Receptor serotonin 5 ht1b. Medical search. Frequent questions

Agonist radioligand [3H]5-HT binding studies showed that the expressed 5-HT1B and m5-HT1B receptors displayed the characteristic pharmacological profile of the neuronal 5-HT1B receptor. (nih.gov)
Indeed, agonist binding to the high-affinity receptor state was regulated in the presence of GTP gamma S, Gpp(NH)p, and pertussis toxin. (nih.gov)
It acts as a 5-HT1A and 5-HT1B receptor agonist. (wikipedia.org)
A selective novel KOP receptor agonist emerged as a notable result and is proposed as a new chemotype for the study of the KOP receptor in the etiology of drug addiction, depression, and/or pain. (acs.org)
Naratriptan tablets are a serotonin (5-HT 1B/1D ) receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. (nih.gov)
It is the seventh serotonin 5-HT1B/1D-receptor agonist (triptan) to be approved by the FDA for this indication. (medletter.com)
We therefore tested the hypothesis that 5-HT 1B receptors might also be located on SCN GABAergic terminals by examining the effects of the highly selective 5-HT 1B receptor agonist CP-93,129 on SCN miniature inhibitory postsynaptic currents (mIPSCs). (unl.edu)
The decrease in the frequency of mIPSCs of SCN neurons produced by the selective 5-HT 1B receptor agonist CP-93,129 is consistent with the interpretation that 5-HT 1B receptors are located on GABA terminals in the SCN and that 5-HT inhibits GABA release via a 5-HT 1B presynaptic receptor-mediated mechanism. (unl.edu)
Frovatriptan succinate (trade name Frova) is a selective 5-hydroxytryptamine1 (5-HT1B/1D) receptor subtype agonist, and is used for the treatment of migraine attacks with or without aura in adults. (ncats.io)
The substance tested by the team, eltoprazine, is a so-called serotonin receptor agonist that targets receptor types 5-HT1A and 5-HT1B. (ki.se)
Besides, the 5-HT1BR agonist is also involved in the mechanisms underlying many neurological dysfunctions, making it a critical target for the rational development of drugs. (chemaxon.com)
We believe that our work is a first step using in silico quantum biochemical design as a means to influence the discovery of new drugs to treat migraine and other diseases related to the 5-HT1BR agonist. (chemaxon.com)
Zembrace® is a serotonin (5-HT1B/1D) receptor agonist (triptan) indicated for the acute treatment of migraine, with or without aura, in adults who have a clear migraine diagnosis. (migraine.com)
The therapeutic activity of zolmitriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on blood vessels in the brain and sensory nerves of the trigeminal system which result in vessel constriction and inhibition of proinflammatory neuropeptide release. (affygility.com)
5-HT 1B R agonist treatment induced an impairing effect on emotional memory in wild type (WT) mice. (uky.edu)
Unexpectedly, 5-HT 1B R agonist stimulation enhanced memory in p11KO mice, and this atypical switch was reversed after hippocampal adeno-associated virus mediated gene transfer of p11. (uky.edu)
Magnetic resonance spectroscopy demonstrated global hippocampal reductions of inhibitory GABA, which may contribute to the memory enhancement and potentiation of pre-and post-synaptic measures of glutamate transmission by a 5-HT 1B R agonist in p11KO mice. (uky.edu)
IMITREX is a 5-HT1B/1D serotonin receptor agonist (triptan) approved for the immediate treatment of migraines in adults with or without aura. (discretepills.com)
As a selective agonist of 5-hydroxytryptamine-1 (5-HT1) receptors in cranial arteries, zolmitriptan causes vasoconstriction and reduces the inflammation associated with antidromic neuronal transmission in CH. It can reduce the severity of headache within 15 minutes of subcutaneous injection. (medscape.com)
Rizatriptan is a selective agonist for 5-HT1 receptors in cranial arteries and suppresses the inflammation associated with migraine headaches. (medscape.com)
Almotriptan is a selective 5-HT1B/1D receptor agonist used to treat acute migraine. (medscape.com)
It is a selective 5-HT 1B/1D receptor agonist with a long half-life (24 hours) and a low headache recurrence rate within 24 hours after taking the drug. (medscape.com)
Eletriptan is a selective serotonin agonist that specifically acts at 5-HT 1B/1D/1F receptors on intracranial blood vessels and sensory nerve endings to relieve pain associated with acute headaches. (medscape.com)

