5 ht 1a antagonist. Medical search. Frequent questions

However, it is unclear whether 5-HT1A receptor antagonists not discriminating between pre- and post-synaptic 5-HT 1A receptors would be clinically effective. (uab.cat)
Key results: DU-125530 showed equal (low nM) potency to displace agonist and antagonist binding to pre- and post-synaptic 5-HT1A receptors in rat and human brain. (uab.cat)
DU-125530 augmented SSRI-induced increases in extracellular 5-HT as effectively as in mice lacking 5-HT1A receptors, indicating a silent, maximal occupancy of pre-synaptic 5-HT1A receptors at the dose used. (uab.cat)
However, blockade of post-synaptic 5- HT1A receptors by DU-125530 cancels benefits obtained by enhancing pre-synaptic 5-hydroxytryptaminergic function. (uab.cat)
The aminotetralins, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and 7-OH-DPAT behave as preferential agonists at serotonin (5-HT) 1A and dopamine D 3 and D 2 receptors, respectively. (aspetjournals.org)
In our study, we evaluated the influence of their (+)- and (-) isomers on the electrical activity of serotoninergic neurones of the dorsal raphe nucleus (DRN), which bear 5-HT 1A autoreceptors, and of dopaminergic neurones of the ventral tegmental area (VTA), which possess inhibitory D 3 and D 2 receptors. (aspetjournals.org)
These actions were compared to their in vitro interactions with cloned, human (h)5-HT 1A , hD 3 and hD 2 receptors. (aspetjournals.org)
In binding studies, racemic 8-OH-DPAT showed 100-fold selectivity for h5-HT 1A vs . hD 2 and hD 3 receptors and there was little difference between its (+)- and (-)-isomers either in terms of their potency at 5-HT 1A receptors or of their selectivity at 5-HT 1A vs hD 2 /hD 3 sites. (aspetjournals.org)
Concerning 5-HT 1A receptors, the (+)-isomer showed 20-fold lower affinity than at hD 3 receptors and, accordingly, it inhibited DRN firing at 20-fold higher doses than for inhibition of VTA firing. (aspetjournals.org)
Finally, in line with this inhibition of DRN firing, both (+)- and (-)-7-OH-DPAT showed substantial efficacy ([ 35 S]-GTPγS binding, 76 and 53%, respectively) at h5-HT 1A receptors. (aspetjournals.org)
In conclusion, for these substituted aminotetralins, stereospecificity is a more marked feature of interactions at hD 3 (and hD 2 ) than at h5-HT 1A receptors and is more pronounced for 7- as compared to 8-OH-DPAT. (aspetjournals.org)
Neither (+)- nor (-)-7-OH-DPAT show substantial selectivity for hD 3 vs . 5-HT 1A receptors and their inhibition of the firing of VTA as compared to DRN neurones is mediated by hD 3 /hD 2 and 5-HT 1A receptors, respectively. (aspetjournals.org)
Finally, VTA neurones are stimulated by (+)-8-OH-DPAT via 5-HT 1A receptors and inhibited by (-)-8-OH-DPAT via hD 3 and/or hD 2 receptors. (aspetjournals.org)
It is a partial agonist at the D 2 and 5-HT 1A receptors and an antagonist at the 5-HT 2 receptor. (psychiatrist.com)
The antipsychotic is a partial agonist at serotonin 5-HT 1A and dopamine D 2 receptors and is an antagonist at serotonin 5-HT 2A and noradrenaline receptors, "all at subnanomolar potency," note the investigators. (medscape.com)
Some evidence has indicated 5-HT and its receptors regulate the cognitive functions, including learning and memory ( 4 - 7 ). (frontiersin.org)
The 5-HT 1A receptors can influence the activity of cholinergic, glutamatergic and GABAergic neurons in the cerebral cortex and hippocampus to affect the declarative and non-declarative memory. (frontiersin.org)
And the 5-HT 1A receptors regulate several transduction mechanisms in the memory formation. (frontiersin.org)
Brexpiprazole is a serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at 5-HT 1A and dopamine D 2 receptors, and an antagonist at 5-HT 2A and noradrenaline alpha 1B/2C receptors. (otsuka.co.jp)
Ziprasidone functioned as a selective antagonist at the D 2 , 5HT 2A , and 5HT 1D receptors, and also as an agonist at the 5HT 1A receptor. (tcichemicals.com)
Activity at 5-HT 2 , H 1 and α 2 receptors. (abcam.com)
The hypophagic effect was not dependent on the interaction with 5-HT 1A receptors. (bvsalud.org)

