I The 1982 John
... pupils, euphoria, sedation, and nausea. Antagonists usually function by competing with the agonist for receptor sites, thus minimizing or eliminating agonist effects. Although they counteract agonists, they may themselves produce some agonistic effects, including analgesia. But in general, they do n ...
... pupils, euphoria, sedation, and nausea. Antagonists usually function by competing with the agonist for receptor sites, thus minimizing or eliminating agonist effects. Although they counteract agonists, they may themselves produce some agonistic effects, including analgesia. But in general, they do n ...
The anorectic effect of fenfluramine is influenced by sex and stage of
... (28). Rather, the orexigenic effect of testosterone appears to arise from its ability to stimulate the development of lean tissue mass, which functions to increase the male rat’s energy requirement (31). In contrast, considerable evidence suggests that estradiol decreases food intake by selectively ...
... (28). Rather, the orexigenic effect of testosterone appears to arise from its ability to stimulate the development of lean tissue mass, which functions to increase the male rat’s energy requirement (31). In contrast, considerable evidence suggests that estradiol decreases food intake by selectively ...
Binding of Imipramine to Phospholipid Bilayers Using
... The tendency to refer to the result of drug-lipid bilayer interaction as “binding” has been subject to discussion because of the general meaning of this term in the classic enzyme-substrate or ligand-receptor interaction studies (Heirwegh et al. 1992). Binding into a bilayer is considered a restrict ...
... The tendency to refer to the result of drug-lipid bilayer interaction as “binding” has been subject to discussion because of the general meaning of this term in the classic enzyme-substrate or ligand-receptor interaction studies (Heirwegh et al. 1992). Binding into a bilayer is considered a restrict ...
Dopamine, behavioral economics, and effort
... cost is too high), the animal reaches the point at which additional responses being required actually tend to suppress responding. For normal rats, responding at levels of FR64, FR100 or higher, even if there is only one 45 mg food pellet being delivered, does not seem to be problematic. A completel ...
... cost is too high), the animal reaches the point at which additional responses being required actually tend to suppress responding. For normal rats, responding at levels of FR64, FR100 or higher, even if there is only one 45 mg food pellet being delivered, does not seem to be problematic. A completel ...
Elicited hippocampal theta rhythm: a screen for anxiolytic and
... of response in the table can be attributed to the variation in receptor occupancy or interaction of particular drugs in different parts of the brain. No drug or drug class produces a specific limited effect (despite the omission of side effects from the table) but the variation in relative effective ...
... of response in the table can be attributed to the variation in receptor occupancy or interaction of particular drugs in different parts of the brain. No drug or drug class produces a specific limited effect (despite the omission of side effects from the table) but the variation in relative effective ...
Opioids - Waterloo Region Integrated Drugs Strategy
... Fentanyl is a potent opioid, used in anesthesia, for pain, chronic pain, pain in end of life care Typically administered as a patch placed on the skin Fentanyl is produced by pharmaceutical manufacturers Small chemical changes to fentanyl can result in drugs with very similar actions These “bootleg” ...
... Fentanyl is a potent opioid, used in anesthesia, for pain, chronic pain, pain in end of life care Typically administered as a patch placed on the skin Fentanyl is produced by pharmaceutical manufacturers Small chemical changes to fentanyl can result in drugs with very similar actions These “bootleg” ...
Opioid Withdrawal: A New Look At Medication
... the alpha-2 adrenergic agonist tizanidine in patients suffering from opioid addiction.13 In this study, 26 intravenous heroin users were divided into 2 groups; each group had the usual detoxification treatment, but patients in the experimental group were given tizanidine 8 mg three times daily. A su ...
... the alpha-2 adrenergic agonist tizanidine in patients suffering from opioid addiction.13 In this study, 26 intravenous heroin users were divided into 2 groups; each group had the usual detoxification treatment, but patients in the experimental group were given tizanidine 8 mg three times daily. A su ...
article in press
... programmed. After that, it was investigated the effect of guanosine, flunarizine and cinnarizine on animal models of psychosis, as well as in other behavioral tasks. Guanosine was chosen because it has been shown to interact with the glutamatergic system – which is known to be involved in the pathop ...
... programmed. After that, it was investigated the effect of guanosine, flunarizine and cinnarizine on animal models of psychosis, as well as in other behavioral tasks. Guanosine was chosen because it has been shown to interact with the glutamatergic system – which is known to be involved in the pathop ...
Psilocybin links binocular rivalry switch rate to attention and
... with clinical psychosis (Leonard et al. 2001; Miller et al. 2003; Pettigrew and Miller 1998), drug-induced altered states of consciousness (Carter et al. 2005b; Frecska et al. 2004), and meditation (Carter et al. 2005c). Previous rivalry studies have used functional imaging (Lee et al. 2005; Lumer e ...
