Cinanserin: A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive activity.Quipazine: A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.Methysergide: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.Tablets: Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)Therapeutic Equivalency: The relative equivalency in the efficacy of different modes of treatment of a disease, most often used to compare the efficacy of different pharmaceuticals to treat a given disease.Love: Affection; in psychiatry commonly refers to pleasure, particularly as it applies to gratifying experiences between individuals.Academic Medical Centers: Medical complexes consisting of medical school, hospitals, clinics, libraries, administrative facilities, etc.Administration, Oral: The giving of drugs, chemicals, or other substances by mouth.Aphids: A family (Aphididae) of small insects, in the suborder Sternorrhyncha, that suck the juices of plants. Important genera include Schizaphis and Myzus. The latter is known to carry more than 100 virus diseases between plants.Taraxacum: A plant genus of the family ASTERACEAE. Members contain chicoric and chlorogenic acids and germacrane- and eudesmane-type SESQUITERPENES.Urtica dioica: A plant species of the genus Urtica, family URTICACEAE. Roots have been used to treat PROSTATIC HYPERPLASIA. Leaves are edible after the stinging quality is eliminated by brief heating.Caesalpinia: A plant genus of the family FABACEAE. The common name of "Bird-Of-Paradise" is also used for other plants such as Heliconia (HELICONIACEAE) and Strelitzia (STRELITZIACEAE) and some birds. The common name of "Cat's-Claw" is more often used with UNCARIA. The common name of "Pernambuco" also refers to a state in Brazil. Furanoditerpenoid lactones and caesalpin are produced by members of this genus.Dengue Virus: A species of the genus FLAVIVIRUS which causes an acute febrile and sometimes hemorrhagic disease in man. Dengue is mosquito-borne and four serotypes are known.Ginger: Deciduous plant rich in volatile oil (OILS, VOLATILE). It is used as a flavoring agent and has many other uses both internally and topically.Dengue: An acute febrile disease transmitted by the bite of AEDES mosquitoes infected with DENGUE VIRUS. It is self-limiting and characterized by fever, myalgia, headache, and rash. SEVERE DENGUE is a more virulent form of dengue.Inhibitory Concentration 50: The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.Aplysia: An opisthobranch mollusk of the order Anaspidea. It is used frequently in studies of nervous system development because of its large identifiable neurons. Aplysiatoxin and its derivatives are not biosynthesized by Aplysia, but acquired by ingestion of Lyngbya (seaweed) species.Ganglia: Clusters of multipolar neurons surrounded by a capsule of loosely organized CONNECTIVE TISSUE located outside the CENTRAL NERVOUS SYSTEM.Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Waxes: A plastic substance deposited by insects or obtained from plants. Waxes are esters of various fatty acids with higher, usually monohydric alcohols. The wax of pharmacy is principally yellow wax (beeswax), the material of which honeycomb is made. It consists chiefly of cerotic acid and myricin and is used in making ointments, cerates, etc. (Dorland, 27th ed)Magnesium: A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.Bathing Beaches: Beaches, both natural and man-made, used for bathing and other activities.Ganglia, Invertebrate: Clusters of neuronal cell bodies in invertebrates. Invertebrate ganglia may also contain neuronal processes and non-neuronal supporting cells. Many invertebrate ganglia are favorable subjects for research because they have small numbers of functional neuronal types which can be identified from one animal to another.Nephropidae: Family of large marine CRUSTACEA, in the order DECAPODA. These are called clawed lobsters because they bear pincers on the first three pairs of legs. The American lobster and Cape lobster in the genus Homarus are commonly used for food.Brachyura: An infraorder of chiefly marine, largely carnivorous CRUSTACEA, in the order DECAPODA, including the genera Cancer, Uca, and Callinectes.Pylorus: The region of the STOMACH at the junction with the DUODENUM. It is marked by the thickening of circular muscle layers forming the pyloric sphincter to control the opening and closure of the lumen.Interneurons: Most generally any NEURONS which are not motor or sensory. Interneurons may also refer to neurons whose AXONS remain within a particular brain region in contrast to projection neurons, which have axons projecting to other brain regions.Neurons: The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.Periodicity: The tendency of a phenomenon to recur at regular intervals; in biological systems, the recurrence of certain activities (including hormonal, cellular, neural) may be annual, seasonal, monthly, daily, or more frequently (ultradian).Lysergic Acid Diethylamide: Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Methoxydimethyltryptamines: Compounds that contain the biogenic monoamine tryptamine and are substituted with one methoxy group and two methyl groups. Members of this group include several potent serotonergic hallucinogens found in several unrelated plants, skins of certain toads, and in mammalian brains. They are possibly involved in the etiology of schizophrenia.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Bufotenin: A hallucinogenic serotonin analog found in frog or toad skins, mushrooms, higher plants, and mammals, especially in the brains, plasma, and urine of schizophrenics. Bufotenin has been used as a tool in CNS studies and misused as a psychedelic.Lysergic AcidAdenylate Cyclase Toxin: One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.Thrombin: An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN.Antithrombins: Endogenous factors and drugs that directly inhibit the action of THROMBIN, usually by blocking its enzymatic activity. They are distinguished from INDIRECT THROMBIN INHIBITORS, such as HEPARIN, which act by enhancing the inhibitory effects of antithrombins.Pipecolic AcidsHirudins: Single-chain polypeptides of about 65 amino acids (7 kDa) from LEECHES that have a neutral hydrophobic N terminus, an acidic hydrophilic C terminus, and a compact, hydrophobic core region. Recombinant hirudins lack tyr-63 sulfation and are referred to as 'desulfato-hirudins'. They form a stable non-covalent complex with ALPHA-THROMBIN, thereby abolishing its ability to cleave FIBRINOGEN.HSP40 Heat-Shock Proteins: A family of heat-shock proteins that contain a 70 amino-acid consensus sequence known as the J domain. The J domain of HSP40 heat shock proteins interacts with HSP70 HEAT-SHOCK PROTEINS. HSP40 heat-shock proteins play a role in regulating the ADENOSINE TRIPHOSPHATASES activity of HSP70 heat-shock proteins.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Hirudin Therapy: Use of HIRUDINS as an anticoagulant in the treatment of cardiological and hematological disorders.Bibliography as Topic: Discussion of lists of works, documents or other publications, usually with some relationship between them, e.g., by a given author, on a given subject, or published in a given place, and differing from a catalog in that its contents are restricted to holdings of a single collection, library, or group of libraries. (from The ALA Glossary of Library and Information Science, 1983)Bibliography of Medicine: A list of works, documents, and other publications on medical subjects and topics of interest to the field of medicine.Isoantigens: Antigens that exist in alternative (allelic) forms in a single species. When an isoantigen is encountered by species members who lack it, an immune response is induced. Typical isoantigens are the BLOOD GROUP ANTIGENS.MississippiBibliographyFerritins: Iron-containing proteins that are widely distributed in animals, plants, and microorganisms. Their major function is to store IRON in a nontoxic bioavailable form. Each ferritin molecule consists of ferric iron in a hollow protein shell (APOFERRITINS) made of 24 subunits of various sequences depending on the species and tissue types.Histocompatibility Antigens: A group of antigens that includes both the major and minor histocompatibility antigens. The former are genetically determined by the major histocompatibility complex. They determine tissue type for transplantation and cause allograft rejections. The latter are systems of allelic alloantigens that can cause weak transplant rejection.

