(NP) Rats
... proximately 10 to 20 times more pote nt tha n ROl5-4S13 in attenua ting EtO H intake. The results with DMCM, a full negative a llosteric mod ula to r of CI\ BAergic activity (Richards e t a l. 1991), showed tha t, a ltho ug h it was ca· pablc of decreasing EtOH intake, the reduction appeared to be p ...
... proximately 10 to 20 times more pote nt tha n ROl5-4S13 in attenua ting EtO H intake. The results with DMCM, a full negative a llosteric mod ula to r of CI\ BAergic activity (Richards e t a l. 1991), showed tha t, a ltho ug h it was ca· pablc of decreasing EtOH intake, the reduction appeared to be p ...
the-serotonergic-hallucinogen-5-meo-dmt-disrupts
... release in PFC mainly via 5-HT1A-R. Moreover, 5-MeO-DMT reduced LFCO in S1, Au1 and V1 of WT mice and only in V1 of KO2A mice, suggesting the involvement of 5-HT1A-R activation in the 5-MeO-DMT-induced disruption of V1 activity. In addition, antipsychotic drugs reversed 5-MeO-DMT effects in WT mice. ...
... release in PFC mainly via 5-HT1A-R. Moreover, 5-MeO-DMT reduced LFCO in S1, Au1 and V1 of WT mice and only in V1 of KO2A mice, suggesting the involvement of 5-HT1A-R activation in the 5-MeO-DMT-induced disruption of V1 activity. In addition, antipsychotic drugs reversed 5-MeO-DMT effects in WT mice. ...
antihistamines in allergic disease
... to 30% for cetirizine. Thus, second-generation H1 antihistamines are relatively free of sedating effects. Through H1 receptors histamine has various effects on the immune system, including the maturation of dendritic cells and modulation of the balance of helper T-cell type 1 (Th1) and Th2 towards T ...
... to 30% for cetirizine. Thus, second-generation H1 antihistamines are relatively free of sedating effects. Through H1 receptors histamine has various effects on the immune system, including the maturation of dendritic cells and modulation of the balance of helper T-cell type 1 (Th1) and Th2 towards T ...
Metabotropic Glutamate Receptors
... is and nobody knows what it is” (Selye, 1973). In spite of its frequent use, the word “stress” is at best an ambiguous term. In fact, it has been used to describe both what creates the stress and the response of the body to it. In order to circumvent this ambiguity, two different terms have been int ...
... is and nobody knows what it is” (Selye, 1973). In spite of its frequent use, the word “stress” is at best an ambiguous term. In fact, it has been used to describe both what creates the stress and the response of the body to it. In order to circumvent this ambiguity, two different terms have been int ...
The leukotriene-receptor antagonist MK-0679
... bronchoconstrictive leukotrienes [26]. Despite meeting these first two criteria of a mediator candidate, it has remained to be established that drugs which inhibit the action or release of leukotrienes can block ASA-induced airway obstruction. In one study, inhalation of a specific receptor antagoni ...
... bronchoconstrictive leukotrienes [26]. Despite meeting these first two criteria of a mediator candidate, it has remained to be established that drugs which inhibit the action or release of leukotrienes can block ASA-induced airway obstruction. In one study, inhalation of a specific receptor antagoni ...
Role for Reactive Oxygen Species in Methamphetamine Modulation
... today’s society, with over 1 in 20 adults over 26 having taken it at least once. While it is known that METH, a common psychostimulant, acts on both the mesolimbic dopamine (DA) and nigrostriatal DA systems by affecting proteins involved in DA reuptake and vesicular packaging, the specific mechanism ...
... today’s society, with over 1 in 20 adults over 26 having taken it at least once. While it is known that METH, a common psychostimulant, acts on both the mesolimbic dopamine (DA) and nigrostriatal DA systems by affecting proteins involved in DA reuptake and vesicular packaging, the specific mechanism ...
Vasopressin Axis in Shock States
... physiological role of vasopressin is the regulation of water balance. It does not appear to play a major role in the vascular regulation of blood pressure and abnormally high endogenous vasopressin levels (syndrome of IADH secretion) do not produce hypertension. ...
... physiological role of vasopressin is the regulation of water balance. It does not appear to play a major role in the vascular regulation of blood pressure and abnormally high endogenous vasopressin levels (syndrome of IADH secretion) do not produce hypertension. ...
Advances in pharmacotherapy for allergic conjunctivitis
... multiple mechanisms of action to help reduce the early phase immune response and the late-phase response by reducing eosinophil activation and infiltration [19,22]. Emedastine is another second-generation antihistamine that has a similar duration of action to levocabastine, but it has been shown to ...
... multiple mechanisms of action to help reduce the early phase immune response and the late-phase response by reducing eosinophil activation and infiltration [19,22]. Emedastine is another second-generation antihistamine that has a similar duration of action to levocabastine, but it has been shown to ...
