Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C32H38N2O8.ClH |
| Molecular Weight | 615.114 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@]12C[C@@H](OC(=O)C3=CC(OC)=C(OC)C(OC)=C3)[C@H](OC)[C@@H](C(=O)OC)[C@@]1([H])C[C@@]4([H])N(CCC5=C4NC6=C5C=CC=C6)C2
InChI
InChIKey=YCNOGQOHKRDAHJ-UZXCFUCJSA-N
InChI=1S/C32H38N2O8.ClH/c1-37-24-12-17(13-25(38-2)29(24)39-3)31(35)42-26-14-18-16-34-11-10-20-19-8-6-7-9-22(19)33-28(20)23(34)15-21(18)27(30(26)40-4)32(36)41-5;/h6-9,12-13,18,21,23,26-27,30,33H,10-11,14-16H2,1-5H3;1H/t18-,21+,23-,26-,27+,30+;/m1./s1
Deserpidine is an ester alkaloid drug isolated from Rauwolfia canescens (family Apocynaceae) with antipsychotic and antihypertensive properties that has been used for the control of high blood pressure and for the relief of psychotic behavior. Rauwolfia alkaloids work by controlling nerve impulses along certain nerve pathways. As a result, they act on the heart and blood vessels to lower blood pressure. Deserpidine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
CNS Activity
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
172 pg/mL |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESERPIDINE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4193 pg × h/mL |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESERPIDINE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
42.9 h |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESERPIDINE plasma | Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
6 mg 3 times / day multiple, oral (max) Highest studied dose Dose: 6 mg, 3 times / day Route: oral Route: multiple Dose: 6 mg, 3 times / day Sources: Page: p.1115 |
unhealthy n = 13 Health Status: unhealthy Condition: Schizophrenia Sex: M Population Size: 13 Sources: Page: p.1115 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Synexin and GTP increase surfactant secretion in permeabilized alveolar type II cells. | 2001 May |
|
| Muscarinic excitation-contraction coupling mechanisms in tracheal and bronchial smooth muscles. | 2001 Sep |
|
| Extensive skinning of cell membrane diminishes the force-inhibiting effect of okadaic acid on smooth muscles of Guinea pig hepatic portal vein. | 2002 Apr |
|
| Xestospongin C, a novel blocker of IP3 receptor, attenuates the increase in cytosolic calcium level and degranulation that is induced by antigen in RBL-2H3 mast cells. | 2002 Apr |
|
| Perforated patch recording of L-type calcium current with beta-escin in guinea pig ventricular myocytes. | 2003 Nov |
|
| Dependence of Ca2+-induced contraction on ATP in alpha-toxin-permeabilized preparations of rat femoral artery. | 2003 Oct |
|
| Characterization of alpha-soluble N-ethylmaleimide-sensitive fusion attachment protein in alveolar type II cells: implications in lung surfactant secretion. | 2003 Sep |
|
| Nitric oxide relaxes rat tail artery smooth muscle by cyclic GMP-independent decrease in calcium sensitivity of myofilaments. | 2004 Aug |
|
| Beta-escin diminishes voltage-gated calcium current rundown in perforated patch-clamp recordings from rat primary afferent neurons. | 2004 Oct 15 |
|
| Beta-escin, a natural triterpenoid saponin from Chinese horse chestnut seeds, depresses HL-60 human leukaemia cell proliferation and induces apoptosis. | 2008 Sep |
|
| Brain Activation by Peptide Pro-Leu-Gly-NH(2) (MIF-1). | 2010 |
|
| KMUP-1 ameliorates monocrotaline-induced pulmonary arterial hypertension through the modulation of Ca2+ sensitization and K+-channel. | 2010 May 8 |
Patents
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| Code System | Code | Type | Description | ||
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73425400
Created by
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6033-69-8
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DBSALT002253
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DTXSID10387112
Created by
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6LPC48045D
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m4189
Created by
admin on Sat Dec 16 10:06:41 GMT 2023 , Edited by admin on Sat Dec 16 10:06:41 GMT 2023
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PRIMARY | Merck Index |
ACTIVE MOIETY
SUBSTANCE RECORD
