Page last updated: 2024-11-12

col-144

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

lasmiditan: a high-affinity, highly selective serotonin 5-HT(1F) receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11610526
CHEMBL ID3039520
SCHEMBL ID536057
MeSH IDM0553298

Synonyms (57)

Synonym
2,4,6-trifluoro-n-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide
L022410
CHEMBL3039520
ly573144
benzamide, 2,4,6-trifluoro-n-(6-((1-methyl-4-piperidinyl)carbonyl)-2-pyridinyl)-
2,4,6-trifluoro-n-(6-((1-methylpiperidine-4-yl)carbonyl)pyridin-2-yl)benzamide
760i9wm792 ,
col 144
lasmiditan [usan:inn]
lasmiditan
col-144
unii-760i9wm792
AKOS016000352
BCP9000841
439239-90-4
BCP0726000027
lasmitidan
lasmiditan (usan/inn)
D10338
2,4,6-trifluoro-n-(6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl)benzamide
2,4,6-trifluoro-n-{6-[(1-methylpiperidine-4-yl)carbonyl]pyridin-2-yl}benzamide
lasmiditan [mi]
lasmiditan [usan]
lasmiditan [who-dd]
lasmiditan [inn]
S5064
reyvow
gtpl3928
CS-2032
HY-14861
SCHEMBL536057
XEDHVZKDSYZQBF-UHFFFAOYSA-N
2,4,6-trifluoro-n-[6-(1-methylpiperidin-4-ylcarbonyl)-pyridin-2-yl]-benzamide
2,4,6-trifluoro-n-[6-(1-methyl-piperidin-4-ylcarbonyl)-pyridin-2-yl]-benzamide
2,4,6-trifluoro-n-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide
DTXSID40469435 ,
lasmiditan; ol-144; ly573144
EX-A1300
mfcd18633238
lasmiditan (col-144; ly573144)
DB11732
BCP04734
EX-A1653
AS-35247
Q6493750
SB19007
439239-90-4 (free base)
AMY27880
col-144; ly573144
2,4,6-tris(fluoranyl)-n-[6-(1-methylpiperidin-4-yl)carbonylpyridin-2-yl]benzamide
05x ,
EN300-18166794
lasmiditanum
dtxcid00203418
2,4,6-trifluoro-n-(6-((1-methylpiperidin-4-yl)carbonyl)pyridin-2yl)benzamide
bdbm50573975
AC-35661

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Lasmiditan penetrates the blood-brain barrier and CNS associated adverse events are common, but mostly in mild to moderate severity."( The safety and efficacy of the 5-HT 1F receptor agonist lasmiditan in the acute treatment of migraine.
Israel, H; Neeb, L; Raffaelli, B; Reuter, U, 2017
)
0.46
" Treatment-emergent adverse events (occurring within 48 hours of first dose) were considered in the analyses."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
" There were no deaths; serious adverse events were reported for seven patients (placebo, n = 2 [0."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
"As a centrally-penetrant drug, lasmiditan use was associated with neurologic treatment-emergent adverse events; most were mild or moderate in severity and self-limiting."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
" Rates of adverse events were similar for patients using and not using preventive medications."( Efficacy and safety of lasmiditan in patients using concomitant migraine preventive medications: findings from SAMURAI and SPARTAN, two randomized phase 3 trials.
Ailani, J; Baygani, S; Hundemer, HP; Krege, JH; Loo, LS; Port, M; Schim, J, 2019
)
0.51
" In patients whose first dose was lasmiditan, the incidence of treatment emergent adverse events (TEAEs) reported after the second dose was similar whether second dose was lasmiditan or placebo."( Effect of a rescue or recurrence dose of lasmiditan on efficacy and safety in the acute treatment of migraine: findings from the phase 3 trials (SAMURAI and SPARTAN).
Case, MG; Dowsett, SA; Krege, JH; Loo, LS; Plato, BM; Raskin, J; Turner, IM, 2019
)
0.51
" Overall, treatment-emergent adverse events (TEAEs) were similar to those in the single-attack studies and included dizziness (18."( Interim results of a prospective, randomized, open-label, Phase 3 study of the long-term safety and efficacy of lasmiditan for acute treatment of migraine (the GLADIATOR study).