Neuropharmacology of N,N-dimethyltryptamine
... distortion, depersonalization at high doses, and at least one (N,Ndiisopropyltryptamine, DiPT) causes auditory distortions, whereas some compounds such as DMT (found in ayahuasca), psilocybin (mushrooms) or mescaline (peyote) cause episodic visual effects. In the late 1990s, Rick Strassman conducted ...
... distortion, depersonalization at high doses, and at least one (N,Ndiisopropyltryptamine, DiPT) causes auditory distortions, whereas some compounds such as DMT (found in ayahuasca), psilocybin (mushrooms) or mescaline (peyote) cause episodic visual effects. In the late 1990s, Rick Strassman conducted ...
Phosphodiesterases Inhibition Enhances the Effect of Glucagon on
... cardiac arrhythmias has been reported in patients taken PDE inhibitors (Crickshank 1993). In summary, the present study provides the first evidence that PDE limits proarrhythmic effects of glucagon. This might have some practical interest since both glucagon and PDE inhibitors are considered to be u ...
... cardiac arrhythmias has been reported in patients taken PDE inhibitors (Crickshank 1993). In summary, the present study provides the first evidence that PDE limits proarrhythmic effects of glucagon. This might have some practical interest since both glucagon and PDE inhibitors are considered to be u ...
Inverted-U dopamine D1 receptor actions on prefrontal neurons
... n ¼ 12) also suppressed cell firing; however, as these neurons had higher firing rates in the NPD as well, suppression was observed for both the PD and the NPD. In summary, we found that high doses of D1R stimulation led to general suppressive effects with loss of cellular spatial information, where ...
... n ¼ 12) also suppressed cell firing; however, as these neurons had higher firing rates in the NPD as well, suppression was observed for both the PD and the NPD. In summary, we found that high doses of D1R stimulation led to general suppressive effects with loss of cellular spatial information, where ...
Coadministration of Galanin Antagonist M40 with a Muscarinic M1
... Subjects. All procedures were approved by the National Institute of Mental Health Animal C are and Use Committee and were conducted in accordance with the NIH Guide for the Care and Use of Laborator y Animals. Subjects were male Sprague Dawley rats (Taconic Farms, Germantown, N Y), 2 months old, and ...
... Subjects. All procedures were approved by the National Institute of Mental Health Animal C are and Use Committee and were conducted in accordance with the NIH Guide for the Care and Use of Laborator y Animals. Subjects were male Sprague Dawley rats (Taconic Farms, Germantown, N Y), 2 months old, and ...
A clickable analogue of ketamine retains NMDA receptor activity
... correlation among NMDAR activity, intracellular accumulation/retention, and behavioral effects. Thus, we advance first generation chemical biology tools to aid in the identification of ketamine targets. The non-competitive N-methyl-D-aspartate receptor (NMDAR) antagonist, ketamine, is a psychotomime ...
... correlation among NMDAR activity, intracellular accumulation/retention, and behavioral effects. Thus, we advance first generation chemical biology tools to aid in the identification of ketamine targets. The non-competitive N-methyl-D-aspartate receptor (NMDAR) antagonist, ketamine, is a psychotomime ...
kopia+_Eli_PR5`2006.vp:CorelVentura 7.0
... and, to a certain extent, glucose metabolism in the so-called peri-stroke region as well as in the relatively intact brain tissue [40]. Vinpocetine has been found to interfere with various stages of the ischemic cascade: adenosine triphosphate (ATP) depletion, activation of voltage-sensitive Na+- an ...
... and, to a certain extent, glucose metabolism in the so-called peri-stroke region as well as in the relatively intact brain tissue [40]. Vinpocetine has been found to interfere with various stages of the ischemic cascade: adenosine triphosphate (ATP) depletion, activation of voltage-sensitive Na+- an ...
patrick_tb_ch10
... 22) A lead compound containing a methyl ester functional group was hydrolysed to give an analogue with a carboxylic acid functional group. An in vivo bioassay which involved oral administration suggested that the ester was active and that the acid was inactive. However, an in vitro bioassay suggeste ...
... 22) A lead compound containing a methyl ester functional group was hydrolysed to give an analogue with a carboxylic acid functional group. An in vivo bioassay which involved oral administration suggested that the ester was active and that the acid was inactive. However, an in vitro bioassay suggeste ...
8 Ultra-low-dose opioid antagonists enhance opioid analgesia while
... that stimulate adenylyl cyclase, instead of coupling to the G proteins normally used by this receptor that inhibit this enzyme. Finally, while ultra-low-dose opioid antagonists enhance the analgesic efficacy of opiates, they decrease the addictive potential of opiates in rat models of drug reward, d ...
