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Identification
NameYohimbine
Accession NumberDB01392
TypeSmall Molecule
GroupsApproved
Description

A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
(+)-yohimbineNot AvailableNot Available
(16alpha,17alpha)-17-Hydroxyyohimban-16-carboxylic acid methyl esterNot AvailableNot Available
17alpha-Hydroxyyohimban-16alpha-carboxylic acid methyl esterNot AvailableNot Available
AphrodineNot AvailableNot Available
CorynineNot AvailableNot Available
JohimbinGermanNot Available
QuebrachinNot AvailableNot Available
QuebrachineNot AvailableNot Available
Yohimbic acid methyl esterNot AvailableNot Available
YohimbinGermanNot Available
YohimbineNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
ActibineNot Available
AphrodyneNot Available
Baron-XNot Available
Dayto himbinNot Available
ThybineNot Available
YoconNot Available
YohimarNot Available
YohimexNot Available
YomanNot Available
YovitalNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number146-48-5
WeightAverage: 354.4427
Monoisotopic: 354.194342708
Chemical FormulaC21H26N2O3
InChI KeyBLGXFZZNTVWLAY-SCYLSFHTSA-N
InChI
InChI=1S/C21H26N2O3/c1-26-21(25)19-15-10-17-20-14(13-4-2-3-5-16(13)22-20)8-9-23(17)11-12(15)6-7-18(19)24/h2-5,12,15,17-19,22,24H,6-11H2,1H3/t12-,15-,17-,18-,19+/m0/s1
IUPAC Name
methyl (1S,15R,18S,19R,20S)-18-hydroxy-3,13-diazapentacyclo[11.8.0.0²,¹⁰.0⁴,⁹.0¹⁵,²⁰]henicosa-2(10),4,6,8-tetraene-19-carboxylate
SMILES
[H][C@@]12CC[C@H](O)[C@H](C(=O)OC)[C@@]1([H])C[C@]1([H])N(CCC3=C1NC1=CC=CC=C31)C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as yohimbine alkaloids. These are alkaloids containing the pentacyclic yohimban skeleton. The Yohimbinoid alkaloids contain a carbocyclic ring E arising through C-17 to C-18 bond formation in a corynantheine precursor.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassYohimbine alkaloids
Sub ClassNot Available
Direct ParentYohimbine alkaloids
Alternative Parents
Substituents
  • Yohimbine
  • Corynanthean skeleton
  • Yohimbine alkaloid
  • Pyridoindole
  • Beta-carboline
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • Beta-hydroxy acid
  • Benzenoid
  • Piperidine
  • Hydroxy acid
  • Heteroaromatic compound
  • Methyl ester
  • Pyrrole
  • Cyclic alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary alcohol
  • Carboxylic acid ester
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationIndicated as a sympatholytic and mydriatic. Impotence has been successfully treated with yohimbine in male patients with vascular or diabetic origins and psychogenic origins.
PharmacodynamicsYohimbine is an indolalkylamine alkaloid with chemical similarity to reserpine. Yohimbine blocks presynaptic alpha-2 adrenergic receptors. Its action on peripheral blood vessels resembles that of reserpine, though it is weaker and of short duration. Yohimbine's peripheral autonomic nervous system effect is to increase parasympathetic (cholinergic) and decrease sympathetic (adrenergic) activity. It is to be noted that in male sexual performance, erection is linked to cholinergic activity and to alpha-2 adrenergic blockade which may theoretically result in increased penile inflow, decreased penile outflow or both. Yohimbine exerts a stimulating action on the mood and may increase anxiety. Such actions have not been adequately studied or related to dosage although they appear to require high doses of the drug. Yohimbine has a mild anti-diuretic action, probably via stimulation of hypothalmic center and release of posterior pituitary hormone. Reportedly Yohimbine exerts no significant influence on cardiac stimulation and other effects mediated by (beta)-adrenergic receptors. Its effect on blood pressure, if any, would be to lower it; however, no adequate studies are at hand to quantitate this effect in terms of Yohimbine dosage.
Mechanism of actionYohimbine is a pre-synaptic alpha 2-adrenergic blocking agent. The exact mechanism for its use in impotence has not been fully elucidated. However, yohimbine may exert its beneficial effect on erectile ability through blockade of central alpha 2-adrenergic receptors producing an increase in sympathetic drive secondary to an increase in norepinephrine release and in firing rate of cells in the brain noradrenergic nuclei. Yohimbine-mediated norepinephrine release at the level of the corporeal tissues may also be involved. In addition, beneficial effects may involve other neurotransmitters such as dopamine and serotonin and cholinergic receptors.
AbsorptionRapidly absorbed following oral administration. Bioavailability is highly variable, ranging from 7 to 87% (mean 33%).
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Yohimbine appears to undergo extensive metabolism in an organ of high flow such as the liver or kidney, however, the precise metabolic fate of yohimbine has not been fully determined.