GSK163090 is a potent, selective and orally active 5-HT 1A/1B/1D receptor antagonist with pK i values of 9.4/8.5/9.7, respectively. (medchemexpress.com)
abstract = "Background and purpose: The antidepressant efficacy of selective 5-HT reuptake inhibitors (SSRI) and other 5-HT-enhancing drugs is compromised by a negative feedback mechanism involving 5-HT1A autoreceptor activation by the excess 5-HT produced by these drugs in the somatodendritic region of 5-HT neurones. (uab.cat)
4 , 5 Previous evidences suggest that selective serotonin reuptake inhibitors (SSRIs), including paroxetine, 6 - 9 sertraline, 10 , 11 citalopram, 12 and escitalopram, 13 , 14 are effective in the treatment of GAD. (dovepress.com)
DESYREL (trazodone hydrochloride) tablets for oral administration contain trazodone hydrochloride, a selective serotonin reuptake inhibitor and 5HT2 receptor antagonist . (rxlist.com)
Hypersensitivity reactions, such as anaphylaxis, shortness of breath, hypotension, and urticaria, may occur in patients with known hypersensitivity to other selective 5-HT 3 receptor antagonists. (nih.gov)
Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT 1A/B/D Receptor Antagonist. (donga.ac.kr)
Potent, non-competitive and non-selective 5-HT 2 antagonist. (abcam.com)
Non-selective receptor antagonist. (abcam.com)

It is hypothesized that the partial agonist and antagonist activities of brexpiprazole at multiple serotonergic, dopaminergic, and noradrenergic receptor systems may have a therapeutic benefit" in AD-related agitation, they write. (medscape.com)
The experimental subjects (rats) were assigned to one of four treatments: to Sham group saline was given, to group ADX saline was applied, the group 8-OH-DPAT was provided with 8-OH-DPAT (5-HT 1A agonist) and the pretreated group received 5-HT 1A antagonist WAY100635 + 8-OHDPAT. (bvsalud.org)

5-HT1A receptor antagonists augment antidepressant-like effects in rodents by preventing this negative feedback, and the mixed β-adrenoceptor/5-HT1A receptor antagonist pindolol improves clinical antidepressant effects by preferentially interacting with 5-HT 1A autoreceptors. (uab.cat)

Also a very potent α 2C adrenergic receptor antagonist. (chemicalbook.com)
Potent H 1 and 5-HT 2B antagonist. (abcam.com)

Ziprasidone hydrochloride monohydrate is a benzisothiazolyl piperazine-type atypical antipsychotic that shares the serotonin 2A /dopamine 2 (5-HT 2A /D 2 ) profile of the atypical antipsychotics. (tcichemicals.com)

It antagonized suppression of 5-hydroxytryptaminergic activity evoked by 8-OH-DPAT and SSRIs in vivo. (uab.cat)
Electroencephalograms (EEGs), spatial learning and memory, and mRNA and protein expression of 5-HT 1A receptor were evaluated in vivo . (frontiersin.org)

[1] If this is not sufficient, a serotonin antagonist such as cyproheptadine may be used. (wikipedia.org)

Experimental approach: We characterized the pharmacological properties of the 5-HT1A receptor antagonist DU-125530 using receptor autoradiography, intracerebral microdialysis and electrophysiological recordings. (uab.cat)

Transcriptional activity of 5-HT 1A receptor promoter containing rs198585630 C/T allele was determined in vitro . (frontiersin.org)

British Journal of Pharmacology , 167 (5), 1021-1034. (uab.cat)

May increase the dose by 5 mg/day every 2 to 3 days as needed. (pdr.net)

