Locomotor effects of imidazoline I₂‐site‐specific ligands and monoamine oxidase inhibitors in rats with a unilateral 6‐hydroxydopamine lesion of the nigrostriatal pathway

Abstract

1 The present study examined the ability of the selective imidazoline I 2 -site ligands 2-(-2-benzofuranyl)-2-imidazoline (2-BFI) and 2-[4,5-dihydroimidaz-2-yl]-quinoline (BU224) and selected monoamine oxidase (MAO) inhibitors to evoke locomotor activity in rats bearing a lesion of the nigrostriatal pathway. 2 Male Sprague-Dawley rats were injected with 12.5 mg 6-hydroxydopamine (6-OHDA) into the right median forebrain bundle to induce a unilateral lesion of the nigrostriatal tract. After 6 weeks, test drugs were administered either alone or in combination with L-DOPA (L-3,4-dihydroxyphenylamine) and the circling behaviour of animals was monitored as an index of anti-Parkinsonian activity. ) significantly increased either the duration or total number of contraversive rotations emitted over the testing period in comparison to L-DOPA alone. 5 These data suggest that I 2 -specific ligands have dual effects in the 6-OHDA-lesioned rat model of Parkinson's disease; a first effect associated with an increase in activity in the intact hemisphere, probably via an increase in striatal dopamine content, and a secondary action which, through the previously documented inhibition of MAO-A and/or MAO-B, increases the availability of dopamine produced by L-DOPA.

Isotopic exchange method for preparation of io-dine-125-n-(1-p-nitrobenzaldhydephenyl)-2- (2-iodophenyl)-4-(4-nitrobenzilidene)-imidazolin -5-one and its biological evaluation

“…Also, several imidazole derivatives have been developed as diagnostic agents for positron emission tomography (PET) or optical imaging [1][2][3][4]. Many imidazolines are biologically active [5,6]. 2-imidazolines have been investigated as antihyperglycemic, anti-inflammatory, antihypertensive, antihypercholesterolemic, and antidepressant reagents [6,7].The imidazole nucleus appears in a number of naturally occurring products among which, the most important are the amino acid, histidine , the purines which comprise many of the important bases in nucleic acids and hydration which occurs in beet sap.…”

“…Many imidazolines are biologically active [5,6]. 2-imidazolines have been investigated as antihyperglycemic, anti-inflammatory, antihypertensive, antihypercholesterolemic, and antidepressant reagents [6,7].The imidazole nucleus appears in a number of naturally occurring products among which, the most important are the amino acid, histidine , the purines which comprise many of the important bases in nucleic acids and hydration which occurs in beet sap. Also, In recent years, different imidazole and benzoimidazole drugs have been found to be associated with several biological activities such as antiparasitic, antifungal, anti-inflammatory, antibacterial activities [8], [9].…”

Activated fly ash catalyzed facile synthesis of novel spiro imidazolidine derivatives as potential antibacterial and antifungal agents

“…The present study describes the use of 6-carbethoxy-3,5-diarylcyclohex-2-enone 23 as a key intermediate with three versative functional groups i.e., ketone, olefin, and ester for the synthesis of imidazolidine derivatives. Owing to our interest in synthesis of fascinating biologically active hybrid heterocyclic compounds [24][25][26] and as part of our research program, herein we planned to design a spiro imidazolidine derivatives bearing a cyclohexene substituent on the carbon between the nitrogen centers to give a new series of spiro imidazolidine heterocycles because most bio-active imidazolidine derivatives bear a substituent (aryl or alkyl group) on the carbon between the nitrogen centers [18][19][20][21] .…”

“…In organic synthesis, imidazolidine units are also used as synthetic intermediates 13,14 , chiral auxiliaries 15 , chiral catalysis 16 , and ligands for asymmetric catalysis 17 . Like imidazole, imidazolidine-based compounds have been used as N-heterocyclic carbene ligands 18 on various transition metals. It is found in the commercially available second generation Grubbs' catalyst.…”

“…Most bio-active derivatives bear a substituent (aryl or alkyl group) on the carbon between the nitrogen centers. Oxymetazoline 18 is a selective α-1 agonist and partial α-2 agonist topical decongestant. Xylometazoline is a drug which is used as a nasal decongestant.…”