Route of eliminationNot Available
Half lifeElimination half-life is approximately 36 minutes.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9782
Blood Brain Barrier-0.5738
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.8762
P-glycoprotein inhibitor IInhibitor0.6002
P-glycoprotein inhibitor IINon-inhibitor0.9318
Renal organic cation transporterInhibitor0.5738
CYP450 2C9 substrateNon-substrate0.8514
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.5677
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 substrateNon-inhibitor0.9071
CYP450 2D6 substrateInhibitor0.8931
CYP450 2C19 substrateNon-inhibitor0.9094
CYP450 3A4 substrateNon-inhibitor0.8333
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.8681
CarcinogenicityNon-carcinogens0.9696
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7324 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8104
hERG inhibition (predictor II)Non-inhibitor0.6141
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage formsNot Available
Prices
Unit descriptionCostUnit
Yohimbine hcl powder22.8USD g
Yohimbine 5.4 mg tablet1.04USD tablet
Yocon 5.4 mg tablet0.96USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point241 °CPhysProp
logP2.73HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.348 mg/mLALOGPS
logP2.36ALOGPS
logP2.1ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)14.68ChemAxon
pKa (Strongest Basic)7.65ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area65.56 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity99.63 m3·mol-1ChemAxon
Polarizability40.22 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Germain Saint-Ruf, Pham Huu Chanh, Buu Hoi, “Yohimbine derivatives, process for their preparation and their applications.” U.S. Patent US3940387, issued April, 1960.