Brandes, JL; Case, M; Khanna, R; Klise, S; Krege, JH; Kudrow, D; Pearlman, EM; Raskin, J; Vasudeva, R, 2019
)
0.51
"We explore factors that may have contributed to differences in treatment-emergent adverse events in the phase 2 and phase 3 lasmiditan clinical trials."( Issues Impacting Adverse Event Frequency and Severity: Differences Between Randomized Phase 2 and Phase 3 Clinical Trials for Lasmiditan.
Berg, PH; Hundemer, HP; Khanna, R; Krege, JH; Kudrow, D; Ossipov, MH; Pozo-Rosich, P, 2020
)
0.56
" Pain free and pain relief, global impression (very much/much better), and no/mild disability at 2 h in efficacy; total treatment-emergent adverse events (TEAEs), dizziness, nausea, fatigue, paraesthesia and somnolence in safety were extracted from the included studies."( Short-term efficacy and safety of lasmiditan, a novel 5-HT
Chen, J; Deng, D; Hou, M; Li, C; Li, J; Wang, X; Xing, H; Zhang, P, 2020
)
0.56
"This meta-analysis suggests that lasmiditan is effective for the acute treatment of migraine with a higher incidence of CNS-related adverse reactions compared with placebo."( Short-term efficacy and safety of lasmiditan, a novel 5-HT
Chen, J; Deng, D; Hou, M; Li, C; Li, J; Wang, X; Xing, H; Zhang, P, 2020
)
0.56
"DFN-15 treatment may be effective and safe for pain control in migraine patients."( The Efficacy and Safety of DFN-15 for the Treatment of Migraine: A Meta-Analysis of Randomized Controlled Studies.
Chen, Y; Deng, Y; Peng, Z; Yang, H,
)
0.13
" One patient in Cohort 2 discontinued due to adverse events."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62
" Outcomes included sustained pain freedom and -relief 2-48 hours post-dose, and adverse events."( Comparative efficacy and safety of rimegepant, ubrogepant, and lasmiditan for acute treatment of migraine: a network meta-analysis.
Coric, V; Croop, R; Dabirvaziri, P; Deighton, A; Harris, L; Johnston, K; L'Italien, G; Moren, J; Popoff, E; Thiry, A, 2022
)
0.72
" However, lasmiditan 200 mg was also associated with higher rates of adverse events, particularly somnolence and dizziness."( Comparative efficacy and safety of rimegepant, ubrogepant, and lasmiditan for acute treatment of migraine: a network meta-analysis.
Coric, V; Croop, R; Dabirvaziri, P; Deighton, A; Harris, L; Johnston, K; L'Italien, G; Moren, J; Popoff, E; Thiry, A, 2022
)
0.72
"These post hoc analyses evaluated the incidence of treatment-emergent adverse events (TEAEs) in elderly (≥65 years of age) versus nonelderly (<65 years of age) lasmiditan-treated patients."( Tolerability and Safety of Lasmiditan Treatment in Elderly Patients With Migraine: Post Hoc Analyses From Randomized Studies.
Ahmed, Z; Baygani, SK; Dong, Y; Hauck, PM; Hochstetler, HM; Khanna, R; Martin, VT, 2021
)
0.62
"Lasmiditan with the 50 mg, 100 mg, and 200 mg doses are effective and safe in acute migraine treatment."( The Effect and Safety of 5-HT
Chen, C; Dong, C; Dong, X; Gu, P; Wan, Q; Wang, T; Wu, Q, 2021
)
0.62
" The incidences of treatment-emergent serious adverse events (SAEs) were - placebo, n=2 (0."( Safety findings from CENTURION, a phase 3 consistency study of lasmiditan for the acute treatment of migraine.
Ardayfio, PA; Bragg, S; Doty, EG; Dowsett, SA; Krege, JH; Ruff, D; Schwedt, T; Tassorelli, C, 2021
)
0.62
" However, treatment-emergent adverse events (TEAEs) were more common than in global studies."( Safety profile of lasmiditan in patients with migraine in an Asian population.
