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The behavioral pharmacology of hallucinogens
... The observation of drug-elicited behaviors can be immensely helpful in the initial characterization of the pharmacological actions of new compounds in vivo. For instance, the Straub tail reaction in rodents (contraction of the sacrococcygeus muscle, resulting in erection of the tail) is readily obse ...
... The observation of drug-elicited behaviors can be immensely helpful in the initial characterization of the pharmacological actions of new compounds in vivo. For instance, the Straub tail reaction in rodents (contraction of the sacrococcygeus muscle, resulting in erection of the tail) is readily obse ...
SYNTHESIS, ANTIOXIDANT AND ANTHELMINTIC ACTIVITY OF THE LINEAR TETRAPEPTIDE L-(Leu-Pro-Gly)-D-Ala (LPGA)
... The linear tetrapeptide L-(Leu-Pro-Gly)-D-Ala (LPGA) is a part of the naturally occurring cyclic heptapeptide, Glaucacyclopeptide A, isolated from the seeds of Annona glauca belonging to the family, Annonaceae. Plants of Annonaceae family are used in folk medicine in various capacities, such as anti ...
... The linear tetrapeptide L-(Leu-Pro-Gly)-D-Ala (LPGA) is a part of the naturally occurring cyclic heptapeptide, Glaucacyclopeptide A, isolated from the seeds of Annona glauca belonging to the family, Annonaceae. Plants of Annonaceae family are used in folk medicine in various capacities, such as anti ...
Atypical Neuroleptics Enhance Histamine Turnover in Brain Via 5
... include a lower propensity to elicit extrapyramidal side-effects, an improved therapeutic efficacy on negative and affective symptomatology of schizophrenia as well as on refractory forms of the disease. These drugs, often designated “atypical” antipsychotics, a rather vague terminology, were mostly ...
... include a lower propensity to elicit extrapyramidal side-effects, an improved therapeutic efficacy on negative and affective symptomatology of schizophrenia as well as on refractory forms of the disease. These drugs, often designated “atypical” antipsychotics, a rather vague terminology, were mostly ...
The Nemertine Toxin Anabaseine and Its Derivative DMXBA (GTS-21): Chemical and Pharmacological Properties
... sites are located at the subunit interface (reviewed in [3,4]), a detailed analysis about the interface, as well as its interaction with the Hepes molecule that has been observed in the AChBP crystal, was performed. Furthermore, a ligand-binding pocket was defined providing useful information for co ...
... sites are located at the subunit interface (reviewed in [3,4]), a detailed analysis about the interface, as well as its interaction with the Hepes molecule that has been observed in the AChBP crystal, was performed. Furthermore, a ligand-binding pocket was defined providing useful information for co ...
Terms and symbols - Guide to Pharmacology
... such, to avoid confusion). Furthermore, a receptor may consist of several proteins, called subunits. In some cases the large number of combinatorial possibilities for assembly of multiple subunits may require NC-IUPHAR to use an interim nomenclature based on the individual subunits (Spedding et al., ...
... such, to avoid confusion). Furthermore, a receptor may consist of several proteins, called subunits. In some cases the large number of combinatorial possibilities for assembly of multiple subunits may require NC-IUPHAR to use an interim nomenclature based on the individual subunits (Spedding et al., ...
Structure-based drug design strategies in medicinal
... The combined use of both HTS and SBVS is an important strategy in medicinal chemistry that has allowed the identification of inhibitors of the protein tyrosine phosphatase 1B (PTP1B) (Fig. 3), which plays an important role in metabolism and has been identified as a target for obesity and type II dia ...
... The combined use of both HTS and SBVS is an important strategy in medicinal chemistry that has allowed the identification of inhibitors of the protein tyrosine phosphatase 1B (PTP1B) (Fig. 3), which plays an important role in metabolism and has been identified as a target for obesity and type II dia ...
