共查询到20条相似文献,搜索用时 31 毫秒
1.
The 5-HT3 receptor is a ligand-gated ion channel activated by serotonin (5-HT). Although originally identified in the peripheral nervous system, the 5-HT3 receptor is also ubiquitously expressed in the central nervous system. Sites of expression include several brain stem nuclei and higher cortical areas such as the amygdala, hippocampus, and cortex. On the subcellular level, both presynaptic and postsynaptic 5-HT3 receptors can be found. Presynaptic 5-HT3 receptors are involved in mediating or modulating neurotransmitter release. Postsynaptic 5-HT3 receptors are preferentially expressed on interneurons. In view of this specific expression pattern and of the well-established role of 5-HT as a neurotransmitter shaping development, we speculate that 5-HT3 receptors play a role in the formation and function of cortical circuits. 相似文献
2.
Colin T. Dourish 《Obesity (Silver Spring, Md.)》1995,3(Z4):449S-462S
Recent progress in the molecular pharmacology of 5-HT receptors and the development of selective ligands for various 5-HT receptor subtypes has advanced our understanding of the role of 5-HT mechanisms in the control of food intake and body weight The most intensively investigated 5-HT receptor subtypes have been the 5-HT1A receptor, the 5-HT1B receptor andthe5-HT2C receptor. The overall pattern of results to date suggests that selective 5-HT2C agonists may be novel anorectic drugs and prove useful in the treatment of obesity. However, a number of issues remain unresolved, particularly regarding potential side-effects, as the 5-HT2C receptor agonist mCPP has been reported to induce anxiety and nausea in humans, actions that would clearly limit its therapeutic utility. In addition, the possible role of recently cloned 5-HT receptor subtypes such as 5-ht5,5-ht6 and 5-ht7 remains unexplored and the development of selective ligands for these sites has the potential to lead to new treatments for obesity . 相似文献
3.
Padmanabhan Anbazhagan Meera Purushottam H. B. Kiran Kumar Odity Mukherjee Sanjeev Jain Ramanathan Sowdhamini 《Journal of biomolecular structure & dynamics》2013,31(5):581-598
Abstract Neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) an ancient neurotransmitter, involved in several neurophysiological and behavioral functions, acts by interacting with multiple receptors (5-HT1-5-HT7). Alterations in serotonergic signalling have also been implicated in various psychiatric disorders. The availability of the genome data of nonhuman primates permits comparative analysis of human 5-HT receptors with sequences of non-human primates to understand evolutionary divergence. We compared and analyzed serotonergic receptor sequences from human and non-human primates. Phylogenetic analysis by Maximum Likelihood (ML) method classified human and primate 5-HT receptors into six unique clusters. There was considerable conservation of 5-HT receptor sequences between human and non-human primates; however, a greater diversity at the sub-group level was observed. Compared to the other subgroups, larger multiplicity and expansion was seen within the 5-HT4 receptor subtype in both human and non-human primates. Analysis of non-synonymous and synonymous substitution ratios (Ka/Ks ratio) using the Nei-Gojobori method suggests that 5-HT receptor sequences have undergone negative (purifying) selection over the course of evolution in human, chimpanzee and rhesus monkey. Abnormal human and non-human primate psychopathalogy and behavior, in the context of these variations is discussed. Analysis of these 5-HT receptors in other species will help understand the molecular evolution of 5-HT receptors, and its possible influence on complex behaviors, and psychiatric disorders. 相似文献
4.
