DGIdb - PHENTOLAMINE Drug Record

PHENTOLAMINE chembl:CHEMBL597 Approved

Alternate Names:

PHENTOLAMINE
REGITINA
DIBASIN
PHENTOLAMINE MESYLATE
REGITINE®
2-(N-(M-HYDROXYPHENYL)-P-TOLUIDINOMETHYL)IMIDAZOLINE
PHENTOLAMIN
ROGITINE®
FENTOLAMIN
VESOMAX
PHENTOLAMINUM
FENTOLAMINA
chemidplus:50-60-2
chembl:CHEMBL597
drugbank:00692
pubchem.compound:5775
rxcui:8153

Drug Info:

FDA Approval	1952
Drug Indications	Antihypertensive Agents
FDA Approval	approved
Drug Class	small molecule
Drug Indications	for treatment of erectile dysfunction
Year of Approval	1952
Drug Class	antihypertensive agents

(3 More Sources)

Publications:

Saeed et al., Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade., J. Cardiovasc. Pharmacol.
Giussani et al., 1995, Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero., J. Physiol. (Lond.)
Bylund, 1992, Subtypes of alpha 1- and alpha 2-adrenergic receptors., FASEB J.
Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol
Trendelenburg et al., 2003, Crosstalk between presynaptic angiotensin receptors, bradykinin receptors and alpha 2-autoreceptors in sympathetic neurons: a study in alpha 2-adrenoceptor-deficient mice., Br. J. Pharmacol.
Polak et al., 2005, Dynamic strength training improves insulin sensitivity and functional balance between adrenergic alpha 2A and beta pathways in subcutaneous adipose tissue of obese subjects., Diabetologia
Blandizzi et al., 2003, Altered prejunctional modulation of intestinal cholinergic and noradrenergic pathways by alpha2-adrenoceptors in the presence of experimental colitis., Br. J. Pharmacol.
Vonend et al., 2007, Alpha(2A)-adrenoceptors regulate sympathetic transmitter release in mice kidneys., Br. J. Pharmacol.
Molderings et al., 2000, Species-specific pharmacological properties of human alpha(2A)-adrenoceptors., Hypertension
Zhang D et al., 2004, Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane., Sci China C Life Sci
Koshimizu et al., 2004, Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors., Cardiovasc. Res.
Egert et al., 1999, Contribution of alpha-adrenergic and beta-adrenergic stimulation to ischemia-induced glucose transporter (GLUT) 4 and GLUT1 translocation in the isolated perfused rat heart., Circ. Res.
Proks et al., 1997, Phentolamine block of KATP channels is mediated by Kir6.2., Proc. Natl. Acad. Sci. U.S.A.
Nakata et al., 1985, Alpha-adrenergic regulation of the activity of thymidylate synthetase and thymidine kinase during liver regeneration after partial hepatectomy., Eur. J. Pharmacol.
Bijman et al., 1987, Modulation of placental alkaline phosphatase activity and cytokeratins in human HN-1 cells by butyrate, retinoic acid, catecholamines and histamine., Br. J. Cancer

PHENTOLAMINE ALPP

Interaction Score: 4.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2444242

Sources:
NCI
PHENTOLAMINE ADRA2A

Interaction Score: 0.74

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Trial Name -

PMIDs:
16407989 12721093 1346768 16273345 7562640 12770936 17115069 10988273 6176798

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology
PHENTOLAMINE KCNJ11

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9326676

Sources:
NCI
PHENTOLAMINE ADRA1D

Interaction Score: 0.31

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
15493479 15306222

Sources:
GuideToPharmacology
PHENTOLAMINE TYMS

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2866100

Sources:
NCI
PHENTOLAMINE ADRA1A

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
6176798 7562640 1346768

Sources:
TdgClinicalTrial GuideToPharmacology
PHENTOLAMINE SLC2A4

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10381893

Sources:
NCI
PHENTOLAMINE ADRA1B

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
15306222

Sources:
GuideToPharmacology
PHENTOLAMINE ADRA2B

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PHENTOLAMINE ADRA2C

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PHENTOLAMINE DRD2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PHENTOLAMINE CYP2C19