Evidence for a role for central 5-HT2B as well as 5-HT2A receptors in cardiovascular regulation in anaesthetized rats. (1/28)

1. The effects of injections i.c.v. of quipazine, (2 micromol kg-1) and 1-(2,5-di-methoxy-4-iodophenyl)-2-aminopropane (DOI; 2 micromol kg-1) on renal sympathetic and phrenic nerve activity, mean arterial blood pressure (MAP) and heart rate were investigated in alpha-chloralose anaesthetized rats pretreated with a peripherally acting 5-HT2 receptor antagonist. 2. Quipazine or DOI caused a rise in MAP which was associated with a tachycardia and renal sympathoinhibition in rats pretreated (i.c.v.) with the antagonist vehicle 10% PEG. These effects of quipazine were completely blocked by pretreatment with cinanserin (a 5-HT2 receptor antagonist) and attenuated by spiperone (a 5-HT2A receptor antagonist). However, pretreatment with SB200646A (a 5-HT2B/2C receptor antagonist) only blocked the sympathoinhibition, while pretreatment with SB204741 (a 5-HT2B receptor antagonist) reversed the sympathoinhibition to excitation as it also did for DOI. Quipazine also caused renal sympathoexcitation in the presence (i.v.) of a vasopressin V1 receptor antagonist. 3. Injection (i.v.) of the V1 receptor antagonist at the peak pressor response evoked by quipazine alone and in the presence of SB204741 caused an immediate fall in MAP. For quipazine alone the renal sympathoinhibition was slowly reversed to an excitation, while the renal sympathoexcitation observed in the presence of SB204741 was potentiated. In both, the quipazine-evoked tachycardia was unaffected. 4. The data indicate that cardiovascular responses caused by i.c.v. quipazine and DOI are primarily due to activation of central 5-HT2A receptors, which causes the release of vasopressin and a tachycardia. This released vasopressin appears to suppress a 5-HT2A receptor-evoked central increase in sympathetic outflow, which involves the activation of central 5-HT2B receptors indirectly by the released vasopressin.  (+info)

Serotonin and NO complementarily regulate generation of oscillatory activity in the olfactory CNS of a terrestrial mollusk. (2/28)