Hirata, K; Khanna, R; Komori, M; Matsumori, Y; Ozeki, A; Tanji, Y, 2023
)
0.91
" There were no adverse consequences of neurological TEAEs, which did not appear to adversely affect lasmiditan efficacy."( Safety profile of lasmiditan in patients with migraine in an Asian population.
Hirata, K; Khanna, R; Komori, M; Matsumori, Y; Ozeki, A; Tanji, Y, 2023
)
0.91
"In controlled clinical trials, compared with placebo, a significantly greater proportion of participants using lasmiditan to treat a migraine attack achieved 2-h pain freedom (PF) and experienced ≥ 1 treatment-emergent adverse event (TEAE)."( The Association Between the Occurrence of Common Treatment-Emergent Adverse Events and Efficacy Outcomes After Lasmiditan Treatment of a Single Migraine Attack: Secondary Analyses from Four Pooled Randomized Clinical Trials.
Dong, Y; Doty, EG; Hake, AM; Hauck, PM; Komori, M; Krege, JH; Lipton, RB, 2022
)
0.72
" The incidence of treatment-emergent adverse events (TEAEs), their severity, and incidence by treated attacks for frequently reported TEAEs (≥ 5%) were evaluated."( Safety Findings in Lasmiditan as a Novel Acute Treatment of Migraine in Chinese Patients: A Post Hoc Analysis of the Randomized Controlled Phase 3 CENTURION Trial.
Dong, Z; Ji, F; Liu, H; Luo, G; Pan, X; Xu, Y; Yang, X; Yu, S; Zhong, S; Zhou, J, 2022
)
0.72
" No deaths and no study drug-related treatment emergent serious adverse events (TESAEs) were reported."( Safety Findings in Lasmiditan as a Novel Acute Treatment of Migraine in Chinese Patients: A Post Hoc Analysis of the Randomized Controlled Phase 3 CENTURION Trial.
Dong, Z; Ji, F; Liu, H; Luo, G; Pan, X; Xu, Y; Yang, X; Yu, S; Zhong, S; Zhou, J, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
"5-2 h post dose and then declined, with a terminal half-life of approximately 4 h in both cohorts."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
" Compared with placebo, more patients dosed with lasmiditan 200 mg were free of headache pain at 2 hours after dosing (32."( Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study.
Berg, PH; Dozier, G; Kuca, B; Lipton, RB; Silberstein, SD; Wietecha, L, 2018
)
0.48
"Lasmiditan dosed at 200 and 100 mg was efficacious and well tolerated in the treatment of acute migraine among patients with a high level of cardiovascular risk factors."( Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study.
Berg, PH; Dozier, G; Kuca, B; Lipton, RB; Silberstein, SD; Wietecha, L, 2018
)
0.48
" In phase 3, patients recorded in electronic diaries whether they experienced unusual feelings after dosing with lasmiditan that they had not felt with a migraine before, and were contacted to determine if an AE had occurred."( Issues Impacting Adverse Event Frequency and Severity: Differences Between Randomized Phase 2 and Phase 3 Clinical Trials for Lasmiditan.
Berg, PH; Hundemer, HP; Khanna, R; Krege, JH; Kudrow, D; Ossipov, MH; Pozo-Rosich, P, 2020
)
0.56
"The PK results support weight-based dosing of lasmiditan in pediatric patients with migraine and no new safety or tolerability issues were identified."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62
" Participants recorded their response to treatment prior to dosing and for 48 h postdose."( Phase 2 randomized placebo-controlled study of lasmiditan for the acute treatment of migraine in Japanese patients.
Homma, G; Katagiri, H; Komori, M; Sakai, F; Takeshima, T; Tanji, Y, 2021
)
0.62
" A statistically significant linear dose-response relationship for pain freedom was achieved at 2 h by a Cochran-Armitage trend test (p < 0."( Phase 2 randomized placebo-controlled study of lasmiditan for the acute treatment of migraine in Japanese patients.
