Abstract Ethnopharmacological relevance Achillea millefolium L
... into and time spent on the open arms, at doses that do not affect locomotor activity (Lister, 1987 and Borsini et al., 2002). However, debatable is whether the elevated plus maze can detect the anxiolytic-like effects of antidepressants, such as selective serotonin reuptake inhibitors (Rodgers and C ...
... into and time spent on the open arms, at doses that do not affect locomotor activity (Lister, 1987 and Borsini et al., 2002). However, debatable is whether the elevated plus maze can detect the anxiolytic-like effects of antidepressants, such as selective serotonin reuptake inhibitors (Rodgers and C ...
Targeting proteases: successes, failures and future prospects
... Development of the current generation of ACE inhibitors (FIG. 2b) is a special story, because 30 years ago neither the sequence nor three-dimensional structure of the enzyme was available. Instead, the structure of carboxypeptidase A, now known to be considerably different from that of ACE, was used ...
... Development of the current generation of ACE inhibitors (FIG. 2b) is a special story, because 30 years ago neither the sequence nor three-dimensional structure of the enzyme was available. Instead, the structure of carboxypeptidase A, now known to be considerably different from that of ACE, was used ...
[Salvia divinorum - a potential drug for abuse]
... humans (Siebert DJ, 1994). Additionally, given that its pharmacological action (kappa-opioid receptor agonist) is quite unique compared to other hallucinogens (some of which act via the serotonin 5-HT receptor), salvinorin A's long-term effects remain to be established. Therefore, the risks of Salvi ...
... humans (Siebert DJ, 1994). Additionally, given that its pharmacological action (kappa-opioid receptor agonist) is quite unique compared to other hallucinogens (some of which act via the serotonin 5-HT receptor), salvinorin A's long-term effects remain to be established. Therefore, the risks of Salvi ...
Docking and Ligand Binding Affinity: Uses and Pitfalls
... predict the structure of the intermolecular complex formed between two or more constituent molecules, trying to predict the position and orientation of a ligand (a small molecule) when it is bound to a protein in order to know the predominant binding mode(s) of a ligand with a protein of known three ...
... predict the structure of the intermolecular complex formed between two or more constituent molecules, trying to predict the position and orientation of a ligand (a small molecule) when it is bound to a protein in order to know the predominant binding mode(s) of a ligand with a protein of known three ...
pharmacology basic principles
... SA of GI tract, mixing of contents, pH differences at different levels; can be destroyed by acid (eg. Some penicillins) and enzymes (eg. Insulin is hydrolysed) and microbial activity INH: can be used from agents that vaporize easily (eg. Amyl nitrite) or can be dispersed in aqueous droplets (eg. Erg ...
... SA of GI tract, mixing of contents, pH differences at different levels; can be destroyed by acid (eg. Some penicillins) and enzymes (eg. Insulin is hydrolysed) and microbial activity INH: can be used from agents that vaporize easily (eg. Amyl nitrite) or can be dispersed in aqueous droplets (eg. Erg ...
Elicited hippocampal theta rhythm: a screen for anxiolytic and
... presence of these gating systems is important for our understanding of the different effects that can be obtained with elicitation of theta from different ascending systems. Stimulation of ascending cholinergic systems can elicit clear theta; but increasing levels of stimulation have a very modest e ...
... presence of these gating systems is important for our understanding of the different effects that can be obtained with elicitation of theta from different ascending systems. Stimulation of ascending cholinergic systems can elicit clear theta; but increasing levels of stimulation have a very modest e ...
Cox-2-Selective Inhibitors: The New Super Aspirins
... properties. Although many of the 1,5-diarylpyrazoles that possessed 5(4-halophenyl) substituents (e.g., SC58128 and SC588; Fig. 1) had good selectivity and in vivo activity, they also possessed unacceptably long in vivo half-lives (.100 h) (Penning et al., 1997). Substitution of the 5(4-halophenyl) ...
... properties. Although many of the 1,5-diarylpyrazoles that possessed 5(4-halophenyl) substituents (e.g., SC58128 and SC588; Fig. 1) had good selectivity and in vivo activity, they also possessed unacceptably long in vivo half-lives (.100 h) (Penning et al., 1997). Substitution of the 5(4-halophenyl) ...
Review Advances in nucleoside monophosphate prodrugs as anti
... As discussed earlier, some nucleoside analogues have poor cell permeability and/or are not suitable substrates for cellular kinases, which transform it to the biologically active NTP. This problem can be alleviated by the use of a substituted MP prodrug strategy that would be converted, initially, t ...
... As discussed earlier, some nucleoside analogues have poor cell permeability and/or are not suitable substrates for cellular kinases, which transform it to the biologically active NTP. This problem can be alleviated by the use of a substituted MP prodrug strategy that would be converted, initially, t ...
09107sgp04
... transient effects that resolved with regular dosing. In dogs, heart rate increases were greater after co-administration than after salmeterol alone. ...
... transient effects that resolved with regular dosing. In dogs, heart rate increases were greater after co-administration than after salmeterol alone. ...
Pharmacokinetics and pharmacodynamics of oral oxycodone in
... O-demethylation of codeine has been shown to account for most, if not all, of the analgesic activity of codeine.6,7 Oxymorphone is a remarkably potent -opioid ligand, with 2 to 5 times higher -opioid receptor affinity and in vivo analgesic potency than morphine.8 –11 However, recent data showed th ...
... O-demethylation of codeine has been shown to account for most, if not all, of the analgesic activity of codeine.6,7 Oxymorphone is a remarkably potent -opioid ligand, with 2 to 5 times higher -opioid receptor affinity and in vivo analgesic potency than morphine.8 –11 However, recent data showed th ...
Role of Mu- and Delta-Opioid Receptors in the
... reinstatement of cocaine seeking, and intra-NAc morphine infusions induce a conditioned place preference (van der Kooy et al, 1982). Opioid receptors are highly expressed by NAc neurons (Mansour et al, 1995, 1987), and local opioid infusions in the NAc modulate behavior in a biphasic manner. Thus, m ...
... reinstatement of cocaine seeking, and intra-NAc morphine infusions induce a conditioned place preference (van der Kooy et al, 1982). Opioid receptors are highly expressed by NAc neurons (Mansour et al, 1995, 1987), and local opioid infusions in the NAc modulate behavior in a biphasic manner. Thus, m ...
Salvia divinorum and Salvinorin A: An Update on Pharmacology and
... A further study evaluated the effect of products of the in vitro autoxidation of salvinorin A. The main product of the neutral fraction after basic cleavage with 1 M KOH in methanol was an enedione. The major product in the base-soluble fraction was the 1,2-secotriester. Both the enedione and 1,2-se ...
... A further study evaluated the effect of products of the in vitro autoxidation of salvinorin A. The main product of the neutral fraction after basic cleavage with 1 M KOH in methanol was an enedione. The major product in the base-soluble fraction was the 1,2-secotriester. Both the enedione and 1,2-se ...
Liver X Receptor Agonists as Potential Therapeutic Agents for
... molecule ligand, such as estradiol for the estrogen receptor, to a nuclear receptor modulates transcription of target genes through the binding of the nuclear receptor/ligand complex to appropriate response elements in the proximal promoter of target genes. The nuclear receptors LXR␣ (NR1H3) and LXR ...
... molecule ligand, such as estradiol for the estrogen receptor, to a nuclear receptor modulates transcription of target genes through the binding of the nuclear receptor/ligand complex to appropriate response elements in the proximal promoter of target genes. The nuclear receptors LXR␣ (NR1H3) and LXR ...