5-ht1d receptor

Donitriptan is a 5-HT receptor agonist with pKis of 9.4 and 9.3 for 5-HT1B and 5-HT1D, respectively.

AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM) with demonstrated selectivity for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM, and 98.5 nM, respectively).

Frovatriptan succinate hydrate (Frova) is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine. Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively.

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).

SEP-363856 is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2/5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively.

PNU-142633 has anti-migraine efficacy. PNU-142633 is a high affinity and selective 5-HT1D receptor agonist (Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively).

Donitriptan hydrochloride (Donitriptan monohydrochloride) is a potent, high efficacy agonist of 5-HT1B/1D receptors with pKis of 9.4 and 9.3, 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.

PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (≥100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors.

Eletriptan, second-generation triptans used to treat migraines, is used as an abortion drug.

AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).

AR-A 2 is a selective 5-HT1B receptor antagonist with high affinity to guinea pig cortex 5-HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM), exhibiting a 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

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.

SEP-363856 (SEP-856) mesylate is an orally active compound that acts as an agonist for both TAAR1 and 5-HT1A receptors. This compound exhibits antipsychotic activity in the central nervous system and has potential for the study of schizophrenia.

CP 135807 is a 5-HT1D receptor agonist.

5-HT1B/1D receptor antagonist

β-adrenoceptor and 5-HT1A/1B receptor antagonist