Jotaro Akiyoshi Akira Nishizono Kenji Yamada Haruo Nagayama Kumato Mifune Isao Fujii 《Journal of neurochemistry》1995,64(6):2473-2479
Abstract: Serotonin 5-HT2C receptor-mediated intracellular Ca2+ mobilization was investigated in Chinese hamster ovary (CHO) cells transfected with 5-HT2C receptors. Fura-2 acetoxymethyl ester was used to investigate the regulation of 5-HT2C receptor function. CHO cells, transfected with a cDNA clone for the 5-HT2C receptor, expressed 287 fmol/mg of the receptor protein as determined by mianserin-sensitive [3H]mesulergine binding (KD = 0.49 nM). The addition of 5-HT mobilized intracellular Ca2+ in a dose-dependent fashion, ranging from a basal level of 99 ± 1.8 up to 379 ± 18 nM, with an EC50 value for 5-HT of 0.029 µM. Exposure to 5-HT, 1-(3-chlorophenyl)piperazine dihydrochloride (a 5-HT2C agonist), and 1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane (a 5-HT2C and 5-HT2A agonist) resulted in increased intracellular Ca2+ levels. Mianserin, mesulergine, ritanserin, and ketanserin each blocked 5-HT-mediated intracellular Ca2+ mobilization more effectively than spiperone. The receptor was rapidly desensitized by preexposure to 5-HT in a time- and concentration-dependent manner. Mezerein and phorbol 12-myristate 13-acetate, protein kinase C activators, weakly inhibited the intracellular Ca2+ mobilization induced by 10 µM 5-HT. Furthermore, the protein kinase C inhibitor H-7 partially prevented the protein kinase C activator-induced inhibition of the 5-HT-mediated increase in intracellular Ca2+ concentration. The desensitization induced by pretreatment with 5-HT was blocked by W-7, added in conjunction with 5-HT, and partially inhibited by W-5, a nonselective inhibitor of protein kinases and weak analogue of W-7. Therefore, the 5-HT2C receptor may be connected with protein kinase C and calcium/calmodulin turnover. These results suggest that 5-HT2C receptor activation mobilizes Ca2+ in CHO cells and that the acute desensitization of the receptor may be due to calmodulin kinase-mediated feedback. 相似文献
5.
Molecular characterization and analysis of a truncated serotonin receptor gene expressed in neural and reproductive tissues of abalone 总被引:1,自引:0,他引:1
Sasiporn Panasophonkul Somjai Apisawetakan Scott F. Cummins Patrick S. York Bernard M. Degnan Peter J. Hanna Porncharn Saitongdee Prasert Sobhon Prapee Sretarugsa 《Histochemistry and cell biology》2009,131(5):629-642
6.
Labasque M Reiter E Becamel C Bockaert J Marin P 《Molecular biology of the cell》2008,19(11):4640-4650
The serotonin (5-hydroxytryptamine; 5-HT)2C receptor is a G protein-coupled receptor (GPCR) exclusively expressed in CNS that has been implicated in numerous brain disorders, including anxio-depressive states. Like many GPCRs, 5-HT2C receptors physically interact with a variety of intracellular proteins in addition to G proteins. Here, we show that calmodulin (CaM) binds to a prototypic Ca2+-dependent “1-10” CaM-binding motif located in the proximal region of the 5-HT2C receptor C-terminus upon receptor activation by 5-HT. Mutation of this motif inhibited both β-arrestin recruitment by 5-HT2C receptor and receptor-operated extracellular signal-regulated kinase (ERK) 1,2 signaling in human embryonic kidney-293 cells, which was independent of G proteins and dependent on β-arrestins. A similar inhibition was observed in cells expressing a dominant-negative CaM or depleted of CaM by RNA interference. Expression of the CaM mutant also prevented receptor-mediated ERK1,2 phosphorylation in cultured cortical neurons and choroid plexus epithelial cells that endogenously express 5-HT2C receptors. Collectively, these findings demonstrate that physical interaction of CaM with recombinant and native 5-HT2C receptors is critical for G protein-independent, arrestin-dependent receptor signaling. This signaling pathway might be involved in neurogenesis induced by chronic treatment with 5-HT2C receptor agonists and their antidepressant-like activity. 相似文献
7.
The aminotetralin 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), pharmacologically characterized as a 5-HT1A receptor agonist, produces a pronounced decrease in ejaculation latency in the male rat. Stimulation of 5-HT receptors by a pharmacologically induced increase in the synaptic availability of 5-HT has been shown to produce the opposite effect. The 8-OH-DPAT-induced decrease in ejaculation latency is specific for this compound, and some chemically related ergot derivatives. In this paper we review the evidence in support for stimulation of serotonergic auto-receptors of the 5-HT1A receptor subtype as a mechanism of action for effects by 8-OH-DPAT on male rat ejaculatory behavior. We also present the questions posed by the fact that quinpirole and lisuride both produce 8-OH-DPAT-like effects on male rat ejaculatory behavior. The effects by quinpirole, lisuride or 8-OH-DPAT are not sensitive to pretreatment with the DA D2/3 receptor antagonist raclopride. Continued studies will show whether the effects of quinpirole and lisuride can be related to stimulation of 5-HT1A receptors, or if all these compounds have as yet undefined common properties. 相似文献
8.
