic ergoline derivatives
Bioorganic & medicinal chemistry letters, 1998Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Robert A Mcarthur, M. G. Fornaretto, Gabriele Damiani, Mario VarasiAbstract:Novel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT1A or 5-HT2 affinity and selectivity respectively.
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synthesis and antihypertensive activity of 2 4 dioxoimidazolidin 1 yl and perhydro 2 4 dioxopyrimidin 1 yl ergoline derivatives
Farmaco, 1998Co-Authors: Sergio Mantegani, E Lamberti, Enrico Di Salle, Enzo Brambilla, Carla Caccia, Laura Chiodini, Daniela Ruggieri, Patricia SalvatiAbstract:The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the Δ9,10 double bond for conferring high potency within these compounds.
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Synthesis and in vitro structure-activity relationship of 13-tert-butyl-ergoline derivatives as 5-HT1A receptor ligands
European Journal of Medicinal Chemistry, 1997Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, M. G. Fornaretto, R. A. Mc Arthur, Mario VarasiAbstract:Summary A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT1A receptors versus α1, α2, D1, D2, and 5-HT2 appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT1A affinity and hundred-fold selectivity versus the other receptors considered.
Enzo Brambilla - One of the best experts on this subject based on the ideXlab platform.
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d1 agonist and or d2 antagonist dopamine receptor properties of a series of ergoline derivatives a structure activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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Serotonergic ergoline derivatives
Bioorganic & medicinal chemistry letters, 1998Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Robert A Mcarthur, M. G. Fornaretto, Gabriele Damiani, Mario VarasiAbstract:Novel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT1A or 5-HT2 affinity and selectivity respectively.
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synthesis and antihypertensive activity of 2 4 dioxoimidazolidin 1 yl and perhydro 2 4 dioxopyrimidin 1 yl ergoline derivatives
Farmaco, 1998Co-Authors: Sergio Mantegani, E Lamberti, Enrico Di Salle, Enzo Brambilla, Carla Caccia, Laura Chiodini, Daniela Ruggieri, Patricia SalvatiAbstract:The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the Δ9,10 double bond for conferring high potency within these compounds.
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Synthesis and in vitro structure-activity relationship of 13-tert-butyl-ergoline derivatives as 5-HT1A receptor ligands
European Journal of Medicinal Chemistry, 1997Co-Authors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, M. G. Fornaretto, R. A. Mc Arthur, Mario VarasiAbstract:Summary A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT1A receptors versus α1, α2, D1, D2, and 5-HT2 appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT1A affinity and hundred-fold selectivity versus the other receptors considered.
Paul E. Schulze - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and Molecular Structure of a Rhenium Complex Derived from 8a-Amino-6-methyl-ergoline†
Chemische Berichte, 1997Co-Authors: Hartmut Spies, Steffi Noll, Matthias Findeisen, Peter Leibnitz, Bernhard Noll, Bernd Johannsen, Paul E. SchulzeAbstract:Current research in radiopharmaceutical chemistry is aimed at the design of technetium-based receptor-binding radiotracers because of the excellent nuclide properties of the isotope 99mTc. Tc tracers and the corresponding complexes of rhenium, as the inactive surrogate of Tc, are required to imitate organic agonists or antagonists of the receptor. We have started studies with Ergolines, which are known to be dopamine substitutes. The present report deals with the functionalization of 8α-amino-6-methyl-ergoline (2) with a 2-mercaptoacetyl group, and the subsequent synthesis of the first rhenium complex containing a pendent ergoline moiety [Re- O(SSS)(RS)] (HSSSH = HS-CH2CH2-S-CH2CH2-SH and RSH = 8a-amino-N-(2-mercaptoacetyl)-6-methyl-ergoline) (4). The molecular structure of the rhenium complex was determined by X-ray crystal structure analysis.
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Synthesis and Molecular Structure of a Rhenium Complex Derived from 8a‐Amino‐6‐methyl‐ergoline
Chemische Berichte, 1997Co-Authors: Hartmut Spies, Steffi Noll, Matthias Findeisen, Peter Leibnitz, Bernhard Noll, Bernd Johannsen, Paul E. SchulzeAbstract:Current research in radiopharmaceutical chemistry is aimed at the design of technetium-based receptor-binding radiotracers because of the excellent nuclide properties of the isotope 99mTc. Tc tracers and the corresponding complexes of rhenium, as the inactive surrogate of Tc, are required to imitate organic agonists or antagonists of the receptor. We have started studies with Ergolines, which are known to be dopamine substitutes. The present report deals with the functionalization of 8α-amino-6-methyl-ergoline (2) with a 2-mercaptoacetyl group, and the subsequent synthesis of the first rhenium complex containing a pendent ergoline moiety [Re- O(SSS)(RS)] (HSSSH = HS-CH2CH2-S-CH2CH2-SH and RSH = 8a-amino-N-(2-mercaptoacetyl)-6-methyl-ergoline) (4). The molecular structure of the rhenium complex was determined by X-ray crystal structure analysis.
Gabriella Traquandi - One of the best experts on this subject based on the ideXlab platform.
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d1 agonist and or d2 antagonist dopamine receptor properties of a series of ergoline derivatives a structure activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study
European Journal of Medicinal Chemistry, 1999Co-Authors: Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert A Mcarthur, Gabriella TraquandiAbstract:Abstract A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.