Document
... four of the adenosine receptors are involved in this effect • Because of this, adenosine itself may be used as a drug, being given as an intravenous bolus injection to terminate supraventricular tachycardia • It is safer than Beta-adrenoceptor antagonists or verapamil, because of its short duration ...
... four of the adenosine receptors are involved in this effect • Because of this, adenosine itself may be used as a drug, being given as an intravenous bolus injection to terminate supraventricular tachycardia • It is safer than Beta-adrenoceptor antagonists or verapamil, because of its short duration ...
patrick_tb_ch05
... based on a drug's pharmacophore. Pharmacodynamics is the study of how a drug interacts with its target binding site at the molecular level. Structure activity relationships is the study of which functional groups are important in binding a drug to its target binding site. Page reference: 77-78 a. Ph ...
... based on a drug's pharmacophore. Pharmacodynamics is the study of how a drug interacts with its target binding site at the molecular level. Structure activity relationships is the study of which functional groups are important in binding a drug to its target binding site. Page reference: 77-78 a. Ph ...
Revisiting AMPA receptors as an antiepileptic drug target
... and also to its epileptogenic effects (18). However, kainate also acts on AMPA receptors, albeit at somewhat higher concentrations, and many of its actions are likely to be mediated by AMPA and not kainate receptors. The role of kainate receptors in the pathophysiology of seizures is still incomplet ...
... and also to its epileptogenic effects (18). However, kainate also acts on AMPA receptors, albeit at somewhat higher concentrations, and many of its actions are likely to be mediated by AMPA and not kainate receptors. The role of kainate receptors in the pathophysiology of seizures is still incomplet ...
Revisiting AMPA Receptors as an Antiepileptic Drug Target
... and also to its epileptogenic effects (18). However, kainate also acts on AMPA receptors, albeit at somewhat higher concentrations, and many of its actions are likely to be mediated by AMPA and not kainate receptors. The role of kainate receptors in the pathophysiology of seizures is still incomplet ...
... and also to its epileptogenic effects (18). However, kainate also acts on AMPA receptors, albeit at somewhat higher concentrations, and many of its actions are likely to be mediated by AMPA and not kainate receptors. The role of kainate receptors in the pathophysiology of seizures is still incomplet ...
Release of norepinephrine: Removal of norepinephrine:
... interacts with the α 1 receptors. A portion of the released norepinephrine (circles back) and reacts with α 2 receptors on the neuronal membrane. The stimulation of the α 2 receptor causes feedback inhibition of the ongoing release of norepinephrine from the stimulated adrenergic neuron. This inhibi ...
... interacts with the α 1 receptors. A portion of the released norepinephrine (circles back) and reacts with α 2 receptors on the neuronal membrane. The stimulation of the α 2 receptor causes feedback inhibition of the ongoing release of norepinephrine from the stimulated adrenergic neuron. This inhibi ...
Anti-platelets
... • Dose: 0.25 mg/kg IV before PCI followed by 10 g/min for 12 hrs 2) Eptifibatide • Cyclic peptide inhibitor of the fibrinogen binding site on GpIIb/IIIa receptor • Short duration of action: 6-12 hrs • Given with aspirin and heparin • Use: – Acute coronary syndrome – Angioplastic coronary interventi ...
... • Dose: 0.25 mg/kg IV before PCI followed by 10 g/min for 12 hrs 2) Eptifibatide • Cyclic peptide inhibitor of the fibrinogen binding site on GpIIb/IIIa receptor • Short duration of action: 6-12 hrs • Given with aspirin and heparin • Use: – Acute coronary syndrome – Angioplastic coronary interventi ...
Polyamine transporter selective compounds as anticancer agents
... access to cells (i.e. polyamine conjugates). Chinese hamster ovary cells which are chemically mutated to be polyamine transport-deficient will be referred to as the CHO-MG cell line. This cell type should have lower susceptibility to polyamine conjugates which use the polyamine transporter to gain a ...
... access to cells (i.e. polyamine conjugates). Chinese hamster ovary cells which are chemically mutated to be polyamine transport-deficient will be referred to as the CHO-MG cell line. This cell type should have lower susceptibility to polyamine conjugates which use the polyamine transporter to gain a ...
