A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive activity.
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.
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.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
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.
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.
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.
Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations, and other alterations of mood and thinking. Despite the name, the feature that distinguishes these agents from other classes of drugs is their capacity to induce states of altered perception, thought, and feeling that are not experienced otherwise.
The major of two hallucinogenic components of Teonanacatl, the sacred mushroom of Mexico, the other component being psilocin. (From Merck Index, 11th ed)
Hallucinogenic alkaloid isolated from the flowering heads (peyote) of Lophophora (formerly Anhalonium) williamsii, a Mexican cactus used in Indian religious rites and as an experimental psychotomimetic. Among its cellular effects are agonist actions at some types of serotonin receptors. It has no accepted therapeutic uses although it is legal for religious use by members of the Native American Church.
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
A psychedelic phenyl isopropylamine derivative, commonly called DOM, whose mood-altering effects and mechanism of action may be similar to those of LSD.
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.
Clusters of multipolar neurons surrounded by a capsule of loosely organized CONNECTIVE TISSUE located outside the CENTRAL NERVOUS SYSTEM.
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.
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)
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.
Beaches, both natural and man-made, used for bathing and other activities.
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.
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.
An infraorder of chiefly marine, largely carnivorous CRUSTACEA, in the order DECAPODA, including the genera Cancer, Uca, and Callinectes.
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.
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.
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.
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).
A plant genus of the family ASTERACEAE. Members contain chicoric and chlorogenic acids and germacrane- and eudesmane-type SESQUITERPENES.
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.
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.
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.
Deciduous plant rich in volatile oil (OILS, VOLATILE). It is used as a flavoring agent and has many other uses both internally and topically.
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.
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.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
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.
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.
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.
One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.
A plant genus of the family RUBIACEAE. Members produce YOHIMBINE.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
Drugs used by veterinarians in the treatment of animal diseases. The veterinarian's pharmacological armamentarium is the counterpart of drugs treating human diseases, with dosage and administration adjusted to the size, weight, disease, and idiosyncrasies of the species. In the United States most drugs are subject to federal regulations with special reference to the safety of drugs and residues in edible animal products.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
An adrenergic alpha-2 agonist used as a sedative, analgesic and centrally acting muscle relaxant in VETERINARY MEDICINE.
The medical science concerned with the prevention, diagnosis, and treatment of diseases in animals.
The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.
A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
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)
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.
Affection; in psychiatry commonly refers to pleasure, particularly as it applies to gratifying experiences between individuals.
Medical complexes consisting of medical school, hospitals, clinics, libraries, administrative facilities, etc.
The giving of drugs, chemicals, or other substances by mouth.
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.

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)

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 ...
Inappropriate platelet aggregation creates a cardiovascular risk that is largely managed with thienopyridines and aspirin. Although effective, these drugs carry risks of increased bleeding and drug resistance, underpinning a drive for new antiplatelet agents. To discover such drugs, one strategy is to identify a suitable druggable target and then find small molecules that modulate it. A good and unexploited target is the platelet collagen receptor, GPVI, which promotes thrombus formation. To identify inhibitors of GPVI that are safe and bioavailable, we docked a FDA-approved drug library into the GPVI collagen-binding site in silico. We now report that losartan and cinanserin inhibit GPVI-mediated platelet activation in a selective, competitive and dose-dependent manner. This mechanism of action likely underpins the cardioprotective effects of losartan that could not be ascribed to its antihypertensive effects. We have, therefore, identified small molecule inhibitors of GPVI-mediated platelet
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 ...
Estrogen-related changes in serotonergic neuronal transmission, including changes in the number of serotonin transporter (SERT) binding sites, have been cited as a possible cause for changes in mood, memory and sleep that occur during the menopausal transition. However, both aging and estradiol regulate SERT binding sites in the brain. The goal of this experiment was to determine how aging and est
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 ...
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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
You are viewing an interactive 3D depiction of the molecule 2-(dimethylamino)-1-(6-methyl-5,5-dioxidodibenzo[c,f][1,2,5]thiadiazepin-11(6h)-yl)ethanone (C17H19N3O3S) from the PQR.
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Nucleus raphe obscurus Brain: Nucleus raphe obscurus Section of the medulla oblongata at about the middle of the olive. (Raphe nuclei not labeled, but raphe
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:
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 30388-20-6(Methanaminium,N-[bis(dimethylamino)methylene]-N-methyl-, chloride (1:1)),please inquire us for 30388-20-6(Methanaminium,N-[bis(dimethylamino)methylene]-N-methyl-, chloride (1:1)).
22750-85-2 - KULWQNVVRBBMKK-VHEBQXMUSA-N - Quinoline, 5-((p-(dimethylamino)phenyl)azo)-, 1-oxide - Similar structures search, synonyms, formulas, resource links, and other chemical information.
22750-86-3 - CRIXZDJOKCDXJL-VHEBQXMUSA-N - Quinoline, 6-((p-(dimethylamino)phenyl)azo)-, 1-oxide - Similar structures search, synonyms, formulas, resource links, and other chemical information.
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
1 Click Chemistry Suppliers ,755008-06-1,[2-(dimethylamino)ethyl][(3-methylphenyl)methyl]amine,CN(C)CCNCC1=CC(C)=CC=C1,C12H20N2,MFCD09046178,[2-(dimethylamino)ethyl][(3-methylphenyl)methyl]aminefor your research needs
Most children with the condition gain developmental skills, only to lose them again later.. Within weeks Charlie was deteriorating, losing her ability to sit up and speak.. Anna says: It was utterly devastating but I wasnt going to show Charlie how I was feeling. I said, Ive got the rest of my life to be sad that she died and to miss her, Im not going to show her that while shes alive.. I just wanted Charlie to have the best life she could and not be scared about why Mummy and Daddy were upset all the time.. ...
Cirripectes obscurus és una espècie de peix de la família dels blènnids i de lordre dels perciformes. És un peix marí de clima tropical i associat als esculls de corall que viu entre 0-6 m de fondària.[4][5] Es troba a Hawaii[6][7][8] i a latol Midway.[4][9] És ovípar.[10] Els mascles poden assolir 20 cm de longitud total.[4][11] ...
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.
Page contains details about (Z)-3-(4-(2,2-bis(4-(dimethylamino)phenyl)-1-phenylvinyl)phenyl)-2-phenylacrylonitrile nanoparticles colloid . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
Suppliers List, E-mail/RFQ Form, Molecular Structure, Weight, Formula, IUPAC, Synonyms for (4-(dimethylamino)phenyl)(pyridin-3-yl)methanol (CAS No. 1409672-93-0)
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.
Lookchem Provide Cas No.84255-31-2 Basic information: Properties,Safety Data,Sds and Other Datebase. We also Provide Trading Suppliers & Manufacture for 84255-31-2 N-[[5-(dimethylamino)-1-naphthyl]sulphonyl]-DL-leucine, compound with piperidine (1:1).
This page contains information on the chemical 1,2-Benzenediol, 4-(2-(dimethylamino)-1-hydroxyethyl)-, (R)-, phosphate (1:1) (salt) including: 3 synonyms/identifiers.
3-(2-(Dimethylamino)ethyl)indole sulfosalicylate | C19H22N2O6S | CID 58944 - 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...