Synchronous oscillation of membrane potentials, generated by assemblies of neurons, is a prominent feature in the olfactory systems of many vertebrate and invertebrate species. However, its generation mechanism is still controversial. Biogenic amines play important roles for mammalian olfactory learning and are also implicated in molluscan olfactory learning. Here, we investigated the role of serotonin, a biogenic amine, in the oscillatory dynamics in the procerebrum (PC), the molluscan olfactory center. Serotonin receptor blockers inhibited the spontaneous synchronous oscillatory activity of low frequency (approximately 0.5 Hz) in the PC. This was due to diminishing the periodic slow oscillation of membrane potential in bursting (B) neurons, which are essential neuronal elements for the synchronous oscillation in the PC. On the other hand, serotonin enhanced the amplitude of the slow oscillation in B neurons and subsequently increased the number of spikes in each oscillatory cycle. These results show that the extracellular serotonin level regulates the oscillation amplitude in B neurons and thus serotonin may be called an oscillation generator in the PC. Although nitric oxide (NO) is known to also be a crucial factor for generating the PC oscillatory activity and setting the PC oscillation frequency, the present study showed that NO only regulates the oscillation frequency in B neurons but could not increase the spikes in each oscillatory cycle. These results suggest complementary regulation of the PC oscillatory activity: NO determines the probability of occurrence of slow potentials in B neurons, whereas serotonin regulates the amplitude in each cycle of the oscillatory activity in B neurons.  (+info)

Quantification of serotonin transporters in nonhuman primates using [(123)I]ADAM and SPECT. (3/28)

We reported recently a highly selective radioligand, 2-([2-([dimethylamino]methyl)phenyl]thio)-5-[(123)I]iodophenylamine (ADAM), for SPECT imaging of serotonin transporters (SERT). In this article we describe the kinetic modeling of [(123)I]ADAM and its ability to quantitatively and reproducibly measure the concentrations of SERT in the nonhuman primate brain. We also investigate simplified models of tracer behavior that do not require invasive arterial blood sampling. METHODS: Three female baboons each underwent 3 [(123)I]ADAM SPECT studies. The studies consisted of a dynamic sequence of seventy-two 5-min scans after injection of 330 +/- 50 MBq (mean +/- SD) [(123)I]ADAM. Rapid arterial blood samples were obtained and corrected for the presence of labeled metabolites. Dynamic imaging and metabolite-corrected plasma data were analyzed using graphic analysis to give the distribution volumes (DVs) of different brain regions. DV ratios (DVRs) of target to cerebellum were derived and compared against a kinetic reference tissue model and simple target-to-background ratio. RESULTS: Averaged over all 9 scans, the mean DV in the midbrain was 4.86 +/- 1.06 mL/mL and the mean DV in the cerebellum was 2.25 +/- 0.48 mL/mL. The mean test-retest repeatability of the midbrain DV was 14.5%. The reference tissue model gave a mean midbrain DVR of 2.01 +/- 0.17 and correlated strongly with the DVR calculated from the full kinetic model (correlation coefficient [R(2)] = 0.94; P < 0.001), but with much improved repeatability (test-retest, 5.4%; intersubject variability, 5.2%). Similarly, the simple ratio method gave strong correlations with the full kinetic model (R(2) = 0.89; P < 0.001) and a test-retest of 7.6%. CONCLUSION: Accurate, repeatable quantification of SERT in the nonhuman primate brain is possible using kinetic modeling of dynamic [(123)I]ADAM SPECT scans. Simplified models, which do not require arterial blood sampling, gave accurate results that correlated strongly with the full kinetic model. The test-retest reliability of the simplified reference region models was excellent. Quantification of SERT is possible using full kinetic modeling and also with simpler reference region methods.  (+info)

Specific binding sites for 5-hydroxytryptamine on rat blood platelets. (4/28)

5-Hydroxytryptamine changes the shape of rat blood platelets by combination with a cinanserin-sensitive receptor which is not associated with the active uptake of 5-hydroxytryptamine. Binding of 5-hydroxy[3H]tryptamine to platelets at 4 degrees C demonstrates the presence of three saturable sites, and the highest-affinity site is apparently this 5-hydroxytryptamine receptor.  (+info)

Serotonergic control of cerebellar mossy fiber activity by modulation of signal transfer by rat pontine nuclei neurons. (5/28)

