Clonidine and the imidazolines, commonly found in topical ophthalmic and nasal decongestants, are chemically related drugs that have been responsible for many pediatric poisonings. These medications can cause significant morbidity in small doses. A review of the available literature reveals that young children have exhibited severe signs and symptoms after ingesting as little as one to two clon...

Human semicarbazide-sensitive amine oxidase (SSAO) is a target for novel anti-inflammatory drugs that inhibit enzymatic activity. However, progress in developing such drugs has been hampered by an incomplete understanding of mechanisms involved in substrate turnover. We report here results of a comparative study of human and bovine SSAO enzymes that reveal binding of substrates and other ligand...

We recently discovered' that agmatine, a primary amine generated by decarboxylation of arginine by the enzyme arginine decarboxylase (ADC),2*3 is stored in bovine brain. As such it is the first clonidine-displacing substance (CDS) isolated whose structure has been determined. (See Reis et al., this volume: for a review.) Like clonidine, agmatine binds to imidazoline (I-) receptors of both 11 an...

Since 20 years the concept of specific imidazoline receptors has remained controversial. The problem with imidazoline receptors is mostly due to their functional similarity to alpha-adrenoceptors. In this work, a pharmacodynamic model of isolated rat jejunum longitudinal muscle strips constricted with acetylcholine (Ach) was applied to separate functional properties of the two types of receptor...

Imidazoline receptors are expressed widely in the CNS. In the present study, whole-cell patch-clamp recordings were made from medium spiny neurons in dorsal striatum slices from the rat brain, and the roles of I1-imidazoline receptors in the modulation of synaptic transmission were studied. Moxonidine, an I1-imidazoline receptor agonist, decreased the GABAA receptor-mediated IPSCs in a concentr...

N-[(Imidazolin-2-yl)amino]indolines and N-[(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines, previously described in patent literature as hypertensive agents, were synthesized and tested in viny for their affinities to α1- and α2-adrenoceptors as well as imidazoline I, and I2 receptors. The compounds most potent at either α1- or α2-adrenoceptors were administered intravenously to normotensi...

OBJECTIVES The aim of this study was to investigate the role of peripheral presynaptic alpha-2 adrenergic receptors in modulating norepinephrine (NE) release in congestive heart failure (CHF). BACKGROUND Activation of the sympathetic nervous system is a hallmark of CHF. Clonidine, an imidazoline and adrenergic agonist with high selectivity for the alpha-2 adrenoceptor, has been shown to reduc...