ADAM12山羊多克隆抗体(ab28747)可与人样本反应并经WB, IHC实验严格验证,被2篇文献引用。所有产品均提供质保服务,中国75%以上现货。
ADAM20兔多克隆抗体(ab118612)可与人样本反应并经IHC实验严格验证。中国75%以上现货,所有产品均提供质保服务,可通过电话、电邮或微信获得本地专属技术支持。
Benzenemethanol,2-chloro-a-[2-(dimethylamino)ethyl]-a-phenyl-,hydrochloride (1:1) CAS 511-13-7 supplier 511-13-7 Suppliers,provide Benzenemethanol,2-chloro-a-[2-(dimethylamino)ethyl]-a-phenyl-,hydrochloride (1:1) CAS 511-13-7 supplier 511-13-7 product and the products related with China (Mainland) Benzenemethanol,2-chloro-a-[2-(dimethylamino)ethyl]-a-phenyl-,hydrochloride (1:1) CAS 511-13-7 supplier 511-13-7 Wuhan Monad Medicine Tech Co.,LTD China (Mainland)
1-[2-(Dimethylamino)ethyl]piperazine 97% | N,N-Dimethyl-2-(piperazin-1-yl)ethylamine, 1-(Dimethylamino)-2-(piperazin-1-yl)ethane | OR6907 | 3644-18-6 | Apollo Scientific Ltd
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?
3-Bromo-n-[2-(dimethylamino)ethyl]benzamide; CAS Number: 425618-78-6; Linear Formula: C11H15BrN2O; find Combi-Blocks, Inc.-COMH93D5B863 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich
This page contains information on the chemical Pyridine, 2-((2-(dimethylamino)ethyl)-3-thenylamino)-, monohydrochloride including: 10 synonyms/identifiers.
Name: 4-(4-Dimethylaminoanilino)phenol CA Name: Phenol,4-[[4-(dimethylamino)phenyl]amino]- Molecular Structure: 4-(4-Dimethylaminoanilino)phenol,Phenol,4-[[4-(dimethylamino)phenyl]amino]-,CAS 6358-22-1,228.29,C14H16N2O 4-(4-Dimethylaminoanilino)phenol,Phenol,4-[[4-(dimethylamino)phenyl]amino]-,CAS 6358-22-1,228.29,C14H16N2O Molecular Formula:C14H16N2O Molecular Weight: 228.29 CAS Registry Number: 6358-22-1
Contact Us. Tel:732-484-9848. Fax:888-484-5008. Email:[email protected]. Add:1 Deer Park Dr, Suite Q,. Monmouth Junction, NJ 08852, USA. ...
Contact Us. Tel:732-484-9848. Fax:888-484-5008. Email:[email protected]. Add:1 Deer Park Dr, Suite Q,. Monmouth Junction, NJ 08852, USA. ...
Dellov ustanovitelj Michael Dell je dokončal prevzem podjetja, za katerega si je prizadeval že od začetka leta. Prevzemnih ponudb je bilo več, a na koncu je zmagal Michael Dell, kar je septembra potrdil tudi Dellov upravni odbor. Transakcija je sedaj dokončana. Vsi Dellovi delničarji bodo dobili 13,75 dolarja za delnico, hkrati pa so upravičeni do izredne dividende v višini 0,13 dolarja, ki jo prejmejo lastniki na presečni datum 28. oktobra...
Cinanserin Deramciclane Ketanserin LY-53,857 Metergoline Methiothepin Pizotifen Ritanserin S-32212 SB-206,553 SB-228,357 SB- ...
... cinanserin MeSH D02.241.223.201.210 - coumaric acids MeSH D02.241.223.201.711 - puromycin MeSH D02.241.223.201.711.650 - ...
... cinanserin (INN) cinaproxen (INN) cinchocaine (INN) cinchophen (INN) cinecromen (INN) cinepaxadil (INN) cinepazet (INN) ...
The molecular formula C20H24N2OS (molar mass: 340.48 g/mol, exact mass: 340.1609 u) may refer to: Cinanserin Lucanthone ...
... (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. The molecule is an inhibitor of ... June 2005). "Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215840, ...
Cinanserin (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. The molecule is an inhibitor of ... June 2005). "Cinanserin is an inhibitor of the 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly ...
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 ...
Cinanserin/AFI1166343 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and ...
Cinanserin [INN] Description: A serotonin antagonist with limited antihistaminic, anticholinergic, and immunosuppressive ...
Cinanserin [INN] View Synonyms. View Structure. Description:. A serotonin antagonist with limited antihistaminic, ...