Homma, G; Katagiri, H; Komori, M; Sakai, F; Takeshima, T; Tanji, Y, 2021
)
0.62
"05) for pain freedom at 2 h post dose across all patient subgroups and lasmiditan doses, except for CVRF (100 mg and 200 mg), migraine with aura (50 mg), triptan response (50 mg), and time to dosing (200 mg)."( Efficacy of Lasmiditan Across Patient and Migraine Characteristics in Japanese Patients with Migraine: A Secondary Analysis of the MONONOFU Trial.
Komori, M; Ozeki, A; Takeshima, T; Tanji, Y; Tatsuoka, Y, 2022
)
0.72
" This review provides tables of guidelines, including reduced dosing recommendations, for the use of abortive and preventative migraine medications in hepatic and renal failure."( Narrative review of migraine management in patients with renal or hepatic disease.
Chiang, CC; Datta, S; Garza, I; Robertson, CE; Stern, JI; Vieira, DL, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.59000.00010.532610.0000AID1855162
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.59200.00010.808710.0000AID1855164
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.59100.00010.54859.2100AID1855163
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.59400.00010.954910.0000AID1855067
5-hydroxytryptamine receptor 1FHomo sapiens (human)IC50 (µMol)0.08780.08781.94393.8000AID1771257
5-hydroxytryptamine receptor 1FHomo sapiens (human)Ki0.00220.00161.786510.0000AID1855157
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.59000.00030.380610.0000AID1855151
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.59300.00030.769310.0000AID1855160
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki0.59500.00080.94335.1600AID1855165
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of locomotion5-hydroxytryptamine receptor 1DHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1DHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1FHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1FHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1FHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1FHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
hippocampus development5-hydroxytryptamine receptor 5AHomo sapiens (human)
response to estradiol5-hydroxytryptamine receptor 5AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 5AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1FHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1FHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1FHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1DHomo sapiens (human)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
perikaryon5-hydroxytryptamine receptor 5AHomo sapiens (human)
postsynaptic specialization membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID1771266Bioavailability in Sprague-Dawley rat at 5 mg/kg, ig measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771265Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771260AUC(0 to t) in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855160Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1855151Binding affinity to 5-HT7 receptor (unknown origin)2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1771262Half life in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855164Binding affinity to 5-HT1D (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1771257Agonist activity at 5HT1F receptor (unknown origin) expressed in HEK293 cells measured after 60 mins by Fluo-4AM dye based FLIPR assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855165Binding affinity to 5-HT5A receptor (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1855067Binding affinity to 5-HT2C (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1771295Antimigraine activity against electrical stimulation of trigeminal ganglion migraine Wistar rat model assessed as reduction in dural plasma protein extravasation at 0.01 ug/kg, po measured after 45 mins by confocal fluorescence microscopic analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771263Half life in Sprague-Dawley rat at 5 mg/kg, ig measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771258Cmax in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855162Binding affinity to 5-HT1A (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1771264Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771267Antimigraine activity against electrical stimulation of trigeminal ganglion migraine Wistar rat model assessed as reduction in c-Fos-positive cells at 10 ug/kg, po measured after 60 mins by confocal fluorescence microscopic analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771259Cmax in Sprague-Dawley rat at 5 mg/kg, ig measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1771261AUC(0 to t) in Sprague-Dawley rat at 5 mg/kg, ig measured for 24 hrs by LC-MS/MS analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855163Binding affinity to 5-HT1B (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1771303Toxicity in NewZealand rabbit Saphenous vein rings assessed as induction of vasoconstriction at 0.01 to 100 uM2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID1855157Binding affinity to human 5-HT1F assessed as inhibition constant incubated for 10 mins by radioligand binding assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)2010Cephalalgia : an international journal of headache, Oct, Volume: 30, Issue:10
Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (92)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's26 (28.26)24.3611
2020's66 (71.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.61 (24.57)
Research Supply Index4.87 (2.92)
Research Growth Index6.47 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials33 (34.38%)5.53%
Reviews33 (34.38%)6.00%
Case Studies1 (1.04%)4.05%
Observational0 (0.00%)0.25%
Other29 (30.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]