We demonstrated that transcriptional activity of 5-HT 1A receptor promoter containing rs198585630 C allele was higher than that of 5-HT 1A receptor promoter containing T allele. (frontiersin.org)
The transcriptional activity of 5-HT 1A receptor promoter was stimulated by 30 mW/cm 2 microwave exposure, and rs198585630 C allele was more sensitive to microwave exposure, as it showed stronger transcriptional activation. (frontiersin.org)
Rats carrying rs198585630 C allele exhibited increased mRNA and protein expression of 5-HT 1A receptor and were more susceptible to 30 mW/cm 2 microwave exposure, showing cognitive deficits and inhibition of brain electrical activity. (frontiersin.org)

The 5-HT receptor family includes at least 7 classes (5-HT 1−7 receptor) and 15 subtypes with different functional and transduction properties. (frontiersin.org)

The main mechanism underlying the modulatory effects of 5-HT is an alteration in 5-HT receptor density during memory formation and in amnesic states ( 8 , 9 ). (frontiersin.org)

These findings suggest SNP rs198585630 of the 5-HT 1A receptor is an important target for further research exploring the mechanisms of hypersensitivity to microwave exposure. (frontiersin.org)

The 5-HT 1A subtype is of particular interest since it plays an important regulatory role in the 5-HT system as one of the main mediators of the action of 5-HT and a potential target for enhancing cognition ( 8 , 10 - 12 ). (frontiersin.org)

Novel Spirotetracyclic Zwitterionic Dual H1/5-HT2AReceptor Antagonists for the Treatment of Sleep Disorders. (donga.ac.kr)

JPET articles become freely available 12 months after publication, and remain freely available for 5 years. (aspetjournals.org)

Multiple receptor antagonist. (abcam.com)

1. Any supposedly legitimate drug bought on line may look like the real thing, but it is all-too-often laced with fentanyl which can kill someone in 5 minutes. (bipolarnews.org)

In a study of pediatric patients with an anxiety disorder, doses of 5 to 30 mg PO twice daily were safe and well-tolerated in adolescents (n = 12). (pdr.net)