Serotonergic modulation of precerebellar nuclei may be crucial for the function of the entire cerebellar system. To study the effects of serotonin (5-HT) on neurons located within the pontine nuclei (PN), the main source of cerebellar mossy fibers, we performed standard intracellular recordings from PN neurons in a slice preparation of the rat pontine brain stem. Application of 5 microM 5-HT significantly altered several intrinsic membrane properties of PN neurons. First, it depolarized the somatic membrane potential by 6.5 +/- 3.5 mV and increased the apparent input resistance from 49.5 +/- 14.6 to 62.7 +/- 21.1 MOmega. Second, 5-HT altered the I-V relationship of PN neurons: it decreased the inward rectification in hyperpolarizing direction, but increased it when depolarizing currents were applied. Third, it decreased the rheobase from 0.32 +/- 0.14 to 0.24 +/- 0.14 nA without affecting the firing threshold. Finally, the amplitude of medium-duration after hyperpolarizations was reduced from -14.9 +/- 2.0 to -12.3 +/- 2.4 mV. Together, these 5-HT effects on the intrinsic membrane properties result in an increase in excitability and instantaneous firing rate. In addition, application of 5 microM 5-HT also modulated postsynaptic potentials (PSPs) evoked by electric stimulations within the cerebral peduncle. The amplitude, maximal slope, and integral of these PSPs were reduced to 46.2 +/- 23.4%, 45.7 +/- 23.7%, and 61.4 +/- 28.4% of the control value, respectively. In contrast, we found no change in the decay and voltage dependence of PSPs. To test modulatory effects on short-term synaptic facilitation, we applied pairs of electrical stimuli at intervals between 10 and 1,000 ms. 5-HT selectively enhanced the paired-pulse facilitation for interstimulus-intervals >20 ms. The alteration of paired-pulse facilitation points to a presynaptic site of action for 5-HT effects on synaptic transmission. Pharmacological experiments suggested that pre- and postsynaptic effects of 5-HT were mediated by two different kinds of 5-HT receptors: changes in intrinsic membrane properties were blocked by the 5-HT(2) receptor antagonist cinanserin while the reduction of PSPs was prevented by the 5-HT(1) receptor antagonist cyanopindolol. In conclusion, 5-HT increases the excitability of PN neurons but decreases the synaptic transmission on them. The selective enhancement of synaptic facilitation may, however, allow high-frequency inputs to effectively drive PN neurons, thus the PN may act as a high-pass filter during periods of 5-HT release.  (+info)

Characterization of the binding sites for 123I-ADAM and the relationship to the serotonin transporter in rat and mouse brains using quantitative autoradiography. (6/28)

Imaging of serotonin transporter (SERT) in the central nervous system may provide an important tool to evaluate some psychiatric disorders. Recently, a novel (123)I-labeled radiotracer, 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine ((123)I-ADAM), has been developed that exhibited a high selectivity for SERT. The aim of this study was to characterize the biodistribution and specificity of (123)I-ADAM to SERT using quantitative autoradiography in both control and neurotoxin-treated animals. METHODS: (123)I-ADAM (74 MBq) was injected intravenously into the mice to access its biodistribution in the brain via quantitative autoradiography. Further, rats with serotonin depleted by intraperitoneal injection of p-chloroamphetamine (PCA) were used to evaluate the specificity of (123)I-ADAM to SERT. The levels of biogenic amines were then measured and correlated with quantitative (123)I-ADAM labeling in control and PCA-treated rat brains. RESULTS: The autoradiographic results showed that (123)I-ADAM accumulated in SERT-rich brain areas after systemic injection, including the globus pallidus, thalamus, hypothalamus, substantia nigra, interpeduncular nucleus, amygdala, and raphe nucleus. The dorsal raphe nucleus had the highest initial uptake with a peak specific binding ratio (i.e., [target - cerebellum]/cerebellum) at 120 min after injection. (123)I-ADAM uptake was dramatically decreased in the hippocampus, thalamus, amygdala, geniculate nuclei, hypothalamus, raphe nucleus, and substantia nigra in PCA-lesioned rats. The decrement in radioactivity was more prominent at higher dosages of PCA and was in parallel with the changes in amounts of serotonin and 5-hydroxyindoleacetic acid in the prefrontal cortex. CONCLUSION: This study demonstrates that regional distribution of (123)I-ADAM radioactivity is similar to the SERT localization in both rat and mouse brains. We also validated that destruction on central serotonergic neurons after PCA treatment inhibits the uptake of (123)I-ADAM in serotonin-rich brain regions. High specific binding to SERT in vivo makes (123)I-ADAM an appropriate radiotracer for solitary studies of serotonin functions in living humans.  (+info)

Biodistribution and imaging with (123)I-ADAM: a serotonin transporter imaging agent. (7/28)

2-((2-((Dimethylamino)methyl)phenyl)thio)-5-(123)I-iodophenylamine ((123)I-ADAM) is a new radiopharmaceutical that selectively binds the central nervous system serotonin transporters. The purpose of this study was to measure its whole-body biokinetics and estimate its radiation dosimetry in healthy human volunteers. The study was conducted within a regulatory framework that required its pharmacologic safety to be assessed simultaneously. METHODS: The sample included 7 subjects ranging in age from 22 to 54 y old. An average of 12.7 whole-body scans were acquired sequentially on a dual-head camera for up to 50 h after the intravenous administration of 185 MBq (5 mCi) (123)I-ADAM. The fraction of the administered dose in 13 regions of interest (ROIs) was quantified from the attenuation-corrected geometric mean counts in conjugate views. Multiexponential functions were iteratively fit to each time-activity curve using a nonlinear, least-squares regression algorithm. These curves were numerically integrated to yield source organ residence times. Gender-specific radiation doses were then estimated with the MIRD technique. SPECT brain scans obtained 3 h after injection were evaluated using an ROI analysis to determine the range of values for the region to cerebellum. RESULTS: There were no pharmacologic effects of the radiotracer on any of the subjects, including no change in heart rate, blood pressure, or laboratory results. Early planar images showed differentially increased activity in the lungs. SPECT images demonstrated that the radiopharmaceutical localized in the midbrain in a distribution that is consistent with selective transporter binding. The dose-limiting organ in both men and women was the distal colon, which received an average of 0.12 mGy/MBq (0.43 rad/mCi) (range, 0.098-0.15 mGy/MBq). The effective dose equivalent and effective dose for (123)I-ADAM were 0.037 +/- 0.003 mSv/MBq and 0.036 +/- 0.003 mSv/MBq, respectively. The mean adult male value of effective dose for (123)I-ADAM is similar in magnitude to that of (111)In-diethylenetriaminepentaacetic acid (0.035 mGy/MBq), half that of (111)In-pentetreotide (0.81 mGy/MBq), and approximately twice that of (123)I-inosine 5'-monophosphate (0.018 mGy/MBq). The differences in results between this study and a previous publication are most likely due to several factors, the most prominent being this dataset used attenuation correction of the scintigraphic data. Region-to-cerebellum ratios for the brain SPECT scans were 1.95 +/- 0.13 for the midbrain, 1.27 +/- 0.10 for the medial temporal regions, and 1.11 +/- 0.07 for the striatum. CONCLUSION: (123)I-ADAM may be a safe and effective radiotracer for imaging serotonin transporters in the brain and the body.  (+info)

Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro. (8/28)

The 3C-like proteinase (3CLpro) of severe acute respiratory syndrome-associated coronavirus (SARS-CoV) is one of the most promising targets for anti-SARS-CoV drugs due to its crucial role in the viral life cycle. In this study, a database containing structural information of more than 8,000 existing drugs was virtually screened by a docking approach to identify potential binding molecules of SARS-CoV 3CLpro. As a target for screening, both a homology model and the crystallographic structure of the binding pocket of the enzyme were used. Cinanserin (SQ 10,643), a well-characterized serotonin antagonist that has undergone preliminary clinical testing in humans in the 1960s, showed a high score in the screening and was chosen for further experimental evaluation. Binding of both cinanserin and its hydrochloride to bacterially expressed 3CLpro of SARS-CoV and the related human coronavirus 229E (HCoV-229E) was demonstrated by surface plasmon resonance technology. The catalytic activity of both enzymes was inhibited with 50% inhibitory concentration (IC50) values of 5 microM, as tested with a fluorogenic substrate. The antiviral activity of cinanserin was further evaluated in tissue culture assays, namely, a replicon system based on HCoV-229E and quantitative test assays with infectious SARS-CoV and HCoV-229E. All assays revealed a strong inhibition of coronavirus replication at nontoxic drug concentrations. The level of virus RNA and infectious particles was reduced by up to 4 log units, with IC50 values ranging from 19 to 34 microM. These findings demonstrate that the old drug cinanserin is an inhibitor of SARS-CoV replication, acting most likely via inhibition of the 3CL proteinase.  (+info)

*Cinanserin

... (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. The preparation is effective ...

*5-HT2C receptor

Cinanserin Deramciclane Ketanserin LY-53,857 Metergoline Methiothepin Pizotifen Ritanserin S-32212 SB-206,553 SB-228,357 SB- ...

*List of MeSH codes (D02)

... cinanserin MeSH D02.241.223.201.210 --- coumaric acids MeSH D02.241.223.201.711 --- puromycin MeSH D02.241.223.201.711.650 --- ...

