5-ht1f

LY 344864 (racemate) is an agonist of the 5-HT1F receptor.

LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM

LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively).

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

Sumatriptan succinate (GR 43175), a serotonin1 (5-HT1) receptor agonist, is used in the acute treatment of a migraine headache.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

Sumatriptan (GR 43175 free base) is an orally active and potent 5-hydroxytryptamine 1 (5-HT1) receptor agonist that crosses the blood-brain barrier and has anti-inflammatory activity with high affinity for 5-HT1D, 5-HT1B, and 5-HT1F receptors for use in acute migraines and acute myocardial infarction.

SB 243213 hydrochloride is an orally active, selective, high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor (pKi of 9.37 and pKb of 9.8), with an improved anxiolytic profile and potential for treating schizophrenia and motor disorders.

SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and 5-HT1F Receptor partial agonist (EC50 = 77.91 nM). It demonstrates significant efficacy in rat models of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins while inhibiting the phosphorylation levels of ERK and CREB. This compound is useful for migraine research.

5-HT1F receptor agonist

UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

Sumatriptan (GR 43175) hydrochloride can be used in the research of migraine headache that is an orally active agonist of 5-HT1 receptor. The Ki values of Sumatriptan hydrochloride against 5-HT1D, 5-HT1B and 5-HT1A receptors are 17 nM, 27 nM and 100 nM, respectively. [1] [2].

FPT is a 2-aminotetralin and acts as a potent partial agonist at 5-HT1AR, as well as a full agonist at 5-HT1BR and 5-HT1DR, with EC50 values of 39.3 nM, 1.2 nM, and 0.5 nM, respectively. It is a weak agonist at 5-HT7R. In Fmr1 knockout mice, FPT demonstrates anticonvulsant effects and exhibits anxiolytic and pro-social effects in mouse models.

LY 344864 S-enantiomer, the S-enantiomer of LY344864, serves as a 5-HT1F receptor agonist.

SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. SB 224289 displays 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand

YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.

LY334370 fumarate is the fumarate salt form of LY334370, which is a selective 5-HT1F receptor agonist with a Ki value of 1.6 nM.

CP-122288 is a potent and selective agonist for the 5-HT1B, 5-HT1D and 5-HT1F serotonin receptor subtypes. CP-122288 is potent as an inhibitor of plasma protein extravasation and neurogenic inflammation.

LY 302148 , a 5-HT1F receptor agonist, inhibits neurogenic dural inflammation in guinea pigs. It has potential for migraine therapeutics.