Minaprine hydrochloride - CAS 25953-17-7
Catalog number: 25953-17-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C17H24Cl2N4O
Molecular Weight:
371.3
COA:
Inquire
Targets:
Monoamine Oxidase
Description:
Minaprine hydrochloride is the hydrochloride salt form of Minaprine. Minaprine, also called as Agr 1240 or Cantor, an atypical antidepressant drug which is effective in most animal models of depression, is a reversible inhibitor of MAO-A and weakly inhibi
Appearance:
Solid powder
Synonyms:
4-methyl-N-(2-morpholin-4-ylethyl)-6-phenylpyridazin-3-amine;dihydrochloride 3-(2-morpholino-ethylamino)-4-methyl-6-phenyl pyridazine, dihydrochloride 3-(morpholinoethyl)amino-4-methyl-6-phenylpyridazine Agr 1240 Cantor minaprine minaprine dihydrochloride
Solubility:
Soluble to 10 mM in H2O
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -133℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Melting Point:
182 °C
InChIKey:
GNUCGROXDZMCJI-UHFFFAOYSA-N
InChI:
1S/C17H22N4O.2ClH/c1-14-13-16(15-5-3-2-4-6-15)19-20-17(14)18-7-8-21-9-11-22-12-10-21;;/h2-6,13H,7-12H2,1H3,(H,18,20);2*1H
Canonical SMILES:
CC1=CC(=NN=C1NCCN2CCOCC2)C3=CC=CC=C3.Cl.Cl
1.Pharmacological evaluation of minaprine dihydrochloride, a new psychotropic drug.
Bizière K;Kan JP;Souilhac J;Muyard JP;Roncucci R Arzneimittelforschung. 1982;32(8):824-31.
Minaprine (3-[2-morpholino-ethlamino]-4-methyl-6-phenyl-pyridazine dihydrochloride; 30038CM; trade name in France: Cantor) is a new psychotropic drug. The therapeutic profile of minaprine differs from that of other known psychotropic agents; in man the drug antagonizes the "inhibitory syndrome" characterized by decreased spontaneous activity, reduction in basic drives, slowed thoughts, feelings of tiredness and social withdrawal. Preliminary clinical trials have indicated that minaprine may also be effective in certain depressive states. This finding prompted us to study the effects of minaprine in animal models for depression. Like most antidepressants minaprine antagonizes behavioral despair, but the effect exhibits a slow onset and maximal activity is reached 24 h after administration. Minaprine also antagonizes reserpine-induced ptosis, this effect has a rapid onset, and is long-lasting. In contrast, minaprine poorly antagonizes reserpine-induced hypothermia. Unlike most antidepressants minaprine does not potentiate yohimbine-induced lethality. Minaprine potently antagonizes prochlorperazine-induced catalepsy in rats and potentiates amphetamine-induced stereotyped behavior, suggesting that the drug may enhance dopaminergic transmission.
2.Serotonin-2 receptor-mediated regulation of release of acetylcholine by minaprine in cholinergic nerve terminal of hippocampus of rat.
Muramatsu M;Tamaki-Ohashi J;Usuki C;Araki H;Aihara H Neuropharmacology. 1988 Jun;27(6):603-9.
5-Hydroxytryptamine (5-HT) inhibited the K+-induced release of [3H]acetylcholine [( 3H]ACh) from slices of the hippocampus of the rat, dose-dependently. Minaprine (3-(2-morpholinoethylamino)-4-methyl-6-phenylpyridazine, Fig. 1) had no effect on the release of [3H]ACh. However, it inhibited the (formula; see text) Fig. 1. Chemical structure of minaprine dihydrochloride. attenuation of the release of [3H]ACh by 5-HT dose-dependently. The 5-HT2 receptor antagonists, mianserine, methysergide and spiperone, prevented the inhibitory effect of the 5-HT, as well as did minaprine. The attenuating effect of 5-HT was not mimicked by the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and was not prevented by a 5-HT1A and 5-HT1B mixed receptor antagonist, propranolol, or by the 5-HT3 receptor antagonists, cocaine and metoclopramide. Minaprine inhibited the bindings of [3H]5-HT, [3H]8-OH-DPAT and [3H]ketanserin in the hippocampus. The inhibitory effect of minaprine on the binding of [3H]ketanserin was more marked than on the binding of [3H]5-HT and [3H]8-OH-DPAT, and was non-competitive. The Ki value of minaprine for the binding of [3H]ketanserin was 2.9 microM. The inhibitory effect of 5-HT on the release of [3H]ACh was observed in the presence of tetrodotoxin.
3.Minaprine and imipramine in the treatment of major depressive disorders. A comparative double-blind study.
Bohacek N;Ravic M;Bizière K Drugs Exp Clin Res. 1987;13(7):435-42.
Minaprine dihydrochloride is an aminopyridazine derivative which is chemically unrelated to other known psychotropic drugs. In rodents minaprine is active in most models of depression and is thought to exert this activity by enhancing serotonergic and dopaminergic transmission. In humans minaprine has been shown to be more effective than placebo in the treatment of major depressive episodes as defined by the DSM-III. In the present study, the efficacy and safety of minaprine (100 mg b.i.d.) in the treatment of major depressive disorders (DSM-III) were compared with those of imipramine (50 b.i.d.) in 104 patients, in a 4-week randomized, double-blind, multicentre trial. The two drugs were comparable in efficacy as judged by the Hamilton Depression Rating Scale, a Clinical Global impression and a Zung Self-Rating Scale. The onset of activity appeared to be significantly more rapid with minaprine. The incidence and intensity of unwanted effects was significantly higher in the imipramine treatment group.
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CAS 25953-17-7 Minaprine hydrochloride

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