Pharmacological Characterization of Nicotine`s Interaction with
... of nicotine’s antinociceptive effect. Their antagonistic potencies are presented in Table 1, and dose-response curves of cocaine and selected analogs are shown in Fig. 2. The latter demonstrates that the antinociceptive effects of nicotine can be completely blocked by these agents. By themselves, th ...
... of nicotine’s antinociceptive effect. Their antagonistic potencies are presented in Table 1, and dose-response curves of cocaine and selected analogs are shown in Fig. 2. The latter demonstrates that the antinociceptive effects of nicotine can be completely blocked by these agents. By themselves, th ...
A New Look at the 5α-Reductase Inhibitor Finasteride
... isozyme is found in prostate, seminal vesicle, epididymis, and hair follicles as well as in liver (140), and is responsible for the remaining two-thirds of circulating DHT. Because of this profile of tissue specific expression and the specificity of finasteride inhibition in humans, few adverse reac ...
... isozyme is found in prostate, seminal vesicle, epididymis, and hair follicles as well as in liver (140), and is responsible for the remaining two-thirds of circulating DHT. Because of this profile of tissue specific expression and the specificity of finasteride inhibition in humans, few adverse reac ...
2.0 Synopsis
... stage and most male subjects (88%) were pubertal stage 3 or higher based on genitalia development at study entry. Mean bone age at baseline was 11.0 years. Bone age was advanced over chronological age by an average of 2.9 and 2.6 years for the leuprolide acetate depot 11.25 mg and 30 mg groups, resp ...
... stage and most male subjects (88%) were pubertal stage 3 or higher based on genitalia development at study entry. Mean bone age at baseline was 11.0 years. Bone age was advanced over chronological age by an average of 2.9 and 2.6 years for the leuprolide acetate depot 11.25 mg and 30 mg groups, resp ...
Drug-induced hypo- and hyperprolactinemia: mechanisms, clinical
... the lactotroph cells [5]. The cholinergic system in the hypophysis, by activation of the muscarinic receptors, exerts a tonic inhibitory action on the prolactin secretion [5,11]. Atropine, the competitive antagonist of muscarinic receptors, induces a dose-dependent increase of the prolactin secretio ...
... the lactotroph cells [5]. The cholinergic system in the hypophysis, by activation of the muscarinic receptors, exerts a tonic inhibitory action on the prolactin secretion [5,11]. Atropine, the competitive antagonist of muscarinic receptors, induces a dose-dependent increase of the prolactin secretio ...
Advances in and applications of proteasome inhibitors
... natural epoxyketone peptides such as epoxomicin (Figure 2) [13] are highly selective, potent and irreversible inhibitors of the proteasome. Numerous peptidyl epoxyketones bearing various chain lengths of acylated di- to tetra-peptides have been characterized from actinomycetes that primarily interac ...
... natural epoxyketone peptides such as epoxomicin (Figure 2) [13] are highly selective, potent and irreversible inhibitors of the proteasome. Numerous peptidyl epoxyketones bearing various chain lengths of acylated di- to tetra-peptides have been characterized from actinomycetes that primarily interac ...
The biochemical effects of ivermectin on reproductive hormones and
... decreased semen parameters and serum testosterone and follicle-stimulating hormone in Red Sokoto buck and serum testosterone in Iraqi Awassi ram, respectively (NAOMAN, 2012). Thus, IVM should be used cautiously in bucks and rams that are meant for breeding due to the deleterious effects observed on ...
... decreased semen parameters and serum testosterone and follicle-stimulating hormone in Red Sokoto buck and serum testosterone in Iraqi Awassi ram, respectively (NAOMAN, 2012). Thus, IVM should be used cautiously in bucks and rams that are meant for breeding due to the deleterious effects observed on ...
Actions of bufalin and cinobufotalin, two bufadienolides respectively
... have been shown to have an effect on ion transport in the amphibia [4]. However, little work has been carried out to compare the activity of the animal bufadienolides in pure form with the cardenolides of plant origin. Studies in recent years have indicated the presence of a substance in animals whi ...