US3940387
General ReferenceNot Available
External Links
ATC CodesG04BE04
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.3 KB)
Interactions
Drug Interactions
Drug
AcebutololMay diminish the antihypertensive effect of Antihypertensives.
AliskirenMay diminish the antihypertensive effect of Antihypertensives.
AlprazolamMay diminish the therapeutic effect of Antianxiety Agents.
AmilorideMay diminish the antihypertensive effect of Antihypertensives.
AmitriptylineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
AmlodipineMay diminish the antihypertensive effect of Antihypertensives.
AmoxapineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
AtenololMay diminish the antihypertensive effect of Antihypertensives.
Azilsartan medoxomilMay diminish the antihypertensive effect of Antihypertensives.
BenazeprilMay diminish the antihypertensive effect of Antihypertensives.
BendroflumethiazideMay diminish the antihypertensive effect of Antihypertensives.
BisoprololMay diminish the antihypertensive effect of Antihypertensives.
BromazepamMay diminish the therapeutic effect of Antianxiety Agents.
BumetanideMay diminish the antihypertensive effect of Antihypertensives.
BuspironeMay diminish the therapeutic effect of Antianxiety Agents.
CandesartanMay diminish the antihypertensive effect of Antihypertensives.
CaptoprilMay diminish the antihypertensive effect of Antihypertensives.
CarvedilolMay diminish the antihypertensive effect of Antihypertensives.
ChlordiazepoxideMay diminish the therapeutic effect of Antianxiety Agents.
ChlorothiazideMay diminish the antihypertensive effect of Antihypertensives.
ChlorthalidoneMay diminish the antihypertensive effect of Antihypertensives.
CilazaprilMay diminish the antihypertensive effect of Antihypertensives.
ClevidipineMay diminish the antihypertensive effect of Antihypertensives.
ClidiniumMay diminish the therapeutic effect of Antianxiety Agents.
ClobazamMay diminish the therapeutic effect of Antianxiety Agents.
ClomipramineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
ClonazepamMay diminish the therapeutic effect of Antianxiety Agents.
ClonidineMay diminish the antihypertensive effect of Antihypertensives.
DesipramineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
DiazepamMay diminish the therapeutic effect of Antianxiety Agents.
DiltiazemMay diminish the antihypertensive effect of Antihypertensives.
DoxazosinMay diminish the antihypertensive effect of Antihypertensives.
EnalaprilMay diminish the antihypertensive effect of Antihypertensives.
EplerenoneMay diminish the antihypertensive effect of Antihypertensives.
EprosartanMay diminish the antihypertensive effect of Antihypertensives.
EsmololMay diminish the antihypertensive effect of Antihypertensives.
EstazolamMay diminish the therapeutic effect of Antianxiety Agents.
Ethacrynic acidMay diminish the antihypertensive effect of Antihypertensives.
FelodipineMay diminish the antihypertensive effect of Antihypertensives.
FlurazepamMay diminish the therapeutic effect of Antianxiety Agents.
FosinoprilMay diminish the antihypertensive effect of Antihypertensives.
FurosemideMay diminish the antihypertensive effect of Antihypertensives.
GuanfacineMay diminish the antihypertensive effect of Antihypertensives.
HydralazineMay diminish the antihypertensive effect of Antihypertensives.
HydrochlorothiazideMay diminish the antihypertensive effect of Antihypertensives.
ImipramineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
IndapamideMay diminish the antihypertensive effect of Antihypertensives.
IrbesartanMay diminish the antihypertensive effect of Antihypertensives.
IsradipineMay diminish the antihypertensive effect of Antihypertensives.
LabetalolMay diminish the antihypertensive effect of Antihypertensives.
LisinoprilMay diminish the antihypertensive effect of Antihypertensives.
LorazepamMay diminish the therapeutic effect of Antianxiety Agents.
LosartanMay diminish the antihypertensive effect of Antihypertensives.
MannitolMay diminish the antihypertensive effect of Antihypertensives.
MeprobamateMay diminish the therapeutic effect of Antianxiety Agents.
MethyclothiazideMay diminish the antihypertensive effect of Antihypertensives.
MethyldopaMay diminish the antihypertensive effect of Antihypertensives.
MetolazoneMay diminish the antihypertensive effect of Antihypertensives.
MetoprololMay diminish the antihypertensive effect of Antihypertensives.
MidazolamMay diminish the therapeutic effect of Antianxiety Agents.
MoexiprilMay diminish the antihypertensive effect of Antihypertensives.
NadololMay diminish the antihypertensive effect of Antihypertensives.
NebivololMay diminish the antihypertensive effect of Antihypertensives.
NifedipineMay diminish the antihypertensive effect of Antihypertensives.
NimodipineMay diminish the antihypertensive effect of Antihypertensives.
NisoldipineMay diminish the antihypertensive effect of Antihypertensives.
NitrazepamMay diminish the therapeutic effect of Antianxiety Agents.
NitroprussideMay diminish the antihypertensive effect of Antihypertensives.
NortriptylineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
OlmesartanMay diminish the antihypertensive effect of Antihypertensives.
OxazepamMay diminish the therapeutic effect of Antianxiety Agents.
PenbutololMay diminish the antihypertensive effect of Antihypertensives.
PerindoprilMay diminish the antihypertensive effect of Antihypertensives.
PhenoxybenzamineMay diminish the antihypertensive effect of Antihypertensives.
PhentolamineMay diminish the antihypertensive effect of Antihypertensives.
PindololMay diminish the antihypertensive effect of Antihypertensives.
PrazosinMay diminish the antihypertensive effect of Antihypertensives.
PropranololMay diminish the antihypertensive effect of Antihypertensives.
ProtriptylineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
QuazepamMay diminish the therapeutic effect of Antianxiety Agents.
QuinaprilMay diminish the antihypertensive effect of Antihypertensives.
RamiprilMay diminish the antihypertensive effect of Antihypertensives.
ReserpineMay diminish the antihypertensive effect of Antihypertensives.
SotalolMay diminish the antihypertensive effect of Antihypertensives.
SpironolactoneMay diminish the antihypertensive effect of Antihypertensives.
TelmisartanMay diminish the antihypertensive effect of Antihypertensives.
TemazepamMay diminish the therapeutic effect of Antianxiety Agents.
TerazosinMay diminish the antihypertensive effect of Antihypertensives.
TorasemideMay diminish the antihypertensive effect of Antihypertensives.
TrandolaprilMay diminish the antihypertensive effect of Antihypertensives.
TriamtereneMay diminish the antihypertensive effect of Antihypertensives.
TriazolamMay diminish the therapeutic effect of Antianxiety Agents.
TrimipramineTricyclic Antidepressants may increase the serum concentration of Yohimbine.
ValsartanMay diminish the antihypertensive effect of Antihypertensives.
Food InteractionsNot Available