An involvement of 5-HT(1A) receptors is postulated in the pathophysiology of affective disorders and mechanism of action of antidepressants. (nih.gov)
Preliminary data suggests that activation of somatodendritic 5-HT(1A) receptors cause a negative shift in the EEG frequency spectrum. (nih.gov)
Animal research suggests that pindolol is an agonist at these receptors but an antagonist at postsynaptic 5-HT(1A) receptors. (nih.gov)
The data obtained are consistent with the EEG effects of buspirone and pindolol being mediated by somatodendritic 5-HT(1A) receptors, in contrast to the neuroendocrine response, which is known to be mediated by postsynaptic receptors. (nih.gov)
The development of this novel method of assessing somatodendritic 5-HT(1A) receptors in humans is a potentially important advance which may allow the testing of hypotheses of its involvement in depression and response to antidepressants. (nih.gov)
In 1995-1996, Dr. Pike introduced the first effective radiotracers for imaging 5-HT 1A receptors in human brain, first [ methyl - 11 C]WAY-100635 13 and second [ carbonyl - 11 C]WAY-100635 14 . (nih.gov)
23 The uptake in skull is troublesome for quantifying 5-HT 1A receptors in adjacent tissue (e.g. neocortex) because of "spillover" of radioactivity through the partial volume effect. (nih.gov)
Under these circumstances, brain 5-HT 1A receptors were clearly imaged, whereas they were unseen in the baseline experiment. (nih.gov)
Mirtazapine is a potent antagonist of 5-HT 2 and 5-HT 3 receptors. (nih.gov)
Mirtazapine has no significant affinity for the 5-HT 1A and 5-HT 1B receptors. (nih.gov)
Mirtazapine is a potent antagonist of histamine (H 1 ) receptors, a property that may explain its prominent sedative effects. (nih.gov)
Mirtazapine is a moderate antagonist at muscarinic receptors, a property that may explain the relatively low incidence of anticholinergic side effects associated with its use. (nih.gov)
Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. (nih.gov)
During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT 3 receptors. (nih.gov)
Animal studies demonstrate that, in binding to 5-HT 3 receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. (nih.gov)
[5] [6] Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes. (wikipedia.org)
The involvement of 5-HT 1A receptors in the antiaggressive actions of these drugs was confirmed by showing that the selective 5-HT 1A receptor antagonist WAY-100635 ( N -[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]- N -(2-pyridinyl)cyclohexanecarboxamide trihydrochloride), which was inactive alone, fully prevented the antiaggressive effects of alnespirone, 8-OH-DPAT, and buspirone and partly reversed those of ipsapirone and eltoprazine. (aspetjournals.org)
These selective antiaggressive actions of alnespirone are mediated by stimulating 5-HT 1A receptors, presumably the somatodendritic autoreceptors at the raphe nuclei. (aspetjournals.org)
Furthermore, the data provide evidence for a major involvement of these 5-HT 1A receptors in the modulation of aggressive behavior by 8-OH-DPAT, ipsapirone, buspirone, and eltoprazine. (aspetjournals.org)
13 It is hypothesized that aripiprazole's efficacy is mediated through a combination of partial agonist activity at dopamine D 2 and 5-hydroxytryptamine (5-HT) 1A receptors and antagonist activity at 5-HT 2A receptors. (ahdbonline.com)
LSD and DOB: interaction with 5-HT2A receptors to inhibit NMDA receptor-mediated transmission in the rat prefrontal cortex. (neurotransmitter.net)
We conclude that phenethylamine and indoleamine hallucinogens may exert their hallucinogenic effect by interacting with 5-HT2A receptors via a Ca2+/CaM-KII-dependent signal transduction pathway as partial agonists and modulating the NMDA receptors-mediated sensory, perceptual, affective and cognitive processes. (neurotransmitter.net)
Consistent with our previous report and in contrast to activation of 5-HT2C or purinergic receptors, activation of 5-HT2A receptors had no effect on CHO/5-HT1B receptor function, although 5-HT2A receptor-mediated activation of PLA2 was measured. (neurotransmitter.net)
Interestingly, purinergic receptor-mediated inhibition of CHO/5-HT1B receptor function was blocked when 5-HT2A receptors were activated simultaneously. (neurotransmitter.net)
These data suggest that the lack of 5-HT2A mediated regulation of CHO/5-HT1B receptors may be due to activation of a third pathway (in addition to PLC and PLA2 pathways), which results in the inhibition of the production or the actions of a cyclooxygenase- dependent arachidonic acid metabolite. (neurotransmitter.net)
By using antagonists for AVP and OXT, we found that these peptides were binding primarily to V 1a and OXT receptors, respectively. (jneurosci.org)
Animal studies have also shown that diminished serotonin neurotransmission and activation of 5-HT 1A receptors were associated with faster ejaculation, whereas activation of 5-HT 2C and 5-HT 1B receptors delayed ejaculation [ 9 , 10 ]. (biomedcentral.com)
Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. (ncats.io)
Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. (ncats.io)
Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors. (ncats.io)
Animals studies indicate that conjoined CB1 cannabinoid receptors and 5-HT2A serotonin receptors mediate the painkilling properties of THC as well as THC's impact on short-term memory deficits. (hempsapa.com)
Reported initially in 2005, the discovery that CBD interacts directly with these (and other) 5-HT receptors hints at a broader relationship between the endocannabinoid and serotonergic systems that scientists are still uncovering. (hempsapa.com)
Flibansetrin has high affinity for serotonin receptors in the brain: it acts as an agonist on 5-HT1A and an antagonist on 5-HT2A. (banglanewsexpress.net)
In vivo, flibanserin binds equally to 5-HT1A and 5-HT2A receptors. (banglanewsexpress.net)
However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. (banglanewsexpress.net)
It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. (banglanewsexpress.net)
The hypophagic effect was not dependent on the interaction with 5-HT 1A receptors. (bvsalud.org)
Psychotropic activity may be due to partial agonist activity at dopamine D 2 and serotonin 5-HT 1A receptors and antagonist activity at the 5-HT 2A receptor. (drugguide.com)
It was speculated that there were two different receptors for 5-HT in the ileum: D receptors, which are blocked by dibenzyline, and M receptors, which are blocked by morphine. (nih.gov)
The binding of [ 3 H] 5-HT to 5-HT 1 receptors was shown to be displaced by spiperone in a biphasic manner, suggesting that what was termed the 5-HT 1 receptor might be a heterogeneous population of receptors. (nih.gov)
The receptors were called " 5-HT 1 -like," 5-HT 2 and 5-HT 3 . (nih.gov)
The development of potent selective antagonists and an agonist, 2-methyl-5-HT, provided useful tools for the pharmacological characterization of 5-HT 3 receptors. (nih.gov)

