The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Aurelio Orjales - One of the best experts on this subject based on the ideXlab platform.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. Design and methods: In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum. Results: Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guineapig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity. Conclusions: These Preclinical studies provide evidence that bilastine has H1-antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.
Luis Labeaga - One of the best experts on this subject based on the ideXlab platform.
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Preclinical Pharmacology of f 98214 ta a novel potent serotonin and norepinephrine uptake inhibitor with antidepressant and anxiolytic properties
Psychopharmacology, 2005Co-Authors: Ines Artaiz, Ana Innerarity, Arturo Zazpe, Elena Del Olmo, Alvaro Diaz, Jose Angel Ruizortega, Elena Castro, Ruth Pena, Luis LabeagaAbstract:Rationale Serotonin (5-HT) and norepinephrine (NE) re-uptake inhibitors (SNRIs) have been proposed to have a higher efficacy and/or faster onset of action than previously available antidepressants.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. Design and methods: In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum. Results: Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guineapig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity. Conclusions: These Preclinical studies provide evidence that bilastine has H1-antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.
Ana Innerarity - One of the best experts on this subject based on the ideXlab platform.
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Preclinical Pharmacology of f 98214 ta a novel potent serotonin and norepinephrine uptake inhibitor with antidepressant and anxiolytic properties
Psychopharmacology, 2005Co-Authors: Ines Artaiz, Ana Innerarity, Arturo Zazpe, Elena Del Olmo, Alvaro Diaz, Jose Angel Ruizortega, Elena Castro, Ruth Pena, Luis LabeagaAbstract:Rationale Serotonin (5-HT) and norepinephrine (NE) re-uptake inhibitors (SNRIs) have been proposed to have a higher efficacy and/or faster onset of action than previously available antidepressants.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. Design and methods: In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum. Results: Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guineapig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity. Conclusions: These Preclinical studies provide evidence that bilastine has H1-antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.
Reyes Corcostegui - One of the best experts on this subject based on the ideXlab platform.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist.
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Preclinical Pharmacology of bilastine a new selective histamine h1 receptor antagonist receptor selectivity and in vitro antihistaminic activity
Drugs in R & D, 2005Co-Authors: Reyes Corcostegui, Luis Labeaga, Ana Innerarity, Agustin Berisa, Aurelio OrjalesAbstract:Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. Design and methods: In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum. Results: Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guineapig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity. Conclusions: These Preclinical studies provide evidence that bilastine has H1-antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.
Hans Rollema - One of the best experts on this subject based on the ideXlab platform.
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Preclinical Pharmacology of the alpha4beta2 nachr partial agonist varenicline related to effects on reward mood and cognition
Biochemical Pharmacology, 2009Co-Authors: Hans Rollema, Mihaly Hajos, Patricia A Seymour, Rouba Kozak, Mark J Majchrzak, Victor Guanowsky, Weldon Horner, Doug S Chapin, William E Hoffmann, David E JohnsonAbstract:The pharmacological properties and pharmacokinetic profile of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target receptor that for a large part explain its efficacy as a smoking cessation aid. Since alpha4beta2 and other nAChR subtypes play important roles in mediating central processes that control reward, mood, cognition and attention, there is interest in examining the effects of selective nAChR ligands such as varenicline in Preclinical animal models that assess these behaviors. Here we describe results from studies on varenicline's effects in animal models of addiction, depression, cognition and attention and discuss these in the context of recently published Preclinical and preliminary clinical studies that collected data on varenicline's effects on mood, cognition and alcohol abuse disorder. Taken together, the Preclinical and the limited clinical data show beneficial effects of varenicline, but further clinical studies are needed to evaluate whether the Preclinical effects observed in animal models are translatable to the clinic.
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Preclinical Pharmacology of the α4β2 nachr partial agonist varenicline related to effects on reward mood and cognition
Biochemical Pharmacology, 2009Co-Authors: Hans Rollema, Mihaly Hajos, Patricia A Seymour, Rouba Kozak, Mark J Majchrzak, Victor Guanowsky, Weldon Horner, Doug S Chapin, William E Hoffmann, David E JohnsonAbstract:The pharmacological properties and pharmacokinetic profile of the α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target receptor that for a large part explain its efficacy as a smoking cessation aid. Since α4β2 and other nAChR subtypes play important roles in mediating central processes that control reward, mood, cognition and attention, there is interest in examining the effects of selective nAChR ligands such as varenicline in Preclinical animal models that assess these behaviors. Here we describe results from studies on varenicline's effects in animal models of addiction, depression, cognition and attention and discuss these in the context of recently published Preclinical and preliminary clinical studies that collected data on varenicline's effects on mood, cognition and alcohol abuse disorder. Taken together, the Preclinical and the limited clinical data show beneficial effects of varenicline, but further clinical studies are needed to evaluate whether the Preclinical effects observed in animal models are translatable to the clinic.
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pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline an effective smoking cessation aid
Neuropharmacology, 2007Co-Authors: Hans Rollema, Leslie K Chambers, John Glowa, Raymond S Hurst, Charles C Rovetti, Robert J Mather, Robert S Mansbach, Lorraine A Lebel, Yi Lu, Steven Bradley SandsAbstract:The Preclinical Pharmacology of the α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline, a novel smoking cessation agent is described. Varenicline binds with subnanomolar affinity only to α4β2 nAChRs and in vitro functional patch clamp studies in HEK cells expressing nAChRs show that varenicline is a partial agonist with 45% of nicotine's maximal efficacy at α4β2 nAChRs. In neurochemical models varenicline has significantly lower (40–60%) efficacy than nicotine in stimulating [3H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than nicotine. In addition, when combined with nicotine, varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of varenicline alone, consistent with partial agonism. Finally, varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. These data suggest that varenicline can reproduce to some extent the subjective effects of smoking by partially activating α4β2 nAChRs, while preventing full activation of these receptors by nicotine. Based on these findings, varenicline was advanced into clinical development and recently shown to be an effective and safe aid for smoking cessation treatment.