Targets

1. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

References:

  1. Laurila JM, Xhaard H, Ruuskanen JO, Rantanen MJ, Karlsson HK, Johnson MS, Scheinin M: The second extracellular loop of alpha2A-adrenoceptors contributes to the binding of yohimbine analogues. Br J Pharmacol. 2007 Aug;151(8):1293-304. Epub 2007 Jun 11. Pubmed
  2. Zadori ZS, Shujaa N, Fulop K, Dunkel P, Gyires K: Pre- and postsynaptic mechanisms in the clonidine- and oxymetazoline-induced inhibition of gastric motility in the rat. Neurochem Int. 2007 Oct;51(5):297-305. Epub 2007 Jun 30. Pubmed
  3. Paul BZ, Jin J, Kunapuli SP: Molecular mechanism of thromboxane A(2)-induced platelet aggregation. Essential role for p2t(ac) and alpha(2a) receptors. J Biol Chem. 1999 Oct 8;274(41):29108-14. Pubmed
  4. Kalkman HO, Loetscher E: alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs. Eur J Pharmacol. 2003 Feb 21;462(1-3):33-40. Pubmed
  5. Ozdogan UK, Lahdesmaki J, Scheinin M: The analgesic efficacy of partial opioid agonists is increased in mice with targeted inactivation of the alpha2A-adrenoceptor gene. Eur J Pharmacol. 2006 Jan 4;529(1-3):105-13. Epub 2005 Dec 2. Pubmed
  6. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

2. Alpha-2B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

References:

  1. Freitag A, Wessler I, Racke K: Adrenoceptor- and cholinoceptor-mediated mechanisms in the regulation of 5-hydroxytryptamine release from isolated tracheae of newborn rabbits. Br J Pharmacol. 1996 Sep;119(1):91-8. Pubmed
  2. Cleary L, Vandeputte C, Docherty JR: Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. Br J Pharmacol. 2002 Jul;136(6):857-64. Pubmed
  3. Gyires K, Mullner K, Ronai AZ: Functional evidence that gastroprotection can be induced by activation of central alpha(2B)-adrenoceptor subtypes in the rat. Eur J Pharmacol. 2000 May 19;396(2-3):131-5. Pubmed
  4. Takada K, Clark DJ, Davies MF, Tonner PH, Krause TK, Bertaccini E, Maze M: Meperidine exerts agonist activity at the alpha(2B)-adrenoceptor subtype. Anesthesiology. 2002 Jun;96(6):1420-6. Pubmed
  5. Alonso E, Garrido E, Diez-Fernandez C, Perez-Garcia C, Herradon G, Ezquerra L, Deuel TF, Alguacil LF: Yohimbine prevents morphine-induced changes of glial fibrillary acidic protein in brainstem and alpha2-adrenoceptor gene expression in hippocampus. Neurosci Lett. 2007 Jan 29;412(2):163-7. Epub 2006 Nov 22. Pubmed
  6. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

