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| Formula | C24H27FN2O2 |
| Molar mass | 394.490 g·mol−1 |
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LY-310762 is a drug which acts as a potent and selective antagonist for the 5-HT1D serotonin receptor, with reasonable selectivity over the closely related 5-HT1B subtype. [1]
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. This drug class was first commercially introduced in the 1990s. While effective at treating individual headaches, they do not provide preventive treatment and are not considered a cure. They are not effective for the treatment of tension–type headache, except in persons who also experience migraines. Triptans do not relieve other kinds of pain.
5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety. It also induces vasoconstriction in the brain.
AR-A000002, also known as AZD-8129, is a drug which is one of the first compounds developed to act as a selective antagonist for the serotonin receptor 5-HT1B, with approximately 10x selectivity for 5-HT1B over the closely related 5-HT1D receptor. It has been shown to produce sustained increases in levels of serotonin in the brain, and has anxiolytic effects in animal studies.
BRL-15,572 is a drug which acts as a selective antagonist for the serotonin receptor subtype 5-HT1D, with around 60x selectivity over other related receptors. The 5-HT1D receptor has a very similar pharmacology to the closely related 5-HT1B receptor, and most older ligands for these receptors bind to both subtypes with approximately equal affinity, so development of compounds such as BRL-15572 which are able to selectively block the 5-HT1D subtype while leaving 5-HT1B unaffected, have been a significant advance which has helped scientists in researching the function of these serotonin receptor subtypes. One function of the 5-HT1D receptor this research has revealed is its role in modulating release of the neurotransmitter glutamate in the brain, as well as functions in regulation of cerebral blood pressure which are important in the pathogenesis of migraine headaches.
SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT1B, with around 25x selectivity over the closely related 5-HT1D receptor. It is used in scientific research, and has demonstrated anxiolytic effects in animal studies.
GR-127935 is a drug which acts as a selective antagonist at the serotonin receptors 5-HT1B and 5-HT1D. It has little effect when given by itself but blocks the antiaggressive effect of 5-HT1B agonists, and alters release of serotonin in the brain, as well as reducing drug-seeking behaviour in cocaine addicted rats.
CGS-12066A is a drug which acts as a potent and selective agonist for the 5-HT1B receptor with lower affinity for the three 5-HT2 receptor subtypes. It is used for studying the role of the 5-HT1B receptor in various processes including perception of pain and the sleep-wake cycle.
Roxindole (EMD-49,980) is a dopaminergic and serotonergic drug which was originally developed by Merck KGaA for the treatment of schizophrenia. In clinical trials its antipsychotic efficacy was only modest but it was unexpectedly found to produce potent and rapid antidepressant and anxiolytic effects. As a result, roxindole was further researched for the treatment of depression instead. It has also been investigated as a therapy for Parkinson's disease and prolactinoma.
Elzasonan (CP-448,187) is a selective 5-HT1B and 5-HT1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy. By preferentially blocking 5-HT1B and 5-HT1D autoreceptors, elzasonan is thought to enhance serotonergic innervations originating from the raphe nucleus, thereby improving signaling to limbic regions like the hippocampus and prefrontal cortex and ultimately resulting in antidepressant effects.
CP-93129 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 150x and 200x selectivity over the closely related 5-HT1D and 5-HT1A receptors. It is used in the study of 5-HT1B receptors in the brain, particularly their role in modulating the release of other neurotransmitters.
5-Ethyl-N,N-dimethyltryptamine is a tryptamine derivative which acts as an agonist at the 5-HT1A and 5-HT1D serotonin receptors, with around 3x selectivity for 5-HT1D.
5-(Nonyloxy)tryptamine (5-NOT) is a tryptamine derivative which acts as a selective agonist at the 5-HT1B receptor. Increasing the O-alkoxy chain length in this series gives generally increasing potency and selectivity for 5-HT1B, with highest activity found for the nonyloxy derivative, having a 5-HT1B binding affinity of 1.0 nM, and around 300-fold selectivity over the related 5-HT1A receptor.
CP-135807 is a drug which acts as a potent and selective agonist for the 5-HT1D serotonin receptor, and is used to study the function of this receptor subtype.
L-694247 is a somewhat selective 5-HT1D agonist, with a 10-fold greater affinity for the 5-HT1B receptor, and 25-fold greater affinity for the 5-HT1A receptor. When L-694247 was injected intraventricularly in dehydrated rats, it inhibited water intake. Pre-treatment with a 5-HT1D antagonist abolished this effect. Administration of L-694,247 to normally hydrated rats had no effect on water intake.
PNU-142633 is an experimental drug candidate for the treatment of migraine. It exerts its effect as a selective, high affinity 5-HT1D receptor antagonist. PNU-142633 is well tolerated after oral administration.
Donitriptan (INN) is a triptan drug which was investigated as an antimigraine agent but ultimately was never marketed. It acts as a high-affinity, high-efficacy/near-full agonist of the 5-HT1B and 5-HT1D receptors, and is among the most potent of the triptan series of drugs. Donitriptan was being developed in France by bioMérieux-Pierre Fabre and made it to phase II clinical trials in Europe before development was discontinued.
CP-122,288 is a drug which acts as a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin receptor subtypes. It is a derivative of the migraine medication sumatriptan, but while CP-122,288 is 40,000 times more potent than sumatriptan as an inhibitor of neurogenic inflammation and plasma protein extravasation, it is only twice as potent as a constrictor of blood vessels. In human trials, CP-122,288 was not found to be effective as a treatment for migraine, but its selectivity for neurogenic anti-inflammatory action over vasoconstriction has made it useful for research into the underlying causes of migraine.
LY-367642 is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function of presynaptic 5-HT1D autoreceptors.
LY-456219 is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function of presynaptic 5-HT1D autoreceptors. LY-456219 lacks significant affinity for the 5-HT1B, α1 adrenergic, and dopamine D2 receptors. It is an enantiomer of LY-456220.
LY-456220 is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function of presynaptic 5-HT1D autoreceptors. LY-456220 lacks significant affinity for the 5-HT1B, α1 adrenergic, and dopamine D2 receptors. It is an enantiomer of LY-456219.
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