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DrugBank target: P28223

DrugBank target: P28223 (5HT2A_HUMAN)     

5-hydroxytryptamine receptor 2A

Serotonin receptor 2A, 5-HT-2, 5-HT-2A.

Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5- dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction..

Structures

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

Schematic diagram of Pfam domains in target sequence

Key:    PfamA domain  PfamB domain

Sequence length: 471 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 61 drugs for this target protein:

 

 
Generic name: DB01239 chlorprothixene
Formula: C18H18Clns
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00458 imipramine
IXX
Formula: C19H24N2
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB01287 dihydroergotoxine
Formula: C34H41N5O8S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00656 trazodone
Formula: C19H22Cln5O
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: DB04946 iloperidone
Formula: C24H27Fn2O4
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00408 loxapine
Formula: C18H18Cln3O
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00875 flupenthixol
Formula: C23H27F3N2Os
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01151 desipramine
DSM
Formula: C18H22N2
Structure: There are 2 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB06148 mianserin
Formula: C18H20N2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00502 haloperidol
Formula: C21H23Clfno2
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: DB00924 cyclobenzaprine
Formula: C20H21N
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: DB00420 promazine
P2Z
Formula: C17H20N2S
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
 
Generic name: DB01623 thiothixene
Formula: C23H29N3O2S2
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: DB01403 methotrimeprazine
Formula: C19H24N2Os
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: DB08810 cinitapride
Formula: C21H30N4O4
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00777 propiomazine
Formula: C20H24N2Os
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00409 remoxipride
Formula: C16H23Brn2O3
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: DB00805 minaprine
Formula: C17H22N4O
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00715 paroxetine
8PR
Formula: C19H20Fno3
Structure: There are 4 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB01224 quetiapine
Formula: C21H25N3O2S
Structure: There are no structures of this molecule in the PDB.
Generic name: DB01242 clomipramine
CXX
Formula: C19H23Cln2
Structure: There are 3 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB01618 molindone
Formula: C16H24N2O2
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: DB01622 thioproperazine
Formula: C22H30N4O2S2
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: DB01069 promethazine
Formula: C17H20N2S
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: DB01621 pipotiazine
Formula: C24H33N3O3S2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00370 mirtazapine
Formula: C17H19N3
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: DB00696 ergotamine
ERM
Formula: C33H35N5O5
Structure: There are 3 PDB structures containing this molecule although none are bound to the above target protein.
 
Generic name: DB00933 mesoridazine
Formula: C21H26N2Os2
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: DB01267 paliperidone
Formula: C23H27Fn4O3
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: DB06216 asenapine
Formula: C21H20Clno5
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: DB00843 donepezil
E20
Formula: C24H29No3
Structure: There are 4 PDB structures containing this molecule although none are 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: DB01149 nefazodone
Formula: C25H32Cln5O2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00726 trimipramine
Formula: C20H26N2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00604 cisapride
Formula: C23H29Clfn3O4
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00751 epinastine
Formula: C16H15N3
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB04842 fluspirilene
Formula: C29H31F2N3O
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: DB00268 ropinirole
Formula: C16H24N2O
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: DB06288 amisulpride
Formula: C17H27N3O4S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01624 zuclopenthixol
Formula: C22H25Cln2Os
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00434 cyproheptadine
Formula: C21H21N
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00248 cabergoline
Formula: C26H37N5O2
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: DB00679 thioridazine
LZU
Formula: C21H26N2S2
Structure: There is one PDB structure containing this molecule but it is not bound to the above target protein.
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.
 
Generic name: DB06144 sertindole
Formula: C24H26Clfn4O
Structure: There are no structures of this molecule in the PDB.

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