3. Alpha-2C adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

References:

  1. Lalchandani SG, Lei L, Zheng W, Suni MM, Moore BM, Liggett SB, Miller DD, Feller DR: Yohimbine dimers exhibiting selectivity for the human alpha 2C-adrenoceptor subtype. J Pharmacol Exp Ther. 2002 Dec;303(3):979-84. Pubmed
  2. Rizzo CA, Ruck LM, Corboz MR, Umland SP, Wan Y, Shah H, Jakway J, Cheng L, McCormick K, Egan RW, Hey JA: Postjunctional alpha(2C)-adrenoceptor contractility in human saphenous vein. Eur J Pharmacol. 2001 Feb 16;413(2-3):263-9. Pubmed
  3. Cleary L, Murad K, Bexis S, Docherty JR: The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2D)-adrenoceptor antagonist. Auton Autacoid Pharmacol. 2005 Oct;25(4):135-41. Pubmed
  4. Kalkman HO, Loetscher E: alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs. Eur J Pharmacol. 2003 Feb 21;462(1-3):33-40. Pubmed
  5. Cleary L, Vandeputte C, Docherty JR: Investigation of neurotransmission in vas deferens from alpha(2A/D)-adrenoceptor knockout mice. Br J Pharmacol. 2002 Jul;136(6):857-64. Pubmed
  6. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

4. 5-hydroxytryptamine receptor 1A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: partial agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

References:

  1. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed
  2. Kaumann AJ: Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):149-54. Pubmed

5. 5-hydroxytryptamine receptor 1B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

References:

  1. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed
  2. Kaumann AJ: Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):149-54. Pubmed

6. 5-hydroxytryptamine receptor 1D

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

References:

  1. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

7. D(2) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

References:

  1. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

8. D(3) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

References:

  1. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Coge F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A: Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT, 5-HT and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse. 2000 Feb;35(2):79-95. Pubmed

9. 5-hydroxytryptamine receptor 2A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

References:

  1. Baxter GS, Murphy OE, Blackburn TP: Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle. Br J Pharmacol. 1994 May;112(1):323-31. Pubmed
  2. Kaumann AJ: Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):149-54. Pubmed

10. 5-hydroxytryptamine receptor 2C

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2C P28335 Details

References:

  1. Baxter GS, Murphy OE, Blackburn TP: Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle. Br J Pharmacol. 1994 May;112(1):323-31. Pubmed
  2. Kaumann AJ: Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):149-54. Pubmed

11. ATP-sensitive potassium channel

Kind: protein group

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
ATP-sensitive inward rectifier potassium channel 1 P48048 Details
ATP-sensitive inward rectifier potassium channel 10 P78508 Details
ATP-sensitive inward rectifier potassium channel 11 Q14654 Details
ATP-sensitive inward rectifier potassium channel 12 Q14500 Details
ATP-sensitive inward rectifier potassium channel 14 Q9UNX9 Details
ATP-sensitive inward rectifier potassium channel 15 Q99712 Details
ATP-sensitive inward rectifier potassium channel 8 Q15842 Details

References:

  1. Plant TD, Henquin JC: Phentolamine and yohimbine inhibit ATP-sensitive K+ channels in mouse pancreatic beta-cells. Br J Pharmacol. 1990 Sep;101(1):115-20. Pubmed

12. 5-hydroxytryptamine receptor 2B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2B P41595 Details

References:

  1. Baxter GS, Murphy OE, Blackburn TP: Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle. Br J Pharmacol. 1994 May;112(1):323-31. Pubmed
  2. Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW, Flippin LA, Eglen RM: RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):621-9. Pubmed

Enzymes

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

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Drug created on July 08, 2007 11:00 / Updated on January 29, 2014 09:41