... have been shown to have an effect on ion transport in the amphibia [4]. However, little work has been carried out to compare the activity of the animal bufadienolides in pure form with the cardenolides of plant origin. Studies in recent years have indicated the presence of a substance in animals whi ...
ACRIDINE: A VERSATILE HETEROCYCLIC NUCLEUS
... that new compounds act as more effective antimicrobial agents than the initial preparation ñ ethacridine (35). Giorgio et al. synthesized two new series of diaminoacridinic derivatives (XVII) from proflavine. Two compounds, N-[6-(acetylamino)-3acridinyl]acetamide and N-[6-(benzoylamino)-3acridinyl]b ...
... that new compounds act as more effective antimicrobial agents than the initial preparation ñ ethacridine (35). Giorgio et al. synthesized two new series of diaminoacridinic derivatives (XVII) from proflavine. Two compounds, N-[6-(acetylamino)-3acridinyl]acetamide and N-[6-(benzoylamino)-3acridinyl]b ...
THE ROLE OF PREGNANE X RECEPTOR IN 2-ACETYLAMINOFLUORENE-MEDIATED
... mRNA levels of MRP2 in PXR⫹/⫹ mice, respectively. However, MRP2 levels in PXR⫺/⫺ mice were not altered by 2-AAF. A dosedependent induction of OATP2 mRNA levels was evident ( p ⬍ 0.001) when PXR⫹/⫹ mice were treated with 150 mg/kg (3.4-fold induction) and 300 mg/kg (4.2-fold induction) of 2-AAF. PXR⫺ ...
... mRNA levels of MRP2 in PXR⫹/⫹ mice, respectively. However, MRP2 levels in PXR⫺/⫺ mice were not altered by 2-AAF. A dosedependent induction of OATP2 mRNA levels was evident ( p ⬍ 0.001) when PXR⫹/⫹ mice were treated with 150 mg/kg (3.4-fold induction) and 300 mg/kg (4.2-fold induction) of 2-AAF. PXR⫺ ...
2013 Accomplishments
... initiation of future clinical studies, expectations of expanding ongoing clinical studies, availability and timing of data from ongoing clinical studies, whether interim results from a clinical trial will be predictive of the final results of the trial or results of early clinical studies will be in ...
... initiation of future clinical studies, expectations of expanding ongoing clinical studies, availability and timing of data from ongoing clinical studies, whether interim results from a clinical trial will be predictive of the final results of the trial or results of early clinical studies will be in ...
REVIEWS
... possibly by binding to the two large extracellular domains of this transporter. This binding seems to constitute an essential step in the efflux of phospholipids and cholesterol to apoA-I. In cholesterol-loaded cells, the oxysterol-activated nuclear receptor liver X receptor (LXR), in partnership wi ...
... possibly by binding to the two large extracellular domains of this transporter. This binding seems to constitute an essential step in the efflux of phospholipids and cholesterol to apoA-I. In cholesterol-loaded cells, the oxysterol-activated nuclear receptor liver X receptor (LXR), in partnership wi ...
her2-negative breast cancer – global drug forecast and market
... a Key Area of Interest in Both HR+ and TNBC GlobalData believes that the adjuvant setting will be a highly lucrative market for companies to test their assets. The sheer size of the adjuvant population, and the high number of treatment cycles that can be administered in this setting, are the reasons ...
... a Key Area of Interest in Both HR+ and TNBC GlobalData believes that the adjuvant setting will be a highly lucrative market for companies to test their assets. The sheer size of the adjuvant population, and the high number of treatment cycles that can be administered in this setting, are the reasons ...
A Comparison of Thermodynamic Parameters for Vinorelbine
... Curve fitting of sedimentation velocity data. The distributions of sedimentation coefficients, g(s), were converted to weight average s̄20,w values by integration of the curves (*s * g(s)ds/*g(s)ds) using Origin 3.5 (Microcal Software, Northampton, MA) and correction for temperature and buffer compo ...