Mice that carry the autosomal recessive gene weaver show a distinctive loss of nigrostriatal dopamine innervation, with the greatest deficits in the dorsal caudate-putamen and almost complete sparing in the nucleus accumbens and ventral caudate. In addition to loss of dopamine in this model, it has recently been shown that markers of serotonin (5-hydroxytryptamine, 5-HT) innervation including 5-HT content, synaptosomal uptake of [3H]5-HT and [3H]citalopram binding were elevated in the dorsal neostriatum of the weaver mutant mouse. Using quantitative autoradiography of specific ligands for dopamine and 5-HT uptake sites as well as serotonin 5-HT1 and 5-HT2A receptors, we found an increased density of 5-HT uptake sites and 5-HT1 receptors restricted to the dorsal portion of the neostriatum of the weaver mouse. In contrast, 5-HT2A receptors were increased in both the dorsal and ventral portions of the rostral neostriatum as well as the nucleus accumbens. The behavioural and functional relevance of these receptor changes is unclear, although, adaptations in 5-HT may play a role in certain aspects of spontaneous behaviour in the weaver mutant mouse. 相似文献
9.
R. A. Newton S. L. Phipps T. P. Flanigan N. R. Newberry J. E. Carey †C. Kumar ‡B. McDonald ‡C. Chen J. M. Elliott 《Journal of neurochemistry》1996,67(6):2521-2531
Abstract: Stable transfection of the human neuroblastoma cell line SH-SY5Y with the human 5-hydroxytryptamine2A (5-HT2A) or 5-HT2C receptor cDNA produced cell lines demonstrating ligand affinities that correlated closely with those for the corresponding endogenous receptors in human frontal cortex and choroid plexus, respectively. Stimulation of the recombinant receptors by 5-HT induced phosphoinositide hydrolysis with higher potency but lower efficacy at the 5-HT2C receptor (pEC50 = 7.80 ± 0.06) compared with the 5-HT2A receptor (pEC50 = 7.30 ± 0.08). Activation of the 5-HT2A receptor caused a transient fourfold increase in intracellular Ca2+ concentration. Whole-cell recordings of cells clamped at ?50 mV demonstrated a small inward current (2 pA) in response to 10 µM 5-HT for both receptors. There were no differences in potency or efficacy of phosphoinositide hydrolysis among four hallucinogenic [d-lysergic acid diethylamide (LSD), 1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane (DOI), 5-methoxy-N,N-dimethyltryptamine, and mescaline] and three nonhallucinogenic drugs (m-chlorophenylpiperazine, quipazine, and ergotamine). Comparison of equipotent doses producing 20% of the maximal response induced by 5-HT revealed selective activation of the 5-HT2A receptor by LSD and to a lesser degree by DOI, mescaline, and ergotamine. Quipazine and 5-methoxy-N,N-dimethyltryptamine were relatively nonselective, whereas m-chlorophenylpiperazine selectively activated the 5-HT2C receptor. It is unlikely therefore that hallucinosis is mediated primarily by activity at the 5-HT2C receptor, whereas activity at the 5-HT2A receptor may represent an important but not unique mechanism associated with hallucinogenic drug action. 相似文献
10.
11.
Abstract: Serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A and 5-HT2C receptors belong to the class of phosphoinositide-specific phospholipase C (PLC)-linked receptors. Conditions were established for measuring 5-HT2A-linked and 5-HT2C-linked PLC activity in membranes prepared from previously frozen rat frontal cortex and caudate. In the presence of Ca2+ (300 nM) and GTPγS (1 µM), 5-HT increased PLC activity in caudate membranes. Pharmacological analysis using the selective 5-HT2A antagonist, spiperone, and the nonselective 5-HT2A/2C antagonist, mianserin, demonstrated that over half of the 5-HT-stimulated PLC activity was due to stimulation of 5-HT2C receptors as opposed to 5-HT2A receptors. Radioligand binding assays with [3H]RP 62203 and [3H]-mesulergine were used to quantify 5-HT2A and 5-HT2C sites, respectively, in caudate. From these data, the Bmax for caudate 5-HT2A sites and 5-HT2C sites was 165.4 ± 9.7 fmol/mg of protein and 49.7 ± 3.3 fmol/mg of protein, respectively. In contrast to that in caudate, PLC activity in frontal cortex was stimulated by 5-HT in a manner that was inhibited by the 5-HT2A-selective antagonists, spiperone and ketanserin. Taken together, the results indicate that 5-HT2A- and 5-HT2C-linked PLC activity can be discerned in brain regions possessing both receptor subtypes using membranes prepared from previously frozen tissue. More importantly, significant 5-HT2C-mediated phosphoinositide hydrolysis was observed in caudate, despite the relatively low density of 5-HT2C sites. The significance of these observations with respect to the physiological function of 5-HT2C receptors is discussed. 相似文献
12.