JDP Featured in BioCentury
... Number of employees: 3 Funds raised: Undisclosed Investors: Private investors CEO: Jie Du Patents: None issued usually very sick, with pulse and breathing rates already below normal. Diphenhydramine can further lower these measures, making constant monitoring a necessity and increasing cost of care. ...
... Number of employees: 3 Funds raised: Undisclosed Investors: Private investors CEO: Jie Du Patents: None issued usually very sick, with pulse and breathing rates already below normal. Diphenhydramine can further lower these measures, making constant monitoring a necessity and increasing cost of care. ...
The lead compound
... •Enzyme Inhibition tests •Identify competitive or non competitive inhibition • Strength of inhibition measured as IC50 • IC50 = concentration of inhibitor required to reduce enzyme activity by 50% •Receptor tests •Not easy to isolate membrane bound receptors • Carried out on whole cells, tissue cult ...
... •Enzyme Inhibition tests •Identify competitive or non competitive inhibition • Strength of inhibition measured as IC50 • IC50 = concentration of inhibitor required to reduce enzyme activity by 50% •Receptor tests •Not easy to isolate membrane bound receptors • Carried out on whole cells, tissue cult ...
Invited Review - International Journal of Pharmaceutical Science
... thiazole acetohydrazones and screened them for their diuretic M. tuberculosis strain H37 Rv showed moderate to better activity. A potent diuretic activity was confirmed for the 2activity. It was noted that the cyano group may not have any methyl derivative bearing a phenyl ring at position C-6 [33]. ...
... thiazole acetohydrazones and screened them for their diuretic M. tuberculosis strain H37 Rv showed moderate to better activity. A potent diuretic activity was confirmed for the 2activity. It was noted that the cyano group may not have any methyl derivative bearing a phenyl ring at position C-6 [33]. ...
Pharmacodynamics of Selective Androgen Receptor
... were used in each animal to deliver TP at 0.5 and 0.75 mg/day. One osmotic pump was used in each animal for other groups. After 14 days of drug treatment, rats were weighed, anesthetized, and sacrificed. Blood samples were collected by venipuncture of the abdominal aorta. For each animal, a whole bl ...
... were used in each animal to deliver TP at 0.5 and 0.75 mg/day. One osmotic pump was used in each animal for other groups. After 14 days of drug treatment, rats were weighed, anesthetized, and sacrificed. Blood samples were collected by venipuncture of the abdominal aorta. For each animal, a whole bl ...
HST-151
... autoreceptors (specific for transmitter released) and heteroreceptors (specific for a different transmitter). At the neuromuscular junction, cholinergic agonists can either enhance (acute response, facilitation) or inhibit (chronic response, from repetitive stimulation) the release of ACh. These sep ...
... autoreceptors (specific for transmitter released) and heteroreceptors (specific for a different transmitter). At the neuromuscular junction, cholinergic agonists can either enhance (acute response, facilitation) or inhibit (chronic response, from repetitive stimulation) the release of ACh. These sep ...
Chalcone-based aryloxypropanolamine as a
... sympathetic nervous system and can be stimulated by 3adrenergic receptor agonists. The stimulation of the receptor mediates lipolysis to initiate the thermogenic process devoid of ATP synthesis, increase oxygen consumption, decrease glucose and food intake7. The dual actions of antiobesity and anti ...
... sympathetic nervous system and can be stimulated by 3adrenergic receptor agonists. The stimulation of the receptor mediates lipolysis to initiate the thermogenic process devoid of ATP synthesis, increase oxygen consumption, decrease glucose and food intake7. The dual actions of antiobesity and anti ...
Anti-platelet agents
... • PGI2- inhibit platelet aggregation • TXA2- platelet aggregation • Elevated c-AMP- inhibit platelet aggregation & vice versa • ADP receptors(P2Y1,P2Y2)-changes shape & platelet aggregation • GPIIb/IIIa receptors- binds fibrinogen & platelets ...