... Curve fitting of sedimentation velocity data. The distributions of sedimentation coefficients, g(s), were converted to weight average s̄20,w values by integration of the curves (*s * g(s)ds/*g(s)ds) using Origin 3.5 (Microcal Software, Northampton, MA) and correction for temperature and buffer compo ...
Medical treatments for male and female pattern hair loss
... keratinocytes and reduces the rate at which cells are lost from the germinative pool. This is similar to what has been found with epidermal growth factor. Minoxidil has been shown to increase the proliferation of dermal papilla cells of the human hair follicle.23 Specifically, minoxidil increased le ...
... keratinocytes and reduces the rate at which cells are lost from the germinative pool. This is similar to what has been found with epidermal growth factor. Minoxidil has been shown to increase the proliferation of dermal papilla cells of the human hair follicle.23 Specifically, minoxidil increased le ...
Selective Inhibitors of Picornavirus Replication
... use DAF as an additional receptor.48–50 The use of additional receptors for infection of picornaviruses may have implications for drug therapy, considering that a virus could escape inhibition by a drug that specifically targets one particular receptor, simply by using an alternative receptor. In su ...
... use DAF as an additional receptor.48–50 The use of additional receptors for infection of picornaviruses may have implications for drug therapy, considering that a virus could escape inhibition by a drug that specifically targets one particular receptor, simply by using an alternative receptor. In su ...
avodart - Urological Sciences Research Foundation
... initial development and subsequent enlargement of the prostate gland. Testosterone is converted to DHT by the enzyme 5α-reductase, which exists as 2 isoforms, type 1 and type 2. The type 2 isoenzyme is primarily active in the reproductive tissues while the type 1 isoenzyme is also responsible for te ...
... initial development and subsequent enlargement of the prostate gland. Testosterone is converted to DHT by the enzyme 5α-reductase, which exists as 2 isoforms, type 1 and type 2. The type 2 isoenzyme is primarily active in the reproductive tissues while the type 1 isoenzyme is also responsible for te ...
Reichenbach_final.pd
... and unfavorable pharmacokinetic properties of the natural epothilones. Lactone hydrolysis is the main pathway of epothilone B metabolism in mice [55]; epothilones with a lactone are rapidly metabolized in murine plasma, with halflives of approximately 20 minutes.[56] In dogs, however, the half-life ...
... and unfavorable pharmacokinetic properties of the natural epothilones. Lactone hydrolysis is the main pathway of epothilone B metabolism in mice [55]; epothilones with a lactone are rapidly metabolized in murine plasma, with halflives of approximately 20 minutes.[56] In dogs, however, the half-life ...
Characterization of Two Pharmacophores on the Multidrug
... Service de Biophysique des Fonctions Membranaires, Département de Biologie Joliot Curie (A.G., J.F., M.G., S.O.); Service de Pharmacologie et d’Immunologie, Département de Recherche Médicale (N.L., M.D.), Service de Bioénergétique, Département de Biologie Joliot Curie (F.A.), Commissariat à l ...
... Service de Biophysique des Fonctions Membranaires, Département de Biologie Joliot Curie (A.G., J.F., M.G., S.O.); Service de Pharmacologie et d’Immunologie, Département de Recherche Médicale (N.L., M.D.), Service de Bioénergétique, Département de Biologie Joliot Curie (F.A.), Commissariat à l ...
8 Ultra-low-dose opioid antagonists enhance opioid analgesia while
... opioid treatment can also cause a hyperalgesia, which has also been called opioidinduced hyperalgesia (Li et al., 2001). While patients receiving prolonged opioid analgesic therapy may or may not develop analgesic tolerance, they usually become physically dependent, requiring careful tapering off of ...
... opioid treatment can also cause a hyperalgesia, which has also been called opioidinduced hyperalgesia (Li et al., 2001). While patients receiving prolonged opioid analgesic therapy may or may not develop analgesic tolerance, they usually become physically dependent, requiring careful tapering off of ...
