5-HT1A Receptors
The serotonin 5-HT1A receptor was the first 5-HT receptor to be fully sequenced. 5-HT1A receptor binding sites are located primarily in limbic brain areas, notably the hypothalamus and cortical areas. The human gene encoding this receptor has been localized to chromosome 5.
Agonists |
|
|---|---|
| Cat No | Product Name / Activity |
| 5584 | Aripiprazole |
| High affinity D2 and 5-HT1A receptor partial agonist; also 5-HT2A antagonist | |
| 3346 | ATC 0175 hydrochloride |
| MCH1 antagonist; also 5-HT2B antagonist and 5-HT1A partial agonist | |
| 1006 | BMY 7378 dihydrochloride |
| 5-HT1A partial agonist | |
| 0556 | BP 554 maleate |
| Selective 5-HT1A agonist | |
| 0962 | Buspirone hydrochloride |
| 5-HT1A partial agonist | |
| 1080 | (R)-(+)-8-Hydroxy-DPAT hydrobromide |
| Selective 5-HT1A agonist. Enantiomer of 8-Hydroxy-DPAT hydrobromide (Cat. No. 0529) | |
| 0529 | 8-Hydroxy-DPAT hydrobromide |
| Selective 5-HT1A agonist; also has moderate affinity for 5-HT7 | |
| 0797 | 8-Hydroxy-PIPAT oxalate |
| High affinity 5-HT1A agonist | |
| 1869 | Ipsapirone |
| Selective 5-HT1A agonist | |
| 0411 | MDL 73005EF hydrochloride |
| Potent and selective 5-HT1A partial agonist | |
| 1746 | Nemonapride |
| 5-HT1A agonist. Also highly potent D2-like dopamine antagonist | |
| 0912 | RU 24969 hemisuccinate |
| 5-HT1B/1A agonist | |
| 1771 | S 14506 hydrochloride |
| Highly potent 5-HT1A agonist; displays unique binding mechanism | |
| 3586 | Sumatriptan succinate |
| 5-HT1A/1B/1D receptor agonist | |
| 2854 | Tandospirone hydrochloride |
| Selective 5-HT1A partial agonist | |
| 1772 | Urapidil hydrochloride |
| 5-HT1A agonist. Also α1-adrenoceptor antagonist | |
| 6202 | Vilazodone hydrochloride |
| Potent 5-HT1A partial agonist and SSRI; antidepressant | |
| 2491 | Xaliproden hydrochloride |
| Orally active, high affinity 5-HT1A agonist | |
Antagonists |
|
| Cat No | Product Name / Activity |
| 2806 | Alprenolol hydrochloride |
| 5-HT1A antagonist | |
| 0993 | Cyanopindolol hemifumarate |
| 5-HT1A/1B antagonist. Also β-adrenergic antagonist | |
| 0933 | MM 77 dihydrochloride |
| 5-HT1A (postsynaptic) antagonist | |
| 3282 | NAD 299 hydrochloride |
| Selective, high affinity 5-HT1A antagonist | |
| 0553 | NAN-190 hydrobromide |
| 5-HT1A antagonist | |
| 0994 | Pindolol |
| 5-HT1A/1B antagonist. Also β-adrenergic antagonist | |
| 1060 | (S)-(-)-Pindolol |
| 5-HT1A/1B antagonist. Also β-adrenergic antagonist. More active enantiomer of pindolol (Cat. No. 0994) | |
| 1516 | SDZ 21009 |
| 5-HT1A/1B antagonist. Also β-adrenoceptor antagonist | |
| 0631 | Spiroxatrine |
| 5-HT1A antagonist | |
| 1253 | (S)-WAY 100135 dihydrochloride |
| Potent, selective 5-HT1A antagonist | |
| 4380 | WAY 100635 maleate |
| Potent, 5-HT1A silent antagonist. Also D4 agonist | |
Ligands |
|
| Cat No | Product Name / Activity |
| 0412 | MDL 72832 hydrochloride |
| Potent 5-HT1A ligand | |
| 0581 | 3-MPPI |
| 5-HT1A ligand | |
The serotonin 5-HT1A receptor was the first 5-HT receptor to be fully sequenced and the human gene encoding this receptor has been localized to chromosome 5 (5q11.2-q13).
5-HT1A receptor binding sites are located primarily in limbic brain areas, notably the hypothalamus, lateral septum, cortical areas and the mesencephalic raphe nuclei. 5-HT1A receptor ligands with agonist activity possess antianxiety, antidepressant, antiaggressive, and perhaps anticraving, anticataleptic, antiemetic, and neuroprotective properties.
External sources of pharmacological information for 5-HT1A Receptors :
Literature for 5-HT1A Receptors
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