Measurements of adenylyl cyclase activity in membranes from cells expressing m5-HT1B receptors showed that serotonergic agonists mediated the inhibition of adenylyl cyclase activity with a rank order of potency comparable to their affinity constants. (nih.gov)
Kappa-opioid (KOP) receptor agonists exhibit analgesic effects without activating reward pathways. (acs.org)
Agonists at serotonin 1D (5-HT 1D ) receptors relieve migraine headache but are not clinically used as general analgesics. (jneurosci.org)
The introduction of agonists that activate serotonin 1B (5-HT 1B ) and 5-HT 1D receptors (the "triptans") has revolutionized treatment for many migraineurs. (jneurosci.org)
Sumatriptan is part of a class of medications called 'triptans', which belong to a group of drugs called serotonin agonists. (headacheaustralia.org.au)
Earlier research on animal models for Parkinson's conducted by Anders Björklund , professor of histology at Lund University , and Per Svenningsson , professor of neurology at Karolinska Institutet, showed promising results using serotonin receptor agonists against L-dopa-induced hyperkinesia, and have prompted the researchers to examine if the principle also operates in humans. (ki.se)
Since the early days of migrainous research, serotonin receptors (5-HTR) have been considered a major target of drugs, and the 5-HT1B and 5-HT1D agonists have been among the most marketed ones for the treatment of migraine attacks. (chemaxon.com)
Rizatriptan Stada belongs to a class of medicines called selective 5-HT 1B / 1D serotonin receptor agonists. (zeepedia.com)

Selective 5-HT(1B/1D), 5-HT(2A), and 5-HT(2B) receptor antagonists were used for comparative testing. (hal.science)

Predictive Models to Identify Small Molecule Activators and Inhibitors of Opioid Receptors. (acs.org)
Serotonin selective reuptake inhibitors (SSRIs), medications commonly prescribed for anxiety and depression, compensate for reduction in serotonin signaling by boosting levels and binding of serotonin to receptors. (scienceblog.com)

Using CsCl-containing microelectrodes with QX314, we isolated mPSCs that were sensitive to the GABA A receptor antagonist, bicuculline. (unl.edu)
Dihydroergotamine has alpha-adrenergic antagonist and serotonin antagonist effects. (medscape.com)
Ergotamine has alpha-adrenergic antagonist and serotonin antagonist effects and causes constriction of peripheral and cranial blood vessels. (medscape.com)

This numerical discrepancy may have distinct functional implications for how triptans modulate afferent activity and emphasizes the importance of knowing the neurochemical properties of the primary afferents bearing the triptan receptors. (jneurosci.org)

Ergotamine and its derivatives work by activating the 5-HT1D receptors, causing vasoconstriction of intracranial blood vessels and inhibiting the release of inflammatory neuropeptides. (pharmacytimes.com)
When the 5-HT 1B receptor is activated, it helps to constrict (narrow) your blood vessels. (headacheaustralia.org.au)
Zembrace is believed to work by binding with 5-HT1B/1D receptors on blood vessels in the brain. (migraine.com)

Axonal release of serotonin (5-hydroxytryptamine, 5-HT) in the CNS is typically regulated by presynaptic 5-HT autoreceptors. (ox.ac.uk)
5-HT 1B Receptor-Mediated Presynaptic Inhibition of GABA Rel" by Jayne R. Bramley, Patricia J. Sollars et al. (unl.edu)
The suprachiasmatic nucleus (SCN) receives a dense serotonergic innervation that modulates photic input to the SCN via serotonin 1B (5-HT 1B ) presynaptic receptors on retinal glutamatergic terminals. (unl.edu)
The 5-HT 1B receptor (5-HT 1B R) regulates serotonin transmission, via presynaptic receptors, but can also affect transmitter release at heterosynaptic sites. (uky.edu)

The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. (osenses.com)
The expressed receptors displayed both high- and low-affinity states for [3H]5-HT, suggesting that the receptors were coupled to endogenous G-proteins. (nih.gov)
To explore how a particular serotonin receptor (5-HT1B) functions, Greengard and colleagues conducted tests to find out what proteins these receptors interact with in brain cells. (scienceblog.com)
Activation of the 5HT 1D receptor stops these proinflammatory proteins from being released. (headacheaustralia.org.au)