... that stimulate adenylyl cyclase, instead of coupling to the G proteins normally used by this receptor that inhibit this enzyme. Finally, while ultra-low-dose opioid antagonists enhance the analgesic efficacy of opiates, they decrease the addictive potential of opiates in rat models of drug reward, d ...
Unusual interactions of benzodiazepine receptor antagonists David
... that specific high-affinity ligands may produce opposite pharmacological effects and yet have a common antagonist. (...) predicted from receptor theory. The allosteric model ... 25/x ...
... that specific high-affinity ligands may produce opposite pharmacological effects and yet have a common antagonist. (...) predicted from receptor theory. The allosteric model ... 25/x ...
A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine
... and has reduced binding affinity for mGluR5 compared with MPEP (Keck et al. 2012). These off-target effects predict potential undesirable side effects or metabolic instability that were deemed too risky to advance these drugs into the clinic. In light of these limitations, extensive efforts have bee ...
... and has reduced binding affinity for mGluR5 compared with MPEP (Keck et al. 2012). These off-target effects predict potential undesirable side effects or metabolic instability that were deemed too risky to advance these drugs into the clinic. In light of these limitations, extensive efforts have bee ...
CRF Enhancement of GIRK Channel-Mediated
... signal is mediated by the activation of a G-protein-gated potassium conductance (GIRK or Kir3; Johnson and North, 1992; Beckstead et al, 2004). Animals lacking GIRK channels exhibit decreased cocaine self-administration behavior, suggesting a role for these channels in drug reinforcement (Morgan et ...
... signal is mediated by the activation of a G-protein-gated potassium conductance (GIRK or Kir3; Johnson and North, 1992; Beckstead et al, 2004). Animals lacking GIRK channels exhibit decreased cocaine self-administration behavior, suggesting a role for these channels in drug reinforcement (Morgan et ...
Laurate Biosensors Image Brain Neurotransmitters In Vivo: Can an Antihypertensive Medication Alter Psychostimulant Behavior?
... ambulatory motion in the central part of the chamber, indicating reduced anxiety). Thus, NMI provides a close cause and effect relationship between brain and behavior. Current technologies, e.g., microdialysis, are limited because microdialysis devices can traumatize brain tissue (1). We used NMI, b ...
... ambulatory motion in the central part of the chamber, indicating reduced anxiety). Thus, NMI provides a close cause and effect relationship between brain and behavior. Current technologies, e.g., microdialysis, are limited because microdialysis devices can traumatize brain tissue (1). We used NMI, b ...
B N ULLETI I N F O R M A T I O...
... Some GHB analog abusers begin consuming dietary supplements believing the claims made by manufacturers, and then find themselves addicted to the product. GHB analogs typically are abused in place of GHB by users who want to experience the effects associated with GHB and who find the analogs more wid ...
... Some GHB analog abusers begin consuming dietary supplements believing the claims made by manufacturers, and then find themselves addicted to the product. GHB analogs typically are abused in place of GHB by users who want to experience the effects associated with GHB and who find the analogs more wid ...
... is produced by cells of myeloid origin and probably mainly by polymorphonuclear leucocytes, is an effective chemotactic signal for leucocytes [2, 3]. The cysteinylcontaining LTC4, LTD4 and LTE4, which also are formed in many cells including mast cells and eosinophils, are potent inducers of bronchoc ...
Drug-induced psychomimetic effects as a model for psychosis
... and reserpine, let to the introduction of many more antipsychotic drugs with a similar mechanism of action, which are now referred to as typical antipsychotics (e.g. haloperidol, flupentixol, droperidol). In 1963, Carlsson and Lidqvist discovered that dopamine acts as a neurotransmitter (Carlsson a ...
... and reserpine, let to the introduction of many more antipsychotic drugs with a similar mechanism of action, which are now referred to as typical antipsychotics (e.g. haloperidol, flupentixol, droperidol). In 1963, Carlsson and Lidqvist discovered that dopamine acts as a neurotransmitter (Carlsson a ...
fullcvenglish_tmavromous
... work of the group on virgin olive oil adulteration is worthy of note”). LMA is involved in both activities. 8. Reference of my research activity on peptidomimetism by the company Synergix Ltd in the software of «Molecular Conceptor”. A chapter is written on the synthesis of Bioactive Molecules with ...
... work of the group on virgin olive oil adulteration is worthy of note”). LMA is involved in both activities. 8. Reference of my research activity on peptidomimetism by the company Synergix Ltd in the software of «Molecular Conceptor”. A chapter is written on the synthesis of Bioactive Molecules with ...
Cannabinoid receptor antagonist
The discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor antagonist, rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been shown to decrease food intake and regulate body-weight gain. The prevalence of obesity worldwide is increasing dramatically and has a great impact on public health. The lack of efficient and well-tolerated drugs to cure obesity has led to an increased interest in research and development of cannabinoid antagonists. Cannabidiol, a naturally occurring cannabinoid, is a non-competitive CB1/2 antagonist.