*List of drugs: Ci

... cinanserin (INN) cinaproxen (INN) cinchocaine (INN) cinchophen (INN) cinecromen (INN) cinepaxadil (INN) cinepazet (INN) ...
In the current study, we sought to study SERT binding properties in the midbrain region in patients with epilepsy, and to determine whether SERT binding differed between depressed vs. non-depressed patients with epilepsy. Our results did not indicate any difference in SERT binding potential between these patient groups.. There could be several reasons for these negative results. Previous work with PET and SPET tracers for SERT in depressed patients has shown some conflicting results. The majority of reports show increased SERT binding in the thalamus and limbic regions of depressed patients compared to controls [30], but others have shown decreased SERT binding potential in the amygdala and midbrain of depressed patients [13-15]. Studies using 123I-ADAM SPET to measure SERT binding in major depressive disorder have also indicated decreased SERT binding in the midbrain, medial temporal lobe, and basal ganglia of depressed patients compared to controls [26, 27]. At the same time, however, reports ...
Early post-mortem data suggest that damage to brain serotonin neurones might play a role in some features (e.g., depression) of Parkinsons disease (PD). However, it is not known whether such damage is a typical characteristic of living patients with PD or whether the changes are regionally widespread. To address this question we measured, by positron emission tomography imaging, levels of the brain serotonin transporter (SERT), a marker for serotonin neurones, as inferred from binding of [11C]-3-amino-4-(2-dimethylaminomethyl-phenylsulfanyl)-benzonitrile (DASB), a second generation SERT radioligand, in subcortical and cerebral cortical brain areas of clinically advanced non-depressed (confirmed by structured psychiatric interview) patients with PD. SERT binding levels in PD were lower than those in controls in all examined brain areas, with the changes statistically significant in orbitofrontal cortex (−22%), caudate (−30%), putamen (−26%), and midbrain (−29%). However, only a slight ...
This thesis describes studies on the effects of obesity, weight loss and meal timing on the human brain and glucose metabolism. We investigated effects of meal timing during a hypocaloric diet and weight loss on brain serotonin transporters (SERT) and dopamine transporters (DAT), neuronal activity patterns and metabolism. In addition, we studied the effect of bright light conditions on glucose and lipid metabolism in lean and obese subjects with type 2 diabetes (T2D). First, we show a trend towards lower hypothalamic SERT binding in obese compared to lean controls and a reduced SERT binding in the diencephalon in obese insulin resistant compared to equally obese insulin sensitive and lean subjects. Second, we show that subjects who consumed most of the calories in the morning during a hypocaloric diet, increased striatal DAT binding and reduced neuronal activation in response to high calorie food pictures in the caudate nucleus, while consuming most of the calories in the evening reduced ...
Comley, R. A., Miller, S., Murthy, V., Bhagwagar, Z., Turner, D., Peers, P., ... Rabiner, E. (2010). Association between serotonin transporter binding, physiological and environmental factors in healthy male subjects. S93-S94. Poster session presented at The Eighth International Symposium on Functional Neuroreceptor Mapping of the Living Brain - NRM 2010, . https://doi.org/10.1016/j.neuroimage.2010.04.075 ...
CAS NO:67751-23-9; Chemical name:4-(dimethylamino)-1,1-dimethoxybut-3-en-2-one ; physical and chemical property of 67751-23-9, 4-(dimethylamino)-1,1-dimethoxybut-3-en-2-one is provided by ChemNet.com
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2-(4-chlorophenyl)-2-(dimethylamino)acetamide - chemical structural formula, chemical names, chemical properties, synthesis references
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Mc Mahon B, Andersen SB, Madsen MK, Hjordt LV, Hageman I, Dam H, et al. Seasonal difference in brain serotonin transporter binding predicts symptom severity in patients with seasonal affective disorder. Brain : a journal of neurology. 2016.. Knudsen GM, Jensen PS, Erritzoe D, Baare WF, Ettrup A, Fisher PM, et al. The Center for Integrated Molecular Brain Imaging (Cimbi) database. NeuroImage. 2016;124(Pt B):1213-9.. Angstmann S, Madsen KS, Skimminge A, Jernigan TL, Baare WF, Siebner HR. Microstructural asymmetry of the corticospinal tracts predicts right-left differences in circle drawing skill in right-handed adolescents. Brain structure & function. 2016.. Schmock H, Vangkilde A, Larsen KM, Fischer E, Birknow MR, Jepsen JR, et al. The Danish 22q11 research initiative. BMC psychiatry. 2015;15:220.. Holm SK, Vestergaard M, Madsen KS, Baare WF, Hammer TB, Born AP, et al. Children and adolescents previously treated with glucocorticoids display lower verbal intellectual abilities. Acta paediatrica ...
Geodermatophilus obscurus ATCC ® 25078D-5™ Designation: Genomic DNA from Geodermatophilus obscurus strain D-20 TypeStrain=True Application:
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You are viewing an interactive 3D depiction of the molecule 4-(dimethylamino)-3-methyl-1,2-diphenyl-1-butanol (C19H25NO) from the PQR.
Disturbances in serotonergic neurotransmission have been suggested to be closely interlinked with hyperactivity of the hypothalamic-pituitary-adrenocortical (HPA) system, and are likely to be involved in the pathophysiology of anxiety disorders and major depression. We therefore investigated markers of serotonergic transmission and their modulation by chronic paroxetine in rats selectively bred for high (HAB) or low (LAB) anxiety-related behaviour, both under basal conditions and in response to emotional stress. Hippocampal serotonin 1 A (5-HT1A) receptor mRNA expression was reduced in HAB rats, whereas 5-HT concentrations in hippocampal microdialysates did not differ between HAB and LAB rats under basal conditions. In the hippocampus, overall expression of serotonin transporter binding sites was increased in HAB compared with LAB rats. Exposure to emotional stress failed to increase intrahippocampal 5-HT release in HAB rats whereas LAB rats displayed a physiological, albeit small rise. Chronic ...
Fozard J.R., 1983: Failure of 5 methoxy tryptamine to evoke the bezold jarisch effect supports homology of excitatory 5 hydroxy tryptamine receptors on vagal afferents and postganglionic sympathetic neurons
With extracellular matrix (ECM) being part of all our bodys tissues, it is crucial to mimic its properties when developing 3D tissue models in vitro. For this purpose, a variety of 3D matrices are available. Here we describe their use in 3D organ-on-a-chip models.
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2-[[4-(dimethylamino)benzyl](methyl)amino]ethanol - chemical structural formula, chemical names, chemical properties, synthesis references
3-[(Dimethylamino)methyl]phenol | C9H13NO | CID 32896 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
1-(Dimethylamino)pyrrole | C6H10N2 | CID 573527 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Tetracaine 2-Dimethylamino) p-butylaminobenzoate; 2-dimethylaminoethylphenol-2-Dimethylamino-p-butylaminobenzoate; 2- (Dimethylamino) (Butylamino) -benzoicaci2- (dimethylamino) ethylester; amethocaine; Anetain CAS: 94-24-6 MF: C15H24N2O2 MW: 264.36...
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What is the difference? Is tryptose a sugar and tryptamine just the tryp base unit with an amine atached to it? Why do they both begin with Tryp?
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This approach is based on the principle of delaying the release of the drug until it enters into the colon. Although gastric emptying tends to be highly variable, small intestinal transit time is relatively constant or little bit variation can be observed. The strategy in designing timed-released systems is to resist the acidic environment of the stomach and to undergo a lag time of predetermined span of time, after which release of drug take place. The lag time in this case is the time requires to transit from the mouth to colon. The first formulation introduced based on this principle was Pulsincap® (196). It is similar in appearance to hard gelatin capsule; the main body is made water insoluble (exposing the body to formaldehyde vapour which may be produced by the addition of trioxymethylene tablets or potassium permanganate to formalin or any other method). The contents are contained within a body by a hydrogel plug, which is covered by a water-soluble cap. The whole unit is coated with an ...
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2-Naphthacenecarboxamide,7-chloro-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,4a,10,12,12a-pentahydroxy-8-methoxy-6-methyl-1,11-dioxo-6-[[2,3,6-trideoxy-3-(hydroxyamino)-3-C-methyl-4-O-methyl-a-L-arabino-hexopyranosyl]oxy]-,[4R-(4a,4aa,5aa,6a,12aa)]- (9CI ...
O-Desmethyl Venlafaxine S-Isomer ;. Desvenlafaxine S-Isomer ;. (S)-4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl) ethyl]phenol ;. CAS # 142761-12-4 ;. C16H25NO2 ;. MW: 263.38 ;. ...
O-Desmethyl Venlafaxine R-Isomer ;. Desvenlafaxine R-Isomer ;. (R)-4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl) ethyl]phenol ; CAS # 142761-11-3 ;. C16H25NO2 ;. MW: 263.38 ;. ...