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENTOLAMINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: PHENTOLAMINE
- Version: 01-August-2011
Alternate Names:

PHENTOLAMINE Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1952

Publications:
TdgClinicalTrial: PHENTOLAMINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications for treatment of erectile dysfunction

Drug Class small molecule

FDA Approval approved

Publications:

NCI: PHENTOLAMINE

Version: 14-September-2017

Alternate Names:

C38691 NCI drug code

Drug Info:

Publications:

Nakata et al., 1985, Alpha-adrenergic regulation of the activity of thymidylate synthetase and thymidine kinase during liver regeneration after partial hepatectomy., Eur. J. Pharmacol.

Bijman et al., 1987, Modulation of placental alkaline phosphatase activity and cytokeratins in human HN-1 cells by butyrate, retinoic acid, catecholamines and histamine., Br. J. Cancer

Proks et al., 1997, Phentolamine block of KATP channels is mediated by Kir6.2., Proc. Natl. Acad. Sci. U.S.A.

DTC: PHENTOLAMINE
- Version: 02-September-2020
Alternate Names:

CHEMBL597 ChEMBL Drug ID

Drug Info:

Publications:

Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol
GuideToPharmacology: 135650818
- Version: 29-September-2020
Alternate Names:

PHENTOLAMINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Phentolamine
- Version: 2020.06.01
Alternate Names:

D01JUF TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL597
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	aviptadil,Invicorp
Novel drug target	Established target
Trial Name	-

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False
Direct Interaction?	True

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	True

PHENTOLAMINE Drug Record

PHENTOLAMINE chembl:CHEMBL597 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2444242

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name aviptadil,Invicorp Novel drug target Established target Trial Name -

PMIDs: 16407989 12721093 1346768 16273345 7562640 12770936 17115069 10988273 6176798

Sources: DTC TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9326676

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Inverse agonist Endogenous Drug? False Direct Interaction? True

PMIDs: 15493479 15306222

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2866100

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name aviptadil,Invicorp Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: 6176798 7562640 1346768

Sources: TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10381893

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 15306222

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: PHENTOLAMINE

Alternate Names: PHENTOLAMINE Primary Drug Name

Drug Info: Drug Class antihypertensive agents Year of Approval 1952

Publications:

TdgClinicalTrial: PHENTOLAMINE

Alternate Names:

Drug Info: Drug Indications for treatment of erectile dysfunction Drug Class small molecule FDA Approval approved

Publications:

NCI: PHENTOLAMINE

Alternate Names: C38691 NCI drug code

Drug Info:

DTC: PHENTOLAMINE

Alternate Names: CHEMBL597 ChEMBL Drug ID

Drug Info:

Publications: Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol

GuideToPharmacology: 135650818

Alternate Names: PHENTOLAMINE GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Phentolamine

Alternate Names: D01JUF TTD Drug ID

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
2444242

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Trial Name -

PMIDs:
16407989 12721093 1346768 16273345 7562640 12770936 17115069 10988273 6176798

Sources:
DTC TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
9326676

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
15493479 15306222

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
2866100

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name aviptadil,Invicorp

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
6176798 7562640 1346768

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
10381893

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
15306222

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

PHENTOLAMINE Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1952

Drug Info:

Drug Indications for treatment of erectile dysfunction

Drug Class small molecule

FDA Approval approved

Alternate Names:

C38691 NCI drug code

Alternate Names:

CHEMBL597 ChEMBL Drug ID

Publications:

Vilardaga JP et al., 2005, Molecular basis of inverse agonism in a G protein-coupled receptor., Nat Chem Biol

Alternate Names:

PHENTOLAMINE GuideToPharmacology Ligand Name

Alternate Names:

D01JUF TTD Drug ID