Nicotine
... the same effects. The salts of nicotine are usually dextrorotatory. Pharmacology-Pharmacokinetics: As nicotine enters the body, it is distributed quickly through the bloodstream and can cross the blood-brain barrier. On average it takes about seven seconds for the substance to reach the brain when i ...
... the same effects. The salts of nicotine are usually dextrorotatory. Pharmacology-Pharmacokinetics: As nicotine enters the body, it is distributed quickly through the bloodstream and can cross the blood-brain barrier. On average it takes about seven seconds for the substance to reach the brain when i ...
Asif, M., 2015. Pharmacological activities and
... the traditional use of these plants are discussed. Aegopodium podagraria showed only modest activity. Pure coumarins found in it, angelicin and apterin, failed to show any anti-inflammatory activity, and the total coumarin content was low, therefore the traditional use described in the literature as ...
... the traditional use of these plants are discussed. Aegopodium podagraria showed only modest activity. Pure coumarins found in it, angelicin and apterin, failed to show any anti-inflammatory activity, and the total coumarin content was low, therefore the traditional use described in the literature as ...
Pharmacology of Hemostasis and Thrombosis
... Figure 22-4. Platelet activation by thromboxane A2 . 1. Thromboxane A2 (TxA2 ) is generated from arachidonic acid in activated platelets; cyclooxygenase catalyzes the committed step in this process. 2. Secreted TxA2 binds to the cell surface TxA2 receptor (TxA2-R), a G proteincoupled receptor. 3. Th ...
... Figure 22-4. Platelet activation by thromboxane A2 . 1. Thromboxane A2 (TxA2 ) is generated from arachidonic acid in activated platelets; cyclooxygenase catalyzes the committed step in this process. 2. Secreted TxA2 binds to the cell surface TxA2 receptor (TxA2-R), a G proteincoupled receptor. 3. Th ...
week5
... • Pore domain of all Nav1.1 – Nav1.9 channels are very similar. There are differences in the turret region, which could play important roles in toxin binding. However no templates can be found for modelling the turret regions. • Another target is the voltage sensor. Disabling the voltage sensor of N ...
... • Pore domain of all Nav1.1 – Nav1.9 channels are very similar. There are differences in the turret region, which could play important roles in toxin binding. However no templates can be found for modelling the turret regions. • Another target is the voltage sensor. Disabling the voltage sensor of N ...
Tamsulosin and dry mouth Introduction Reports
... which was not reported disproportionally. The Reporting Odds Ratio (ROR) is 1.3 (95% CI 0.6-3.0). Furthermore, the Lareb database contained two reports of dry mouth for doxazosin, one report for silodosin and one report for terazosin. The WHO database of the Uppsala Monitoring Centre contained 77 re ...
... which was not reported disproportionally. The Reporting Odds Ratio (ROR) is 1.3 (95% CI 0.6-3.0). Furthermore, the Lareb database contained two reports of dry mouth for doxazosin, one report for silodosin and one report for terazosin. The WHO database of the Uppsala Monitoring Centre contained 77 re ...
Discovery and development of antiandrogens
In the 1960s, the first antiandrogen, or androgen antagonist, was discovered. Antiandrogens antagonise the androgen receptor (AR) and thereby block the biological effects of testosterone and dihydrotestosterone (DHT). Antiandrogens are important for men with hormonally responsive diseases like prostate cancer, benign prostatic hyperplasia (BHP), acne, seborrhea, hirsutism and androgen alopecia. Antiandrogens are mainly used for the treatment of prostate diseases. Research from 2010 suggests that ARs could be linked to the disease progression of triple-negative breast cancer and that antiandrogens can potentially be used to treat it.As of 2010 antiandrogens are small molecules and can be either steroidal or nonsteroidal depending on ligand chemistry. Steroidal antiandrogens share a similar steroid structure, while nonsteroidal antiandrogens may have structurally distinctive pharmacophores. Only a limited number of compounds are available for clinical use despite the fact that a very large variety of antiandrogen compounds have been discovered and researched.