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 hydrochlorideNew |
| 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
GPCR Product Listing
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Secretin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
Neurodegeneration Product Guide
A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:
- Alzheimer's disease
- Parkinson's disease
- Huntington's disease
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Our Neurodegeneration guide highlights over 275 products for neurodegeneration research.
Request copyDownload PDFWritten by N. Barnes & J. Neumaler
Our 5-HT review summarizes the serotonin receptor subtypes and highlights their importance in mediating various physiological & pharmacological processes.
Request copyDownload PDFWritten by P. Skolnich et al
Our Depression poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder.
Request copyDownload PDFWritten by Anthony H.V. Schapira
Our Parkinson's disease (PD) poster summarizes the neurobiology of the disease, and highlights current therapeutic treatments for symptomatic PD.
Request copyDownload PDF