Relation Results

Summary

Name HTR1B
Full Name 5-hydroxytryptamine receptor 1B
Synonyms 5-HT-1B, 5-HT1B, S12, Serotonin 1D beta receptor, 5-HT-1D-beta, Serotonin receptor 1B | HTR1DB
Primary ID P28222
Links - -
Type protein
Relations 18
Inhibitors sertindole; paliperidone; risperidone; zotepine; pipamperone
Function G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and an ...
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Type: Score: Layout: SPV 
0.80.80.80.4130.80.4440.80.80.80.470.80.80.80.80.80.2520.2520.8oxymetazolineHTR1Bsertindoleserotonin(1+)GNAI3clozapineGNAI1paliperidoneserotoninziprasidoneGNAO1(S,S)-asenapinerisperidoneolanzapinefrovatriptanzotepineGNA14GNAZpipamperone

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Relations
Regulator
Mechanism
target
score ℹ
+ oxymetazolineup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258928 Bos taurus
pmid sentence
Benzylimidazolines may represent a class of 5-HT1D ligands that has yet to be exploited. On the basis of a previous report that the 2-(substituted-benzyl)imidazoline alpha-adrenergic agonist oxymetazoline (8) binds with high affinity at calf brain 5-HT1D receptors, we explored the structure-affinity relationships of a series of related derivatives.
Publications: 1 Organism: Bos Taurus
Tissue: Brain
+ sertindoledown-regulates activity img/direct_inhibition.png chemical inhibition HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258545 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ serotonin(1+)up-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257517 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ HTR1Bup-regulates activity img/direct-activation.png binding GNAI3 0.413
Identifier Residue Sequence Organism Cell Line
SIGNOR-256863 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ clozapineup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258519 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ HTR1Bup-regulates activity img/direct-activation.png binding GNAI1 0.444
Identifier Residue Sequence Organism Cell Line
SIGNOR-256720 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ paliperidonedown-regulates activity img/direct_inhibition.png chemical inhibition HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258560 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ serotoninup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-264284 Homo sapiens Neuron
pmid sentence
Serotonin or 5-hydroxytryptamine (5-HT) remains one of the most widely studied chemical messengers. Serotonin produces a myriad of physiological effects in humans, mediated through 14 distinct receptor subtypes, of which 13 are G protein coupled receptors (GPCRs), and one ligand-gated cation channel
Publications: 1 Organism: Homo Sapiens
+ ziprasidoneup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258501 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ HTR1Bup-regulates activity img/direct-activation.png binding GNAO1 0.47
Identifier Residue Sequence Organism Cell Line
SIGNOR-256999 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ (S,S)-asenapineup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258567 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
+ risperidonedown-regulates activity img/direct_inhibition.png chemical inhibition HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258526 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ olanzapineup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258507 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ frovatriptanup-regulates activity img/direct-activation.png chemical activation HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259075 in vitro
pmid sentence
As far as the selectivity against the 5-HT1A receptor, compound 10 shows similar selectivity as VML-251 (4) but has slightly lower selectivity as compared to sumatriptan (1), naratriptan (2), and rizatriptan (3). Although none of the 5-HT1D receptor agonists in the current study demonstrate as good selectivity versus the 5-HT1B receptor, the N-methyl-5-tert-butyltryptamine (10) remains the most selective (4-fold).
Publications: 1 Organism: In Vitro
+ zotepinedown-regulates activity img/direct_inhibition.png chemical inhibition HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258554 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
+ HTR1Bup-regulates activity img/direct-activation.png binding GNA14 0.252
Identifier Residue Sequence Organism Cell Line
SIGNOR-257207 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ HTR1Bup-regulates activity img/direct-activation.png binding GNAZ 0.252
Identifier Residue Sequence Organism Cell Line
SIGNOR-257115 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ pipamperonedown-regulates activity img/direct_inhibition.png chemical inhibition HTR1B 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258573 Rattus norvegicus
pmid sentence
Risperidone and its active metabolite 9-OH-risperidone were compared to reference antipsychotic drugs (haloperidol, pipamperone, fluspirilene, clozapine, zotepine) and compounds under development (olanzapine, seroquel, sertindole, ORG-5222, ziprasidone) for in vitro binding to neurotransmitter receptors in brain tissue and on membranes of recombinant cells expressing cloned human receptors and for in vivo occupancy of neurotransmitter receptors in rat and guinea-pig brain following acute treatment (2 h., s.c.). The binding affinities of the compounds for various neurotransmitter receptors were measured using membrane preparations of animal brain regions and of recombinant cells expressing cloned, mostly human receptors. Receptors, tissues and cells are indicated in Table I; results are shown in Table 4A-B.
Publications: 1 Organism: Rattus Norvegicus
Tissue: Corpus Striatum
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