E. K. Nénonéné F. Radja M. Carli L. Grondin T. A. Reader 《Journal of neurochemistry》1994,62(5):1822-1834
Abstract: The selective serotonin (5-HT) agonist 8-hydroxydipropylaminotetralin (8-OH-DPAT) has been extensively used to characterize the physiological, biochemical, and behavioral features of the 5-HT1A receptor. A further characterization of this receptor subtype was conducted with membrane preparations from rat cerebral cortex and hippocampus. The saturation binding isotherms of [3H]8- OH-DPAT (free ligand from 200 pM to 160 nM) revealed high-affinity 5-HT1A receptors (KH= 0.7–0.8 nM) and lowaffinity (KL= 22–36 nM) binding sites. The kinetics of [3H]8-OH-DPAT binding were examined at two ligand concentrations, i.e., 1 and 10 nM, and in each case revealed two dissociation rate constants supporting the existence of high- and low-affinity binding sites. When the high-affinity sites were labeled with a 1 nM concentration of [3H]8- OH-DPAT, the competition curves of agonist and antagonist drugs were best fit to a two-site model, indicating the presence of two different 5-HT1A binding sites or, alternatively, two affinity states, tentatively designated as 5-HT1AHIGH and 5-HT1ALOW. However, the low correlation between the affinities of various drugs for these sites indicates the existence of different and independent binding sites. To determine whether 5-HT1A sites are modulated by 5′-guanylylimidodiphosphate, inhibition experiments with 5-HT were performed in the presence or in the absence of 100 μM 5′-guanylylimidodiphosphate. The binding of 1 nM [3H]8-OH-DPAT to the 5-HT1AHIGH site was dramatically (80%) reduced by 5′-guanylylimidodiphosphate; in contrast, the low-affinity site, or 5-HT1ALOW, was seemingly insensitive to the guanine nucleotide. The findings suggest that the high-affinity 5-HT1AHIGH site corresponds to the classic 5-HT1A receptor, whereas the novel 5-HT1ALOW binding site, labeled by 1 nM [3H]8-OH-DPAT and having a micromolar affinity for 5-HT, may not belong to the G protein family of receptors. To further investigate the relationship of 5-HT1A sites and the 5-HT innervation, rats were treated with p-chlorophenylalanine or with the neurotoxin p-chloroamphetamine. The inhibition of 5-HT synthesis by p-chlorophenylalanine did not alter either of the two 5-HT1A sites, but deafferentation by p-chloroamphetamine caused a loss of the low-affinity [3H]8-OH- DPAT binding sites, indicating-that these novel binding sites may be located presynaptically on 5-HT fibers and/or nerve terminals. 相似文献
13.
The regulation of neuronal excitability is complex, as ion channels and neurotransmitter receptors are underlying a large
variety of modulating effects. Alterations in the expression patterns of receptors or channel subunits as well as differential
splicing contribute to the regulation of neuronal excitability. RNA editing is another and more recently explored mechanism
to increase protein diversity, as the genomic recoding leads to new gene products with novel functional and pharmacological
properties. In humans A-to-I RNA editing targets several neuronal receptors and channels, including GluR2/5/6 subunits, the
Kv1.1 channel, and the 5-HT2C receptor. Our review summarizes that RNA editing of these proteins does not only change protein function, but also the pharmacology
and presumably the drug therapy in human diseases. 相似文献
14.