Here, we report the 3.5-angstrom crystal structure of mouse dopamine receptor D4 (DRD4) complexed with a subtype-selective antagonist, L745870. (elifesciences.org)

The [ 3 H]5-HT-binding site that showed high affinity for spiperone was termed the 5-HT 1A subtype, whereas the component of [ 3 H]5-HT binding that showed low affinity for spiperone was called the 5-HT 1B subtype. (nih.gov)

These studies have shown that mirtazapine acts as an antagonist at central presynaptic α 2- adrenergic inhibitory autoreceptors and heteroreceptors, an action that is postulated to result in an increase in central noradrenergic and serotonergic activity. (nih.gov)
R ATIONALE: Buspirone is used as a neuroendocrine challenge in which the increase of circulating prolactin is taken as a measure of the sensitivity of central serotonergic (5-HT(1A)) pathways. (biopsychiatry.com)

The development of potent and selective antagonists of the 5-HT 2 receptor, such as ketanserin, facilitated the assignment of certain effects mediated by 5-HT to the 5-HT 2 receptor. (nih.gov)

OBJECTIVE: To characterise the dual action of buspirone in stimulating the secretion of prolactin by blocking the 5-HT(1A) action with the 5-HT1A antagonist action of pindolol. (biopsychiatry.com)
METHODS: Healthy male subjects (n=35) received buspirone (0.5 mg x kg bw(-1) orally) with and without pre-treatment with the 5-HT(1A) receptor antagonist pindolol (40 mg over 2 days, 0.5 mg x kg bw(-1) on test day). (biopsychiatry.com)
However, if two challenges are carried out, one with buspirone and the other with buspirone plus pindolol, quantitative measures can be made of the sensitivity of both the 5-HT(1A) and the putative D(2) pathways controlling prolactin release. (biopsychiatry.com)

Mirtazapine is a moderate peripheral α 1- adrenergic antagonist, a property that may explain the occasional orthostatic hypotension reported in association with its use. (nih.gov)

The 5-HT 1A autoreceptor-mediated inhibition did not develop until P21. (jneurosci.org)

After radial-arm acquisition training, we assessed the role of 5HT by challenging the animals with the 5HT 2 receptor antagonist ketanserin. (nih.gov)
Although short-term (i.e., 10 min) 5-HT and ketanserin exposure resulted in the same degree of desensitization, ketanserin-induced desensitization was not prevented by these agents and did not involve receptor internalization. (neurotransmitter.net)
5-HT2A receptor desensitization induced by 5-HT and prolonged ketanserin treatment, but not by short-term ketanserin treatment, was prevented by the expression of the dominant negative mutant of G protein-coupled receptor kinase (GRK)2, GRK2-K220R, and by an anti-GRK2/3 antibody. (neurotransmitter.net)

The increased excitability was due to depolarized resting membrane potential, increased resistance, increased firing rate, lack of 5-HT 1A autoreceptor response, and lack of GABA synaptic activity. (jneurosci.org)

The data clearly indicate that alnespirone effectively suppresses offensive aggression with an advantageous profile of action compared with other full or partial 5-HT 1A agonists. (aspetjournals.org)

Few highly selective ligands are commercially available for the 5-HT 5A receptor. (wikipedia.org)

Animal studies suggest that some of the metabolites may also have 5-HT 3 receptor antagonist activity. (nih.gov)

The serotonin subtype-1A (5-HT 1A ) receptor is one of the most extensively studied, especially because specific agonists and antagonists exist, and because it is a target for therapy in various neuropsychiatric disorders, notably depression. (nih.gov)
Rodents have been shown to possess two functional 5-HT 5 receptor subtypes, 5-HT 5A and 5-HT 5B , [9] however while humans possess a gene coding for the 5-HT 5B subtype, its coding sequence is interrupted by stop codons, making the gene non-functional, and so only the 5-HT 5A subtype is expressed in human brain. (wikipedia.org)
These [ 3 H]5-HT-binding sites were termed the 5-HT 1C subtype as they did not show the pharmacological characteristics used to classify the 5-HT 1A , 5-HT 1B or 5-HT 2 binding sites. (nih.gov)

The neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) has been implicated in a wide range of psychiatric conditions and also has vasoconstrictive and vasodilatory effects. (wikipedia.org)

4 , 5 These results contrast sharply with prior trials conducted outside the United States, in which 5- and 10-mg doses demonstrated efficacy over placebo in adults with MDD, 6-8 and 1 trial in which vortioxetine 10-20 mg/d proved superior to agomelatine in treatment-resistant MDD. (psychiatrist.com)

Conserved as an evolutionary through-line in all bilateral animals, including worms and insects, the serotonin molecule modulates the release of a swathe of other neurotransmitters.2 Serotonin (which is often abbreviated as 5-HT because of its proper chemical name 5-hydroxytryptamine) is involved in behaviors as diverse as aggression, learning, appetite, sleep, cognition, and reward activity. (hempsapa.com)

The 5-HT 1D receptor was identified by pharmacological criteria only in brains of species devoid of the 5-HT 1B receptor, such as pig, cow, guinea pig and human. (nih.gov)

5 This has resulted in an alarming increase in opioid addiction and overdose deaths. (nih.gov)

5-Hydroxytryptamine (serotonin) receptor 5A , also known as HTR5A , is a protein that in humans is encoded by the HTR5A gene . (wikipedia.org)

Additional mutagenesis studies suggest that the antagonist L745870 prevents DRD4 activation by blocking the relative movement between transmembrane helices 2 and 3. (elifesciences.org)
In conclusion, these data suggest that 5-HT2A receptor activation can amplify cAMP formation in A1A1 cells by two distinct pathways coupled to the hydrolysis of inositol phosphates, i.e. (neurotransmitter.net)

But CBD and LSD act at 5-HT2A, the psychedelic receptor, in different ways, resulting in markedly different effects. (hempsapa.com)

The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins , negatively influencing cAMP levels via G i and G o . [7] This protein has been shown to function in part through the regulation of intracellular Ca 2+ mobilization. (wikipedia.org)

Two distinct serotonin receptor binding sites - 5-HT1 and 5-HT2 (later renamed 5-HT1A and 5-HT2A) - were identified in the rat brain in 1979. (hempsapa.com)
Subsequently, a fourth binding site for [ 3 H]5-HT was identified in bovine brain and called the 5-HT 1D receptor. (nih.gov)

Many subsequent experiments have shown that the D receptor and the 5-HT 2 receptor are pharmacologically indistinguishable. (nih.gov)

The overall distribution of radioactivity is consistent with high specific binding to 5-HT 1A receptor-rich regions. (nih.gov)
A high density of binding sites for [ 3 H]5-HT was found in the choroid plexus. (nih.gov)

Serotonin [5-hydroxytryptomine(5-HT)] likely plays a critical role in the etiology of anxiety and mood disorders as drugs that affect 5-HT physiology (e.g., selective serotonin reuptake inhibitors) are among the most efficacious in treating such disorders ( Koen and Stein, 2011 ) and have anxiolytic properties in rodent anxiety models ( Carr and Lucki, 2011 ). (jneurosci.org)

27). Although potent 5-HT 1A antagonists were found by this approach, 27,28 this strategy failed to provide a superior radiotracer, as assessed by PET experiments in cynomolgus monkey. (nih.gov)

Taken together, the results suggest that CUMI-101 is a potent 5-HT1A receptor antagonist with significant, regional-dependent cross-reactivity with the α1A receptor. (nih.gov)

[5] The 5-HT 5A receptor has been shown to be functional in a native expression system. (wikipedia.org)

Anatomy11

Organisms9

Diseases1

Chemicals and Drugs203

Analytical, Diagnostic and Therapeutic Techniques and Equipment11

Psychiatry and Psychology2

Phenomena and Processes17

Disciplines and Occupations1

Information Science2

Health Care1

Receptors22

Selective8

Agonist2

Autoreceptors1

Potent2

Antipsychotic1

Vivo2

Cyproheptadine1

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Vitro1

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Dose1

Activity3

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Drug1

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Receptors42

Dopamine1

Affinity1

Serotonergic2

Selective antagonists1

Buspirone3

Adrenergic1

Inhibition1

Ketanserin3

Autoreceptor1

Partial1

Ligands1

Metabolites1

Subtype3

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