Ligand binding activates second messengers that inhibit the activity of adenylate cyclase and manage the release of serotonin, dopamine, and acetylcholine in the brain. (abbkine.com)

Figure S1: Plot of competitive inhibition of 3 H -diprenorphine binding at the KOP receptor. (acs.org)
Figure S3 shows the cAMP accumulation inhibition curves at DOP and MOP receptors. (acs.org)
Prejunctional activation of α2A/2C-adrenergic, serotonin 5-HT1B/1F, or dopamine D2-like receptors results in inhibition of this CGRPergic outflow. (eur.nl)
Since DHE displays affinity for these receptors, this study investigated the pharmacological profile of DHE-induced inhibition of the vasodepressor sensory CGRPergic outflow. (eur.nl)
Conclusion: DHE-induced inhibition of the vasodepressor sensory CGRPergic outflow is mainly mediated by prejunctional rauwolscine-sensitive α2-adrenoceptors and GR127935-sensitive 5-HT1B/1D receptors, which correlate with α2A/2C-adrenoceptors and 5-HT1B receptors, respectively. (eur.nl)
Serotonin transporter inhibition prevents and reverses monocrotaline-induced pulmonary hypertension in rats. (hal.science)
The effect of serotonin receptor 5-HT1B on lateral inhibition between spiny projection neurons in the mouse striatum. (ac.be)

MDMA, a potent monoamine-releaser with particularly pronounced serotonin- releasing properties, has unique subjective effects that include: marked positive mood, pleasant/unusual bodily sensations and pro-social, empathic feelings. (researchgate.net)

Mapping the distribution of serotonin transporter in the human brainstem with high-resolution PET: Validation using postmortem autoradiography data. (ki.se)
BACKGROUND: Progression of pulmonary hypertension (PH) is associated with increased lung expression of the serotonin transporter (5-HTT), which leads to hyperplasia of the pulmonary artery smooth muscle cells (PA-SMCs). (hal.science)

Given the postulated causal relation between 5-HTT overexpression and PH, we herein investigated whether the highly selective 5-HTT inhibitor fluoxetine prevented and/or reversed PH induced by monocrotaline (MCT) in rats. (hal.science)

Journal of Medicinal Chemistry 2021 , 64 (5) , 2489-2500. (acs.org)

The researchers also examined the effect of treatments designed to boost weak serotonin systems on p11 levels in brain cells by administering to mice two types of antidepressants - a tricyclic, a monoamine oxidase (MAO) inhibitor - and electroconvulsive therapy (ECT). (scienceblog.com)
Compared to control mice, knockout mice had fewer receptors at the cell surface, reduced serotonin signaling, decreased responsiveness to sweet reward, and were less mobile, behaviors which are considered depression-like. (scienceblog.com)
Also, the 5-HT1B receptors of p11 knockout mice were less responsive to serotonin and antidepressant drugs compared to those of control mice, which further implicates p11 in the main action of antidepressant medications. (scienceblog.com)
In mice lacking functional 5-HT 1B receptors, CP-93,129 (1 mM) had no clear effect on the frequency or the amplitude of mIPSCs recorded in any of the cells tested ( n = 4). (unl.edu)
This study aimed at investigating the roles of the 5-HT 1B R, and its adapter protein p11, in emotional memory and object recognition memory processes by the use of p11 knockout (p11KO) mice, a genetic model for aspects of depression-related states. (uky.edu)
Notably, 5-HT 1B R stimulation increased glutamatergic neurotransmission in the hippocampus in p11KO mice, but not in WT mice, as measured by both pre-and postsynaptic criteria. (uky.edu)

Most Axon Ligands™ in this category of compounds are labeled antipsychotic (typical, or atypical), since many of the common drugs to treat this class of mental disorders show affinity for both dopaminergic and serotonergic receptors (among several others). (axonmedchem.com)
Table S2: Details of the 500 top-scoring docked compounds from virtual screening at the KOP receptor. (acs.org)

a few axons penetrate to lamina V. At the ultrastructural level, 5-HT 1D receptors in the spinal cord dorsal horn are localized exclusively within dense core vesicles of synaptic terminals. (jneurosci.org)

The suppression involved the ability of male flies to detect females by contact chemosensation through the pheromone-sensing ion channel ppk29 and was mediated by male-specific GABAergic neurons acting on the GABAA receptor RDL in target cells. (nih.gov)
We also examined the neurochemical identity of 5-HT 1D -IR neurons with markers of primary afferent nociceptors, peripherin, isolectin B4, and substance P, and markers of myelinated afferents, N52 and SSEA3. (jneurosci.org)
We observed a striking similarity in the size, distribution, and neurochemical identity of 5-HT 1D -IR neurons in TRG and lumbar DRG afferents. (jneurosci.org)
Furthermore, the vast majority of 5-HT 1D -IR neurons are unmyelinated peptidergic afferents that distribute peripherally, including the dura, cornea, and the sciatic nerve. (jneurosci.org)
We observed scattered 5-HT 1D -IR neurons in the nodose ganglia, and there was sparse terminal immunoreactivity in the solitary nucleus. (jneurosci.org)

Based on a phylogenetic analysis, the family of serotonin (5-HT) receptors should be separated into two different classes among the subgroup of biogenic amine receptors of the rhodopsin-like family of GPCRs . (axonmedchem.com)
FUNCTION: This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. (osenses.com)

Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands. (axonmedchem.com)
A synthetic peptide from mouse 5HT1B receptor conjugated to blue carrier protein was used as the antigen. (osenses.com)
Analysis of the primary protein structure of the human serotonin1B (5-HT1B) receptor reveals consensus sites for phosphorylation and a putative site for palmitoylation. (nih.gov)
This newfound protein may provide a more specific target for new treatments for depression, anxiety disorders and other psychiatric conditions thought to involve malfunctions in the serotonin system," said NIH director Elias Zerhouni, M.D. (scienceblog.com)
The 5-hydroxytryptamine receptor 1B encoded by HTR1B is a G-protein coupled receptor for serotonin (5-hydroxytryptamine). (abbkine.com)
MCT-induced PH was also associated with increased expression of various cytokines, but only interleukin-1beta and monocyte chemotactic protein-1 increased at the early phase and stimulated 5-HTT expression by cultured PA-SMCs. (hal.science)
Furthermore, we predict the relevance (energetically) of the DHE regions, as well as the influence of each protein segment to DHE-serotonin receptor binding. (chemaxon.com)

Serotonin is a neurotransmitter involved in the regulation of many biological phenomena, such as satiation, sleep and mental wellbeing, as well as movement. (ki.se)

Previous studies have suggested that serotonin receptors are essential in regulating moods and in mediating the effects of SSRIs, but given the complexity of the serotonin system, exactly how these receptors work remains a mystery. (scienceblog.com)

Our finding, that 5-HT 1D receptors are distributed in nociceptors throughout the body, raises the possibility that triptans can regulate not only headache-associated pain but also nociceptive responses in extracranial tissues. (jneurosci.org)
Triptans work by activating your serotonin receptors, specifically the 5-HT 1B and 5HT 1D receptors (2). (headacheaustralia.org.au)

5-HT(1B) receptor regulation of serotonin (5-HT) release by endogenous 5-HT in the substantia nigra. (ox.ac.uk)
The SNr receives one of the highest densities of 5-HT innervation in mammalian brain and yet negative feedback regulation of axonal 5-HT release by endogenous 5-HT has not been identified here. (ox.ac.uk)
These data reveal that 5-HT release in SNr is not devoid of autoreceptor regulation by endogenous 5-HT, but rather is under modest control which only weakly limits 5-HT signaling. (ox.ac.uk)

The American Headache Society released a list of 5 commonly performed tests or procedures that are not always necessary in the treatment of migraine and headache, as part of the American Board of Internal Medicine (ABIM) Foundation's Choosing Wisely campaign. (medscape.com)

Serotonin syndrome: Discontinue naratriptan tablets if occurs. (nih.gov)

