Forty-two extracts of folk medicinal plant organs from Pakistan were tested in competition binding assays for their interaction with the specific ligand recognition sites on the human alpha2-adrenoceptor subtypes alpha2A, alpha2B and alpha2C Strong binding of the extracts (40 mg/ml) from Acacia nilotica (L.) Delile leaves (88-98% displacement of radiolabel) and Peganum harmala seeds (89-96% dis...

The effects of the South American psychotropic beverage ayahuasca on subjective and cardiovascular variables and urine monoamine metabolite excretion were evaluated, together with the drug's pharmacokinetic profile, in a double-blind placebo-controlled clinical trial. This pharmacologically complex tea, commonly obtained from Banisteriopsis caapi and Psychotria viridis, combines N,N-dimethyltry...

Various effects of harmidine hydrochloride, an alkaloid of Peganum harmalla, have been studied in rats treated with harmidine hydrochoride 12 mg/kg body weight alone and pretreated with pyridoxine. Harmidine produced shivering, ataxia, diarrhoea, reduction in motor activity, loss of postural reflex and hypothermia. Weight of animals, respiratory rate, heart rate, urinary output, oestrous cycle,...

The biarylpropylsulfonamide class of -amino-3-hydroxy-5methyl-4-isoxazolepropionic acid (AMPA) potentiators represented by N-2-(4-(4-cyanophenol)phenol)propyl-2-propanesulfonamide (LY404187) and (R)-4 -[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide (LY503430) are positive, allosteric AMPA receptor activators, which enhance AMPA receptor-mediated neu...

In the present review an attempt has been made to explore and study the various in vitro animal models used for the evaluation of hypolipidemic and antihyperlipidemic drugs. Hyperlipidemia has been ranked as one of the greatest risk factors contributing to the prevalence and severity of coronary heart disease. The main aim of treatment in patients with hyperlipidemia is to reduce the risk of th...

There is evidence that intracellular Na+ entry potentiates hypoxic-ischemic cell death by causing cytotoxic cell edema, intracellular acidosis, and gating of Ca2+ entry by reverse activation of the Na(+)-Ca2+ exchanger. In this study, we examined the role of Na+ in mediating traumatic injury to spinal cord axons. Dorsal column segments from adult rats (n = 87) were isolated and maintained in an...

The cerebellum is a phylogenetically ancient part of the vertebrate brain, which is crucial for accurately timing complex motor tasks. Accumulating evidence suggests that the cerebellum is also involved in other tasks, such as sensory processing and cognitive tasks. The role of the cerebellum in this diverse set of tasks is heatedly debated. The cerebellum has been suggested to...

I joined the department of medicine at Yale as an assistant professor in 1977 and had a laboratory in the department of physiology. My initial studies and grants were for the characterization of Na+-glucose cotransport in renal brush border membrane vesicles, a research interest and experimental model system that I had brought from my research training with Bert Sacktor at the Gerontology Resea...

Pinoline, 6-methoxy-1,2,3,4-tetrahydro-carboline, is a serotonin analog that selectively inhibits the activity of monoamine oxidase-A and shows antidepressant activity. Our previous study using a panel of recombinant cytochrome P450 (P450) enzymes suggests that pinoline O-demethylation may be selectively catalyzed by polymorphic CYP2D6. The current study, therefore, aimed to delineate the impac...