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 partial agonist; also 5-HT2A antagonist | |
3346 | ATC 0175 hydrochloride |
5-HT1A partial agonist; also 5-HT2B antagonist and MCH1 antagonist | |
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-HT1A and 5-HT1B agonist | |
1771 | S 14506 hydrochloride |
Highly potent 5-HT1A agonist; displays unique binding mechanism | |
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 |
High affinity 5-HT1A agonist; orally active | |
Antagonists |
Cat. No. | Product Name / Activity |
2806 | Alprenolol hydrochloride |
5-HT1A antagonist; also β-adrenoceptor antagonist | |
0993 | Cyanopindolol hemifumarate |
5-HT1A and 5-HT1B 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 | |
1060 | (S)-(-)-Pindolol |
5-HT1A and 5-HT1B antagonist; also β-adrenergic antagonist; more active enantiomer of pindolol (Cat. No. 0994) | |
1516 | SDZ 21009 |
5-HT1A and 5-HT1B antagonist; also β-adrenoceptor antagonist | |
0631 | Spiroxatrine |
5-HT1A antagonist | |
1253 | (S)-WAY 100135 dihydrochloride |
Potent and selective 5-HT1A antagonist | |
4380 | WAY 100635 maleate |
Potent 5-HT1A antagonist; also D4 agonist | |
Ligands |
Cat. No. | Product Name / Activity |
0412 | MDL 72832 hydrochloride |
Potent 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.
Tocris offers the following scientific literature for 5-HT1A Receptors to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
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.
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