CINANSERIN cirazoline cisapride CITCO clofenotane clomipramine cortisone coumafos crotamiton CYANOPINDOLOL(+) cyclobenzaprine ...
... by cinanserin. Can J Physiol Pharmacol 51:976-980PubMedCrossRefGoogle Scholar ...
... by BC-105 and cinanserin (CN). The effect on M -mediated stimulus control of 5HT depletion by p-chlorphenylalanine (CPA), an ...
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 ...
... including cinanserin, methiothepin, and cyproheptadine (Goldsmith and Abrams 1992; Mercer et al. 1991; Sun and Schacher 1996) ...
The antagonists then available, drugs such as cinanserin, methysergide, cyproheptadine, mianserin, and pizotyline (BC-105), ...
11202572:Cinanserin Is an Inhibitor of the 3C-Like Proteina. *11202573:Deletion of M2 Gene Open Reading Frames 1 and 2 of ...
... an effect blocked by the antagonists ritanserin and cinanserin and apparently mediated by 5-HT2 receptors. A hyperpolarization ...
Cinanserin Deramciclane Ketanserin LY-53,857 Metergoline Methiothepin Pizotifen Ritanserin S-32212 SB-206,553 SB-228,357 SB- ...
... and cinanserin, at physiological pH, on proteins essential for SARS-CoV-2 virus survival. ...
If 5-HT were the cause of the delayed excitation it should be blocked with cinanserin which has been shown to be an effective ...
extract, quercetin, quercetrin and cinanserin on murine coronavirus and dengue virus infection. Asian Pac J Trop Med. 2016;9(1 ...
Cinanserin hydrochloride. 5-HT2 Receptor, Ki: 41 nM 99.74%. 2-Methyl-5-HT. 5-HT3 Receptor ...
... cinanserin, mianserin, and methergoline) interacted with both dopaminergic and serotoninergic receptors but not with beta ...
Design and Synthesis of Cinanserin Analogs as Severe Acute Respiratory Syndrome Coronavirus 3CL Protease Inhibitors Qingang ...
... such as cinanserin, pizotifen, cyproheptadine, lysenyl, mianserin, methysergide, promethazine, octreotide, trypsin, papain, ...
... cinanserin cinca = chronic infantile neurological, cutaneous and articular syndrome cioms = council for international ...
Cinanserin. *CSP-2503. *Deramciclane. *Dotarizine. *Eplivanserin. *Ergolines (e.g., amesergide, LY-53857, LY-215,840, ...
Cinanserin. *Cyproheptadine. *Deramciclane. *Dotarizine. *Eltoprazine. *Ergolines (e.g., amesergide, bromocriptine, LY-53857, ...
Adatanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine.. All-Night Herbal Viagra Tablets. . macular edema; ...
Cinanserin]]{{•}} [[CSP-2503]]{{•}} [[Cyproheptadine]]{{•}} [[Deramciclane]]{{•}} [[Dotarizine]]{{•}} [[Eplivanserin]]{{•}} [[ ...
CINANSERIN HYDROCHLORIDE. C20H25ClN2OS. 53-44-1. 3-[(3-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a] ...
Cinanserin. *Cyproheptadine. *Deramciclane. *Dotarizine. *Eltoprazine. *麥角靈(如:amesergide、溴隱亭、LY-53857、LY-215840、mesulergine、 ...
  • Cinanserin, a well-characterized serotonin antagonist, scored high in the screening and was selected for further experimentation. (rxpgnews.com)
  • These findings demonstrate that the old drug cinanserin is an inhibitor of SARS-CoV replication, acting most likely via inhibition of the 3CL proteinase," say the researchers. (rxpgnews.com)
  • RxPG] Cinanserin, a drug that underwent preliminary clinical testing on humans in the 1960's, may inhibit the SARS virus say researchers from Europe and China. (rxpgnews.com)
  • Cinanserin (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. (wikipedia.org)