(1) Pre-mRNA editing of serotonin 2C (5-HT2C) and glutamate (Glu) receptors (R) influences higher brain functions and pathological states such as epilepsy, amyotrophic
lateral sclerosis, and depression. Adenosine deaminases acting on RNA (ADAR1–3) convert adenosine to inosine on synthetic
RNAs, analogous to 5-HT2cR and GluR. The order of editing as well as mechanisms controlling editing in native neurons is unknown. (2) With single-cell
RT-PCR we investigated the co-expression of ADAR genes with GluR and 5-HT2CR and determined the editing status at known sites in the hypothalamic tuberomamillary nucleus, a major center for wakefulness
and arousal. (3) The most frequently expressed enzymes were ADAR1, followed by ADAR2. The Q/R site of GluR2 was always fully
edited. Editing at the R/G site in the GluR2 (but not GluR4) subunit was co-ordinated with ADAR expression: maximal editing
was found in neurons expressing both ADAR2 splice variants of the deaminase domain and lacking ADAR3. (4) Editing of the 5-HT2CR did not correlate with ADAR expression. The 5-HT2CR mRNA was always edited at A, in the majority of cells at B sites and variably edited at E, C and D sites. A negative correlation
was found between editing of C and D sites. The GluR4 R/G site editing was homogeneous within individuals: it was fully edited
in all neurons obtained from 12 rats and under-edited in six neurons obtained from three rats. (5) We conclude that GluR2
R/G editing is controlled at the level of ADAR2 and therefore this enzyme may be a target for pharmacotherapy. On the other
hand, further factors/enzymes besides ADAR must control or influence 5-HT2CR and GluR pre-mRNA editing in native neurons; our data indicate that these factors vary between individuals and could be
predictors of psychiatric disease. 相似文献
15.
Suk Youn Kang Eun-Jung Park Woo-Kyu Park Hyun Jung Kim Daeyoung Jeong Myung Eun Jung Kwang-Seop Song Suk Ho Lee Hee Jeong Seo Min Ju Kim MinWoo Lee Ho-Kyun Han Eun-Jung Son Ae Nim Pae Jeongmin Kim Jinhwa Lee 《Bioorganic & medicinal chemistry letters》2010,20(5):1705-1711
Arylpiperzine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated as novel antidepressant compounds. The various analogues were efficiently prepared and bio-assayed for binding to 5-HT2A, 5-HT2C receptor, and 5-HT transporter. Based on their in vitro and in vivo activities as well as selectivity over other neurotransmitter receptors and PK profiles, 33 and 34 were identified as lead compounds. Consequently, this pyrrole series of compounds appears to be promising enough to warrant further investigation. 相似文献
16.
Ma. Teresa Peña-Rangel Rosalio Mercado-C. Jorge Hernández-Rodríguez 《Neurochemical research》1999,24(5):643-649
The purpose of the present study was the characterization of the receptors participating in the regulatory mechanism of glial Na+/K+-ATPase by serotonin (5-HT) in rat brain. The activity of the Na+ pump was measured in four brain regions after incubation with various concentrations of serotoninergic agonists or antagonists. A concentration-dependent increase in enzyme activity was observed with the 5-HT1A agonist R (+)-2-dipropylamino-8-hydroxy-1,2,3, 4-tetrahydronaphthalene hydrobromide (8-OH-DPAT) in homogenates or in glial membrane enriched fractions from cerebral cortex and in hippocampus. Spiperone, a 5-HT1A antagonist, completely inhibited the response to 8-OH-DPAT but had no effect on Na+/K+-ATPase activity in cerebellum where LSD, a 5-HT6 agonist, elicited a dose-dependent response similar to that of 5-HT. In brainstem, a lack of reponse to 5-HT and other agonists was confirmed. Altogether, these results show that serotonin modulates glial Na+/K+-ATPase activity in the brain, apparently not through only one type of 5-HT receptor. It seems that the receptor system involved is different according to the brain region. In cerebral cortex, the response seems to be mediated by 5-HT1A as well as in hippocampus but not in cerebellum where 5-HT6 appears as the receptor system involved. 相似文献
17.