H(2)(15)O]-Positron Emission Tomography (PET) was used to examine regional cerebral blood flow (rCBF) after administration of a single oral dose of the serotonin realeaser and uptake inhibitor MDMA (1.7 mg/kg) or placebo to 16 MDMA-naïve subjects. (researchgate.net)
If the migraine returns or if the patient has only partial response, the dose may be repeated once after 4 hours, for a maximum dose of 5 mg in a 24 hour period. (nih.gov)
In the four-way crossover study, patients were given a single tablet of placebo and eltoprazine 2.5, 5 and 7.5 mg, alongside a challenge dose of levodopa that was 1.5 times that of their usual L-dopa dose. (ki.se)
It was found that a 5 mg and 7.5 mg dose of eltoprazine both significantly reduced the patients' dyskinesia. (ki.se)

We explored whether we could identify autoregulation of 5-HT release by 5-HT(1B) receptors in rat SNr slices using fast-scan cyclic voltammetry at carbon-fiber microelectrodes to detect 5-HT release evoked by discrete stimuli (50 Hz, 20 pulses) paired over short intervals (1-10 s) within which any autoreceptor control should occur. (ox.ac.uk)

Capmatinib is a small molecule kinase inhibitor targeted against c-Met (a.k.a. hepatocyte growth factor receptor [HGFR]), a receptor tyrosine kinase that, in healthy humans, activates signaling cascades involved in organ regeneration and tissue repair. (drugbank.com)

It is concluded that the level of hippocampal p11 determines the directionality of 5-HT 1B R action on emotional memory processing and modulates hippocampal functionality. (uky.edu)

furthermore, it inhibits the vasodepressor sensory CGRPergic outflow, but the receptors involved remain unknown. (eur.nl)

These data indicate that 5-HT release can activate a 5-HT(1B)-receptor autoinhibition of subsequent release, which is mediated directly via 5-HT axons and not via GABAergic or histaminergic inputs. (ox.ac.uk)
However, the majority of 5-HT 1B binding sites in the SCN are located on nonretinal terminals and most axonal terminals in the SCN are GABAergic. (unl.edu)

Evoked 5-HT release exhibited short-term depression after an initial stimulus that recovered by 10 s. (ox.ac.uk)
He and his colleagues found that p11 appears to help regulate signaling of the brain messenger chemical serotonin, a key target of antidepressants, which has been implicated in psychiatric illnesses such as depression and anxiety disorders. (scienceblog.com)
This finding led the researchers to suspect that p11 levels might be directly involved in the development of depression, anxiety and similar psychiatric illnesses thought to involve faulty serotonin receptors. (scienceblog.com)
Cognitive impairments are common in depression and involve dysfunctional serotonin neurotransmission. (uky.edu)

They found that 5-HT1B interacts with p11, and according to Greengard, p11 plays a role in the recruitment of receptors to the cell surface where they are more functional. (scienceblog.com)

In the search for nonaddictive opioid therapeutics and novel chemical tools to study physiological functions regulated by the KOP receptor, we screened in silico its recently released inactive crystal structure. (acs.org)

5] Side effects of atypical antipsychotics: a brief overview. (axonmedchem.com)
A treatment study published in the journal Brain shows that a drug that stimulates certain serotonin receptors in the brain counteracts the dyskinesia causing effects of L-dopa. (ki.se)
Serotonin contributes to the spinal antinociceptive effects of morphine. (omeka.net)

Patterns of age related changes for phosphodiesterase type-10A in comparison with dopamine D2/3 receptors and sub-cortical volumes in the human basal ganglia: A PET study with 18F-MNI-659 and 11C-raclopride with correction for partial volume effect. (ki.se)

Anatomy17

Organisms5

Diseases4

Chemicals and Drugs122

Analytical, Diagnostic and Therapeutic Techniques and Equipment11

Psychiatry and Psychology10

Phenomena and Processes18

Disciplines and Occupations2

Anthropology, Education, Sociology and Social Phenomena1

Health Care1

Agonist23

Agonists8

Selective 5-HT 1B1

Inhibitors2

Antagonist3

Triptan1

Blood vessels3

Presynaptic4

Proteins4

Release of serotonin1

Inhibition7

Potent1

Transporter2

Rats1

20211

Mice6

Compounds2

Spinal cord1

Neurons5

Biogenic2

Protein7

Neurotransmitter1

SSRIs1

Triptans2

Endogenous3

Headache1

Naratriptan1

Dose4

Occur1

Activates1

Modulates1

Inhibits1

GABAergic2

Depression4

Functional1

Chemical1

Effects3

Human1