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.

Products
Background
Literature
Gene Data

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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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