J. Daniel Hothersall Amy Alexander Andrew J. Samson Christopher Moffat Karen A. Bollan Christopher N. Connolly 《The Journal of biological chemistry》2014,289(46):32020-32029
The serotonergic synapse is dynamically regulated by serotonin (5-hydroxytryptamine (5-HT)) with elevated levels leading to the down-regulation of the serotonin transporter and a variety of 5-HT receptors, including the 5-HT type-3 (5-HT3) receptors. We report that recombinantly expressed 5-HT3 receptor binding sites are reduced by chronic exposure to 5-HT (IC50 of 154.0 ± 45.7 μm, t½ = 28.6 min). This is confirmed for 5-HT3 receptor-induced contractions in the guinea pig ileum, which are down-regulated after chronic, but not acute, exposure to 5-HT. The loss of receptor function does not involve endocytosis, and surface receptor levels are unaltered. The rate and extent of down-regulation is potentiated by serotonin transporter function (IC50 of 2.3 ± 1.0 μm, t½ = 3.4 min). Interestingly, the level of 5-HT uptake correlates with the extent of down-regulation. Using TX-114 extraction, we find that accumulated 5-HT remains soluble and not membrane-bound. This cytoplasmically sequestered 5-HT is readily releasable from both COS-7 cells and the guinea pig ileum. Moreover, the 5-HT level released is sufficient to prevent recovery from receptor desensitization in the guinea pig ileum. Together, these findings suggest the existence of a novel mechanism of down-regulation where the chronic release of sequestered 5-HT prolongs receptor desensitization. 相似文献
18.
Abstract: The serotonin 5-HT2C receptor (formerly designated the 5-HT1C receptor) of the choroid plexus triggers phosphoinositide turnover. In the present study, we demonstrate that receptor activation also triggers the formation of cyclic GMP (cGMP). Application of 1 µM 5-HT to porcine choroid plexus tissue slices resulted in stimulation of cGMP formation to a maximum of five-fold basal level, with an EC50 of 11 nM. This response was not inhibited by muscarinic or β-adrenergic receptor antagonists. Serotonin receptor antagonists inhibited cGMP formation with apparent Ki values of 1.3 (mianserin), 200 (ketanserin), and 5,500 (spiperone) nM, respectively. Neither serotonin-stimulated cGMP formation nor PI turnover was inhibited by pertussis toxin pretreatment. Preliminary biochemical studies suggested that serotonin-stimulated cGMP formation was calcium, phospholipase A2, and lipoxygenase dependent, as incubation in low calcium buffers or inclusion of the phospholipase A2 or lipoxygenase inhibitors p-bromophenacyl bromide or BW 755c resulted in significant reduction of cGMP formation. The present results suggest that in addition to triggering phosphoinositide turnover, choroid plexus serotonin 5-HT2C receptors trigger cGMP formation in a calcium-sensitive manner. 相似文献
19.
20.
The serotonin 5-HT1D receptor: A progress review 总被引:4,自引:0,他引:4
Christian Waeber Philippe Schoeffter Daniel Hoyer José M. Palacios 《Neurochemical research》1990,15(6):567-582
Most of the known neurotransmitters interact with more than one type of receptor. Some of them even dispose of receptor subtypes to exert their actions. Serotonin, far from being an exception to that, possesses at least 3 classes of receptors, which have all been reported to be heterogeneous, although convincing data only exist for the 5-HT1 class. This name has been proposed in 1979, two years before the introduction of A and B in the nomenclature to account for the observed heterogeneity of these cites. The 5-HT1C receptor subtype was first described in 1984 and the last member of the family, named 5-HT1D, was characterized in 1987. The pharmacological profiles, the signal transducing systems and the anatomical localizations, both at the regional and cellular levels, of all these subtypes have been investigated and possible functions have been proposed for each of them. Moreover, last and most definitive demonstration of the subtype individuality, the gene or complementary DNA coding for the 5-HT1A and 5-HT1C (and 5-HT2) receptors have been cloned and sequenced. Such data are still missing for 5-HT1D (and 5-HT1B) receptors, but will certainly be provided in the next few years. However and waiting for this decisive clue, the characterization of the 5-HT1D subtype leaves no doubt concerning its significance as a functional 5-HT receptor. This review will concentrate on the characteristics of this subtype of 5-HT receptor.Abbreviations 5-CT
5-carboxamidotryptamine
- 5-MeOT
5-methoxy-tryptamine
- 5-MeODMT
N,N-dimethyl-5-methoxytryptamine
- 8-OH-DPAT
8-hydroxy-2[di-n-propylamino]tetralin
- CYP
cyanopindolol
- DHE
dihydroergotamine
- DOI
2,5-dimethoxy-4-iodophenylisopropylamine
- DP-5-CT
N,N-dipropyl 5-carboxamidotryptamine
- ICPY
2-iodo-cyanopindolol
- mCPP
m-chloro-phenyl-piperazine
- TFMPP
m-trifluoro-methyl-phenyl-piperazine
- EMAX
Maximal effect
- EC50
Half maximal effective concentration
- KD
Dissociation constant
- KB
Antagonist dissociation constant 相似文献