Theodrenaline - CAS 13460-98-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H21N5O5
Molecular Weight:
375.38
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
Theodrenaline, also known as noradrenalinoethyltheophylline, is a cardiac stimulant with anti-hypotensive property together with cafedrine.
Synonyms:
7-[2-[[2-(3,4-dihydroxyphenyl)-2-hydroxyethyl]amino]ethyl]-1,3-dimethylpurine-2,6-dione; noradrenaline theophylline; noradrenaline theophylline, (R)-isomer; noradrenaline theophylline, hydrochloride; noradrenaline theophylline, monohydrochloride, (R)-isomer; theodrenaline; theodrenaline hydrochloride; theodrenaline hydrochloride, (R)-isomer; theodrenaline, (R)-isomer
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
723.6±70.0 ℃ at 760 Torr
Density:
1.51±0.1 g/cm3
InChIKey:
WMCMJIGLYZDKRN-UHFFFAOYSA-N
InChI:
1S/C17H21N5O5/c1-20-15-14(16(26)21(2)17(20)27)22(9-19-15)6-5-18-8-13(25)10-3-4-11(23)12(24)7-10/h3-4,7,9,13,18,23-25H,5-6,8H2,1-2H3
Canonical SMILES:
CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CCNCC(C3=CC(=C(C=C3)O)O)O
1.Differences in the lipolytic and cyclic AMP accumulative action of noradrenaline-theophylline and norephedrine-theophylline.
Nencini P Arzneimittelforschung. 1980;30(7):1080-2.
The action of theophylline derivatives (-)-7-2-(2-hydroxy-1-methyl-2-phenyl-ethylamino)-ethyl-theophyl-line (cafedrine) and 7-2-2-(3,4-dihydroxy-phenyl-2-hydroxy-ethylamino)-ethyl-theophylline (theodrenaline) on free fatty acids (FFA) levels in rat blood serum and on cyclic AMP (cAMP) accumulation and FFA mobilization in isolated fat cells has been studied and compared to the action of a noradrenaline plus aminophylline mixture (NAA). A significant in vivo increase of FFA appeared 15 min after NAT and 90 min after NET i.p. administration. NAA was active at both times. Unlike NET, NAT stimulated in vitro FFA mobilization and cAMP accumulation: NAA action was however stronger. NAT-mediated cAMP accumulation, but not that which was NAA-induced, was totally inhibited by timolol. Our results suggest the existence of a beta-adrenergic mechanism for NAT and a tyraminic mechanism for NET. A theophyllinic action dos not seem to apply to either drug.
2.[Cerebral infarction in an adolescent girl following an overdose of paroxetine and caffedrine combined with theodrenaline].
Conde López VJ;Ballesteros Alcalde MC;Blanco Garrote JA;Marco Llorente J Actas Luso Esp Neurol Psiquiatr Cienc Afines. 1998 Sep-Oct;26(5):333-8.
Selective serotonin reuptake inhibitors (SSRI) have demonstrated to be effective, well tolerated and relatively safe drugs in cases of overdosage. However, and related to the potentiation of the serotonergic transmission elicited by them, these drugs have been associated by some authors with the possibility of causing vascular complications. Serotonin is a vasoactive substance with complex actions on vessel wall as a result of its interaction with specific receptors existing at this level. We present the case of an adolescent girl who suffered a cerebral infarction after consuming a toxic dose of paroxetine and two other products, one of them containing caffedrine and theodrenaline, and the other one a phlebotonic agent. In connection with the possible pathophysiological mecanism the implied products as well as the serotonergic vascular receptors are briefly reviewed. Finally, a reference is made to Calls syndrome as a possible entity related to the unfortunate event suffered by the patient. As a conclusion risks of the combined pharmacotherapy, especially in cases of overdosage and in child and adolescent populations, are underlined.
3.Akrinor
Kloth B;Pecha S;Moritz E;Schneeberger Y;Söhren KD;Schwedhelm E;Reichenspurner H;Eschenhagen T;Böger RH;Christ T;Stehr SN Front Pharmacol. 2017 May 23;8:272. doi: 10.3389/fphar.2017.00272. eCollection 2017.
Background:; Intraoperative hypotension is a common problem and direct or indirect sympathomimetic drugs are frequently needed to stabilize blood pressure. Akrinor;TM; consists of the direct and the indirect sympathomimetic noradrenaline and norephedrine. Both substances are covalently bound to the phosphodiesterase (PDE) inhibitor theophylline, yielding theodrenaline and cafedrine, respectively. We investigated pharmacodynamic effects of Akrinor;TM; and its constituents on contractile force and tension in human atrial trabeculae and internal A. mammaria rings. ;Methods:; Isometric contractions were measured in human atrial trabeculae at 1 Hz and 37°C. CGP 20712A and ICI 118,551 were used to elaborate β;1;- and β;2;-adrenoceptor (AR) subtypes involved and phenoxybenzamine to estimate indirect sympathomimetic action. PDE-inhibition was measured as a potentiation of force increase upon direct activation of adenylyl cyclase by forskolin. Human A. mammaria preparations were used to estimate intrinsic vasoconstriction and impact on the noradrenaline-induced vasoconstriction. ;Results:; Clinically relevant concentrations of Akrinor;TM; (4.2-420 mg/l) robustly increased force in human atrial trabeculae (EC;50; 41 ± 3 mg/l).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Phosphodiesterase (PDE) Products


CI-1018
(CAS: 245329-99-1)

CI-1018 is a selective type 4 phosphodiesterase inhibitor associated with vasculitis. CI-1018 has been in development to suppress inflammation.

CAS 58337-38-5 EHNA hydrochloride

EHNA hydrochloride
(CAS: 58337-38-5)

EHNA hydrochloride is a selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 μM) and also an inhibitor of adenosine deaminase. EHNA i...

CAS 152815-28-6 RS 25344 hydrochloride

RS 25344 hydrochloride
(CAS: 152815-28-6)

RS 25344 hydrochloride is a potent and selective inhibitor of four cloned isoforms of PDE4 (A, B, C and D) and phosphorylated PDE4D (IC50= 0.28, > 100, 160 and ...

CAS 1440898-82-7 Deltarasin hydrochloride

Deltarasin hydrochloride
(CAS: 1440898-82-7)

Small molecule inhibitor of the KRAS–PDEδ interaction that impairs oncogenic KRAS signalling by altering its localization to endomembranes (in cell Kd value 41 ...

CAS 939055-18-2 FIPI

FIPI
(CAS: 939055-18-2)

FIPI, a derivative of halopemide, is a potent and selective phospholipase D (PLD) inhibitor with IC50 values of 20 and 25 nM for PLD2 and PLD1 respectively. It ...

CP 461
(CAS: 227619-96-7)

CP 461, belonging to a class of novel proapoptotic drugs with antineoplastic effect, specifically inhibit cyclic GMP phosphodiesterases but not cyclooxygenase-1...

CAS 224785-90-4 Vardenafil HCl Trihydrate

Vardenafil HCl Trihydrate
(CAS: 224785-90-4)

Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil was co-marketed by Bayer Pharmaceu...

CAS 686770-80-9 BC 11-38

BC 11-38
(CAS: 686770-80-9)

BC 11-38 is a potent and selective phosphodiesterase (PDE) 11 inhibitor (IC50 = 0.28 μM for PDE11; IC50 values are >100 μM for PDE1 - PDE10). BC 11-38 increases...

Chemical Structure

CAS 13460-98-5 Theodrenaline

Quick Inquiry

Verification code

Featured Items