Trimipramine receptor profile request

[EN21]

I am urgently searching for the receptor/transporter profile of trimipramine.
At the PDSP database I only can find the affinity for the histamine receptor.
If anybody has more data with references, please post it.

Thank you!

 

[Helios.]

from the physician's desk reference

Trimipramine maleate is an antidepressant with an anxiety-reducing sedative component to its action. The mode of action of trimipramine maleate on the central nervous system is not known. However, unlike amphetamine-type compounds it does not act primarily by the stimulation of the central nervous system. It does not act by inhibition of the monoamine oxidase system.

Brand Names:
Surmontil.
Stangyl.
Apo-trimip.
Novo-tripramine.
Rho-trimine.

IUPAC Name:
5-(3-dimethylamino-2-methylpropyl)-10,11-dihydro-5H-dibenz(b,f)azepine acid maleate racemate.

 

[jasoncrest]

Trimipramine is a serotonin and noradrenalin reuptake inhibitor.
It has central and peripheric anticholinergic properties.
It blocks Alpha 1 adrenergic receptors.
It blocks Dopamine receptors.
It's also an H1 and H2 an antihistamine.

At a low doses, it's a tricyclic antidepressant, just like Amitriptyline.
At higher doses, it has antipsychotic properties.

 

[EN21]

Thanks alot for the help,
-but I am looking for IC50 or Ki values.
The only one I have is the Ki for the H1 receptor with 1.4 nM.

 

[Smyth]

I'd guess you will just have to use imipramine as the template, which is metabolised in-vivo to desipramine. I dont know why the other compound is important to you. But the other two compounds would serve as a closest approximation.

 

[EN21]

I need them for comparison in an article.
-And found some literature, I cannot get:
Franzer, A. Pharmacology of antidepressants; J. Clin. Psychopharmacol. 1997, Apr;17 Suppl 1:2S-18S
This must be a review

and:
Gross, G.; Xin,X.; Gastpar, M. Trimipramine: pharmacological reevaluation and comparison with clozapine
Neuropharmacology 1991 Nov; 30(11) 1159 - 1166

If someone has access, it would be great.

 

[jasoncrest]

I'd guess you will just have to use imipramine as the template, which is metabolised in-vivo to desipramine. I dont know why the other compound is important to you. But the other two compounds would serve as a closest approximation.

Trimipramine is a tricyclic antidepressant, so it shares some properties with thm; but it's a very unique tricyclic, it's the only only one that shows neuroleptic/antipsychotic effects at (not so) higher doses.

To the OP, it's not Ki values (I don't even know what it is...)
But on Wikipedia, they say this:
Trimipramine antagonism is:
-strong : 5-HT2, Muscarinic, H1, H2, Alpha1
-moderate : D2
-weak : 5-HT1, Alpha2

EDIT:
I think I found some "Ki" values:

In radioligand binding studies, D,L-trimipramine showed fairly high affinities (KI 10-60 nM) for some dopamine (DA), noradrenaline and 5-hydroxytryptamine (5-HT) receptor subtypes (5-HT2 receptors = alpha 1A/B-adrenoceptors greater than or equal to D2 receptors), intermediate affinities (300-550 nM) for D1 receptors, alpha 2B-adrenoceptors and 5-HT1C receptors but only low affinities (greater than 1000 nM) for alpha 2A-adrenoceptors, 5-HT1A, 5-HT1D and 5-HT3 receptors

 

[EN21]

Oh, thanks alot, jasoncrest for your effort. I found the same, it's the abstract of one of the articles I citated above. They must contain exact values, so I don't give up the search for the pdfs.
If I can't get it, I must find an other solution for this problem.