Cinanserin - WikipediaCinanserin - Wikipedia

Cinanserin (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. The preparation is effective ...
more infohttps://en.wikipedia.org/wiki/Cinanserin

Cinanserin May Offer New Hope in Treating SARSCinanserin May Offer New Hope in Treating SARS

RxPG] Cinanserin, a drug that underwent preliminary clinical testing on humans in the 1960s, may inhibit the SARS virus say ... Cinanserin May Offer New Hope in Treating SARS. Jun 20, 2005 - 4:08:00 PM ... Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces ... Cinanserin, a well-characterized serotonin antagonist, scored high in the screening and was selected for further ...
more infohttp://www.rxpgnews.com/severeacuterespiratorysyndrome-sars/Cinanserin_May_Offer_New_Hope_in_Treating_SARS_1736_1736.shtml

Cinanserin - Alfa ChemistryCinanserin - Alfa Chemistry

Cinanserin/AFI1166343 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and ...
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Drug Information Portal - Mobile - U.S. National Library of Medicine - Drug Search ResultsDrug Information Portal - Mobile - U.S. National Library of Medicine - Drug Search Results

Cinanserin [INN] Description: A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive ...
more infohttps://druginfo.nlm.nih.gov/m.drugportal/rn/1166-34-3

Drug Information Portal - U.S. National Library of Medicine - Quick Access to Quality Drug InformationDrug Information Portal - U.S. National Library of Medicine - Quick Access to Quality Drug Information

Cinanserin [INN] View Synonyms. View Structure. Description:. A serotonin antagonist with limited antihistaminic, ...
more infohttps://druginfo.nlm.nih.gov/drugportal/rn/1166-34-3

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11202572:Cinanserin Is an Inhibitor of the 3C-Like Proteina. *11202573:Deletion of M2 Gene Open Reading Frames 1 and 2 of ...
more infohttp://www.100md.com/index/other/byinfono/022/406.htm

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Design and Synthesis of Cinanserin Analogs as Severe Acute Respiratory Syndrome Coronavirus 3CL Protease Inhibitors Qingang ...
more infohttp://mol.medicalonline.jp/archive/search?jo=cs7chemi&ye=2008&vo=56&issue=10

Effect of Hallucinogens on Unconditioned Behavior | SpringerLinkEffect of Hallucinogens on Unconditioned Behavior | SpringerLink

... by cinanserin. Can J Physiol Pharmacol 51:976-980PubMedCrossRefGoogle Scholar ...
more infohttps://link.springer.com/chapter/10.1007/7854_2016_466

oxatomide - meddicoxatomide - meddic

Cinanserin. *Cyproheptadine. *Deramciclane. *Dotarizine. *Eltoprazine. *Ergolines (e.g., amesergide, bromocriptine, LY-53857, ...
more infohttps://meddic.jp/oxatomide

Cyproheptadine 4 mg tablet ivx / Revista pronto españa 2015Cyproheptadine 4 mg tablet ivx / Revista pronto españa 2015

Adatanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine.. All-Night Herbal Viagra Tablets. . macular edema; ...
more infohttp://modeway.tk/noha/cyproheptadine-4-mg-tablet-ivx-wum.php

tripelennamine - meddictripelennamine - meddic

Cinanserin. *Cyproheptadine. *Deramciclane. *Dotarizine. *Eltoprazine. *Ergolines (e.g., amesergide, bromocriptine, LY-53857, ...
more infohttps://meddic.jp/tripelennamine

Invertebrate serotonin receptors: a molecular perspective on classification and pharmacology | Journal of Experimental BiologyInvertebrate serotonin receptors: a molecular perspective on classification and pharmacology | Journal of Experimental Biology

In P. interruptus, ritanserin, (+)-butaclamol and cinanserin were antagonists at 5-HT2βPan receptors, but inactive at 5-HT1αPan ... receptors; in P. clarkii, methiothepin and cinanserin were antagonists at 5-HT2βPro receptors, but inactive at 5-HT1αPro ...
more infohttps://jeb.biologists.org/content/221/19/jeb184838

Plus itPlus it

... including cinanserin, methiothepin, and cyproheptadine (Goldsmith and Abrams 1992; Mercer et al. 1991; Sun and Schacher 1996) ...
more infohttp://jn.physiology.org/content/95/4/2713

Hallucinogens as discriminative stimuli in animals: LSD, phenethylamines, and tryptamines | SpringerLinkHallucinogens as discriminative stimuli in animals: LSD, phenethylamines, and tryptamines | SpringerLink

The antagonists then available, drugs such as cinanserin, methysergide, cyproheptadine, mianserin, and pizotyline (BC-105), ...
more infohttps://link.springer.com/article/10.1007%2Fs00213-008-1356-8

David Prince | Stanford Medicine ProfilesDavid Prince | Stanford Medicine Profiles

... an effect blocked by the antagonists ritanserin and cinanserin and apparently mediated by 5-HT2 receptors. A hyperpolarization ...
more infohttps://med.stanford.edu/profiles/david-prince

Plus itPlus it

... cinanserin, mianserin, and methergoline) interacted with both dopaminergic and serotoninergic receptors but not with beta ...
more infohttp://molpharm.aspetjournals.org/content/14/1/11

Application # 2017/0189654. SYSTEM AND METHODS FOR TREATING MVO - Patents.comApplication # 2017/0189654. SYSTEM AND METHODS FOR TREATING MVO - Patents.com

... such as cinanserin, pizotifen, cyproheptadine, lysenyl, mianserin, methysergide, promethazine, octreotide, trypsin, papain, ...
more infohttp://patents.com/us-20170189654.html

5-HT2C receptor - Wikipedia5-HT2C receptor - Wikipedia

Cinanserin Deramciclane Ketanserin LY-53,857 Metergoline Methiothepin Pizotifen Ritanserin S-32212 SB-206,553 SB-228,357 SB- ...
more infohttps://en.wikipedia.org/wiki/5-HT2C_receptor

FAC - 5-fluorouracil-adriamycin-cyclophosphamide | AcronymAtticFAC - 5-fluorouracil-adriamycin-cyclophosphamide | AcronymAttic

... cinanserin cinca = chronic infantile neurological, cutaneous and articular syndrome cioms = council for international ...
more infohttps://www.acronymattic.com/5_fluorouracil_adriamycin_cyclophosphamide-

March | 2013 | Thrombin InhibitorsMarch | 2013 | Thrombin Inhibitors

Non certain binding was defined as that persisting during the presence of one M cinanserin. Underneath common assay ailments, ...
more infohttp://thrombininhibitors.com/2013/03

Subject Strain Bibliography 1969 | Subject Strain Bibliography records from the 1960s | The Jackson LaboratorySubject Strain Bibliography 1969 | Subject Strain Bibliography records from the 1960s | The Jackson Laboratory

Prolongation of survival of skin homografts in mice with cinanserin alone and in combination with azathioprine., E P. Ambinder ...
more infohttp://mouseion.jax.org/ssbb1969/

publisher:Cornell University +contributor:(Cleland, Thomas A.) - OATDpublisher:'Cornell University' +contributor:('Cleland, Thomas A.') - OATD

Within the habituation task we found that infusion of a 5- HT2 receptor antagonist, cinanserin, impaired habituation memory at ... When sampling behavior and decision times were analyzed, we found that cinanserin infusion significantly increased decision ... cinanserin. Using signal processing techniques, we analyzed the effects of 5-HT on multiunit activity (MUA) and local field ... Within the forced choice discrimination task we found a significant reduction in task performance following cinanserin infusion ...
more infohttps://oatd.org/oatd/search?q=%2Bpublisher%3A%22Cornell%20University%22%20%2Bcontributor%3A%28%22Cleland%2C%20Thomas%20A.%22%29&pagesize-30

immune-source.comimmune-source.com

For medication studies, platelets had been incubated with losartan or cinanserin for 60 s and period, agonist was added and ...
more infohttp://www.immune-source.com/page/3/