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.

Literature (5)
Gene Data

5-HT1A Receptor 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
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
1869 Ipsapirone
Selective 5-HT1A 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

5-HT1A Receptor 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)
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

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

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.


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5-HT Receptors

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.


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5-HT1A Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human HTR1A NM_000524 P08908
Mouse Htr1a NM_008308 Q64264
Rat Htr1a NM_012585 P19327