... • PGI2- inhibit platelet aggregation • TXA2- platelet aggregation • Elevated c-AMP- inhibit platelet aggregation & vice versa • ADP receptors(P2Y1,P2Y2)-changes shape & platelet aggregation • GPIIb/IIIa receptors- binds fibrinogen & platelets ...
Selective Inhibitors of Picornavirus Replication
... Numerous studies have been performed in the past decades on a series of compounds developed by Sterling-Winthrop, commonly known as ‘‘WIN compounds.’’ Following lead optimization of an accidentally discovered compound, a drug was developed that would meet most of the criteria of a successful anti-pi ...
... Numerous studies have been performed in the past decades on a series of compounds developed by Sterling-Winthrop, commonly known as ‘‘WIN compounds.’’ Following lead optimization of an accidentally discovered compound, a drug was developed that would meet most of the criteria of a successful anti-pi ...
51th ICAAC Chicago, IL September 17
... Four reports at this meeting spelled out early findings on BI 224436, an HIV integrase inhibitor with a mechanism different from that of the "tegravir" strand-transfer integrase inhibitors. This novel agent, being developed by Boehringer Ingelheim, binds to a highly conserved allosteric pocket of th ...
... Four reports at this meeting spelled out early findings on BI 224436, an HIV integrase inhibitor with a mechanism different from that of the "tegravir" strand-transfer integrase inhibitors. This novel agent, being developed by Boehringer Ingelheim, binds to a highly conserved allosteric pocket of th ...
Structure-Based Identification of Binding Sites, Native Ligands and
... As described earlier, a standard experimental method for identifying ligands for new GPCRs is to rigorously test in vitro many hundreds of potential binding compounds. This is extremely time-consuming and as a result of the sheer scale of the task means that many important potential ligands are miss ...
... As described earlier, a standard experimental method for identifying ligands for new GPCRs is to rigorously test in vitro many hundreds of potential binding compounds. This is extremely time-consuming and as a result of the sheer scale of the task means that many important potential ligands are miss ...
... similarity to mianserin, an antidepressant drug with antihistamine and 5-HT2 antagonistic properties [1]. Epinastine was originally introduced as an antihistamine drug without sedative side-effects on the central nervous system, due to favourable physicochemical properties. Its low lipophilicity and ...
this PDF file - Journal of the Indian Institute of Science
... (3) The existence of specific antagoaiats, such as naloxone and others, which block not only the actions of morphine, but also of many other classes of narcotic analgesics. (4) The fact that small structural changes, which are likely to alter the phya~cnlproperties of the ~noleculein only minor degr ...
... (3) The existence of specific antagoaiats, such as naloxone and others, which block not only the actions of morphine, but also of many other classes of narcotic analgesics. (4) The fact that small structural changes, which are likely to alter the phya~cnlproperties of the ~noleculein only minor degr ...
CCR5 receptor antagonist
![](https://commons.wikimedia.org/wiki/Special:FilePath/HIV_attachment.gif?width=300)
CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this receptor are entry inhibitors and have potential therapeutic applications in the treatment of HIV infections.The life cycle of the HIV presents potential targets for drug therapy, one of them being the viral entry pathway. The C-C motif chemokine receptors CCR5 and CXCR4 are the main chemokine receptors involved in the HIV entry process. These receptors belong to the seven transmembrane G-protein-coupled receptor (GPCR) family and are predominantly expressed on human T-cells, dendritic cells and macrophages, Langerhans cells. They play an important role as co-receptors that HIV type 1 (HIV-1) uses to attach to cells before viral fusion and entry into host cells. HIV isolates can be divided into R5 and X4 strains. R5 strain is when the virus uses the co-receptor CCR5 and X4 strain is when it uses CXCR4. The location of CCR5 receptors at the cell surface, both large and small molecules have the potential to interfere with the CCR5-viral interaction and inhibit viral entry into human cells.