5-ht1b/1d

Almotriptan Malate (PNU180638), a selective 5-HT1B/1D receptor agonist, is used in the therapy of Migraine attacks in adults.

Almotriptan (LAS 31416) is a 5-HT1B/1D-receptor agonist used to treat migraine.Almotriptan is a triptan drug for treatment of migraine headaches.Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels.

GR 125743 is a novel antagonist of 5-HT1B/1D receptor.

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).

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

Eletriptan hydrobromide (Eletriptan HBr) is an orally active agonist with specific affinity for the 5-hydroxytriptamine1B/1D [5-HT1B/1D] receptor.

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.

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.

Avitriptan is a 5-HT1B/1D receptor agonist with pKi values of 7.44 for 5-HT1Brat, 7.68 for 5-HT1Bhuman, and 8.36 for 5-HT1Dhuman. It can induce contraction in isolated coronary arteries and is used for the treatment of migraines.

Frovatriptan Succinate is a synthetic triptan with 5-HT1B/1D receptors agonist activity. It is indicated for the acute treatment of migraine.

5-HT1B/1D receptor antagonist

GR 55562 dihydrochloride is a selective serotonin 5-HT 1B antagonist with weak antagonistic activity against 5-HT 1D, and can be used for research on neurological diseases.

Dual 5-HT1B/1D receptor antagonist

Donitriptan Mesylate, a 5-HT1B/1D agonist, is used potentially for the treatment of migraines.

GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist.