spacer
spacer

Search 

DrugBank target: P08908

DrugBank target: P08908 (5HT1A_HUMAN)     

5-hydroxytryptamine receptor 1A

G-21, Serotonin receptor 1A, 5-HT-1A, 5-HT1A.

Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5- hydroxytryptamine release and in the regulation of dopamine and 5- hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli..

Disease(s)

Periodic fever, menstrual cycle-dependent (PFMC) [MIM:614674]: A condition characterized by recurrent fevers up to 40 degrees Celsius associated with the luteal phase of the menstrual cycle. Women show menstrual cycle-dependent physiologic changes in relation to sex hormone levels. Because ovulation triggers a significant change in the hormonal milieu that is similar to local inflammation, a 0.5 to 1.0 degree Celsius increase in basal body temperature after ovulation is commonly associated with progesterone secretion and is believed to be triggered by the induction of several inflammatory cytokines. Note=The disease is caused by mutations affecting the gene represented in this entry.

Structures

There are currently no structures for this UniProt code in the PDB.

Schematic diagram of Pfam domains in target sequence

Key:    PfamA domain

Sequence length: 422 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 45 drugs for this target protein:

 

 
Generic name: DB01224 quetiapine
Formula: C21H25N3O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00315 zolmitriptan
Formula: C16H21N3O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01238 aripiprazole
Formula: C23H27Cl2N3O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01621 pipotiazine
Formula: C24H33N3O3S2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08807 bopindolol
Formula: C23H28N2O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00714 apomorphine
Formula: C17H17No2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00571 propranolol
Formula: C16H21No2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00363 clozapine
Formula: C18H19Cln4
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01142 doxepin
D7V
Formula: C19H21No
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB00247 methysergide
Formula: C21H27N3O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08815 lurasidone
Formula: C28H36N4O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01267 paliperidone
Formula: C23H27Fn4O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01622 thioproperazine
Formula: C22H30N4O2S2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01618 molindone
Formula: C16H24N2O2
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01614 acepromazine
PMZ
Formula: C19H22N2Os
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB00656 trazodone
Formula: C19H22Cln5O
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB04946 iloperidone
Formula: C24H27Fn2O4
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00246 ziprasidone
Formula: C21H21Cln4Os
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00334 olanzapine
Formula: C17H20N4S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01616 alverine
Formula: C20H27N
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00321 amitriptyline
TP0
Formula: C20H23N
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB00726 trimipramine
Formula: C20H26N2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB06216 asenapine
Formula: C21H20Clno5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00952 naratriptan
Formula: C17H25N3O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00589 lisuride
Formula: C20H26N4O
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01392 yohimbine
Formula: C21H26N2O3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00413 pramipexole
Formula: C10H17N3S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01049 ergoloid mesylate
Formula: C30H41N5O8S
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00477 chlorpromazine
Z80
Formula: C17H19Cln2S
Structure: There are 3 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB00248 cabergoline
Formula: C26H37N5O2
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00540 nortriptyline
21B
Formula: C19H21N
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB00490 buspirone
Formula: C21H31N5O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00960 pindolol
Formula: C14H20N2O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01149 nefazodone
Formula: C25H32Cln5O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00734 risperidone
Formula: C23H27Fn4O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB08810 cinitapride
Formula: C21H30N4O4
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00866 alprenolol
JTZ
Formula: C15H23No2
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB05271 rotigotine
Formula: C19H25Nos
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01186 pergolide
Formula: C19H26N2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00268 ropinirole
Formula: C16H24N2O
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00216 eletriptan
Formula: C22H26N2O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00669 sumatriptan
Formula: C14H21N3O2S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB06684 vilazodone
Formula: C26H27N5O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00904 ondansetron
Formula: C18H19N3O
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01200 bromocriptine
08Y
Formula: C32H40Brn5O5
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.

  spacer

spacer