... with clinical psychosis (Leonard et al. 2001; Miller et al. 2003; Pettigrew and Miller 1998), drug-induced altered states of consciousness (Carter et al. 2005b; Frecska et al. 2004), and meditation (Carter et al. 2005c). Previous rivalry studies have used functional imaging (Lee et al. 2005; Lumer e ...
A Multifaceted GABAA Receptor Modulator
... insomnia patients than benzodiazepines and barbiturates (Barcelo, 1961; Ionescu-Pioggia et al., 1988). Furthermore, unlike most sedatives, methaqualone is also quite efficacious as an antispasmodic (Gass, 2008). Finally, the euphoria and aphrodisiac properties constituting some of the major psycholo ...
... insomnia patients than benzodiazepines and barbiturates (Barcelo, 1961; Ionescu-Pioggia et al., 1988). Furthermore, unlike most sedatives, methaqualone is also quite efficacious as an antispasmodic (Gass, 2008). Finally, the euphoria and aphrodisiac properties constituting some of the major psycholo ...
An Introduction to Medicinal Chemistry
... distinctly dangerous. Morphine is one such example. It is an excellent analgesic, yet it suffers from the serious side-effects of tolerance, respiratory depression, and addiction. It can even kill if taken in excess. Barbiturates are also known to be dangerous. At Pearl Harbor, American casualties u ...
... distinctly dangerous. Morphine is one such example. It is an excellent analgesic, yet it suffers from the serious side-effects of tolerance, respiratory depression, and addiction. It can even kill if taken in excess. Barbiturates are also known to be dangerous. At Pearl Harbor, American casualties u ...
Endocrine disrupting substances
... Chemical substances may disturb these functions by affecting hormonal signalling. In order to understand how hormonal systems are disturbed it is essential to have knowledge of their natural functions. The report has focused on three hormonal systems, the sex hormones (estrogens, androgens and proge ...
... Chemical substances may disturb these functions by affecting hormonal signalling. In order to understand how hormonal systems are disturbed it is essential to have knowledge of their natural functions. The report has focused on three hormonal systems, the sex hormones (estrogens, androgens and proge ...
Effects of rimonabant on body weight, glucose control
... advanced pharmacological approach targets C1 receptors [32]. There are different possible mechanisms by which CB1 receptor antagonists produce their effects on the CB1 receptor. The ligands can be pure competitive antagonists of CB1 receptor activation by endogenously released ECs (neutral antagonis ...
... advanced pharmacological approach targets C1 receptors [32]. There are different possible mechanisms by which CB1 receptor antagonists produce their effects on the CB1 receptor. The ligands can be pure competitive antagonists of CB1 receptor activation by endogenously released ECs (neutral antagonis ...
Alpha-2 Adrenergic Regulation of Melatonin Release in Chick
... and cyclic nucleotide levels (Zatz et al., 1978). Recent evidence indicates that the classic beta-adrenergic effect in the rat is potentiated by postsynaptic alpha- 1 adrenoceptors (Auerbach et al., 198 1; Sugden and Klein, 1984; Sugden et al., 1984). Combined treatment of pineal glands by both alph ...
... and cyclic nucleotide levels (Zatz et al., 1978). Recent evidence indicates that the classic beta-adrenergic effect in the rat is potentiated by postsynaptic alpha- 1 adrenoceptors (Auerbach et al., 198 1; Sugden and Klein, 1984; Sugden et al., 1984). Combined treatment of pineal glands by both alph ...
Volume 48 Number 4
... The ASPET election for President-Elect, Secretary/Treasurer-Elect, and a Councilor is now open. All Regular and Retired members are eligible to vote. In addition, the following Divisions are holding elections: Division for Drug Discovery, Drug Development & Regulatory Affairs; Division for Drug Meta ...
... The ASPET election for President-Elect, Secretary/Treasurer-Elect, and a Councilor is now open. All Regular and Retired members are eligible to vote. In addition, the following Divisions are holding elections: Division for Drug Discovery, Drug Development & Regulatory Affairs; Division for Drug Meta ...
Antidepressant specificity of serotonin transporter suggested by three LeuT–SSRI structures Zheng Zhou
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
Glucagon Receptor Agonists and Antagonists
... Disclosure: K.A. Vessey, None; K.A. Lencses, None; D.A. Rushforth, None; V.J. Hruby, None; W.K. Stell, None The publication costs of this article were defrayed in part by page charge payment. This article must therefore be marked “advertisement” in accordance with 18 U.S.C. §1734 solely to indicate ...
... Disclosure: K.A. Vessey, None; K.A. Lencses, None; D.A. Rushforth, None; V.J. Hruby, None; W.K. Stell, None The publication costs of this article were defrayed in part by page charge payment. This article must therefore be marked “advertisement” in accordance with 18 U.S.C. §1734 solely to indicate ...
The Serotonin Syndrome - University of Colorado Denver
... serotonergic agonism of central nervous system (CNS) receptors and peripheral serotonergic receptors.1,2 Second, excess serotonin produces a spectrum of clinical findings.3 Third, clinical manifestations of the serotonin syndrome range from barely perceptible to lethal. The death of an 18-year-old p ...
... serotonergic agonism of central nervous system (CNS) receptors and peripheral serotonergic receptors.1,2 Second, excess serotonin produces a spectrum of clinical findings.3 Third, clinical manifestations of the serotonin syndrome range from barely perceptible to lethal. The death of an 18-year-old p ...
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 ...
Butorphanol-Mediated Antinociception in Mice: Partial Agonist
... Clinically, opioids are most commonly used to provide relief of moderate-to-severe pain. The analgesics used for this purpose are predominantly mu agonists, although some effective analgesics possess significant activity at other opioid receptors. A vast number of analogs and congeners have been syn ...
... Clinically, opioids are most commonly used to provide relief of moderate-to-severe pain. The analgesics used for this purpose are predominantly mu agonists, although some effective analgesics possess significant activity at other opioid receptors. A vast number of analogs and congeners have been syn ...
Salvinorin A: A novel and highly selective n
... (Roth et al., 2002; Chavkin et al., 2004). Salvinorin A is the main active ingredient of the hallucinogenic plant Salvia divinorum-a member of the sage family (Valdes et al., 1983; Siebert, 1994). In humans, ingestion of Salvia divinorum via mastication of a quid induces a short-lived experience whi ...
... (Roth et al., 2002; Chavkin et al., 2004). Salvinorin A is the main active ingredient of the hallucinogenic plant Salvia divinorum-a member of the sage family (Valdes et al., 1983; Siebert, 1994). In humans, ingestion of Salvia divinorum via mastication of a quid induces a short-lived experience whi ...
Is there a role for EGFR Tyrosine Kinase Inhibitors in recurrent
... Cohort A will include 32 patients at first recurrence with EGFRVIII mutations. Cohort B will include 32 patients at first recurrence with EGFR gene amplification but no EGFRVIII mutation ...
... Cohort A will include 32 patients at first recurrence with EGFRVIII mutations. Cohort B will include 32 patients at first recurrence with EGFR gene amplification but no EGFRVIII mutation ...
Serotonin 2A Receptors Differentially Contribute to Abuse
... maintained by the unit dose of cocaine that engendered the highest response rates (0.03 mg/kg/infusion). Each round of reinstatement testing consisted of extinguishing the behavior, a reinstatement test day, and subsequently re-establishing stable cocaine self-administration. Behavior was extinguish ...
... maintained by the unit dose of cocaine that engendered the highest response rates (0.03 mg/kg/infusion). Each round of reinstatement testing consisted of extinguishing the behavior, a reinstatement test day, and subsequently re-establishing stable cocaine self-administration. Behavior was extinguish ...
The Serotonin Syndrome - Department of Psychiatry
... serotonergic agonism of central nervous system (CNS) receptors and peripheral serotonergic receptors.1,2 Second, excess serotonin produces a spectrum of clinical findings.3 Third, clinical manifestations of the serotonin syndrome range from barely perceptible to lethal. The death of an 18-year-old p ...
... serotonergic agonism of central nervous system (CNS) receptors and peripheral serotonergic receptors.1,2 Second, excess serotonin produces a spectrum of clinical findings.3 Third, clinical manifestations of the serotonin syndrome range from barely perceptible to lethal. The death of an 18-year-old p ...
Opioid and Cannabinoid Modulation of Precipitated Withdrawal in
... Morphine Sulfate Pellet Implantation. Mice were made dependent to morphine as previously described (Way et al., 1969). Each subject was anesthetized with diethyl ether and a 2-cm lateral incision was made 1 cm posterior to its ears on the midline of its back. The skin was then separated from the mus ...
... Morphine Sulfate Pellet Implantation. Mice were made dependent to morphine as previously described (Way et al., 1969). Each subject was anesthetized with diethyl ether and a 2-cm lateral incision was made 1 cm posterior to its ears on the midline of its back. The skin was then separated from the mus ...
5-HT3 antagonist
The 5-HT3 antagonists, informally known as ""setrons"", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain.With the notable exception of alosetron and cilansetron, which are used in the treatment of irritable bowel syndrome, all 5-HT3 antagonists are antiemetics, used in the prevention and treatment of nausea and vomiting. They are particularly effective in controlling the nausea and vomiting produced by cancer chemotherapy and are considered the gold standard for this purpose.The 5-HT3 antagonists may be identified by the suffix –setron, and are classified under code A04AA of the WHO's Anatomical Therapeutic Chemical Classification System.