617 0022-3565/82/2233-0617$02.00/0 THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THxRAPEUTICS Copyright © 1982 by The American Society for Pharmacology and Experimental Therapeutics Effects of Drugs on Stimulus Control of Behavior. I. Independent Assessment of Effects on Response Rates and Stimulus Control1 Pigeons were trained to peck one of two concurrently available, differently colored respo...

The inaugural ASPET–Ray Fuller Symposium was held in Indianapolis, Indiana at the Omni Severin Hotel, on September 17–19, 1999. This was the first in a series of symposia sponsored by the American Society for Pharmacology and Experimental Therapeutics that are intended to bring together individuals from academia and industry in an interactive program. This first ASPET–Ray Fuller Symposium focus...

A novel analog of prostaglandin F2a [AL-8810; (5Z, 13E)(9S,11S,15R)-9,15-dihydroxy-11-fluoro-15-(2-indanyl)-16,17, 18,19,20-pentanor-5,13-prostadienoic acid] has been discovered with uniquely low efficacy (Emax) at the endogenous prostaglandin F2a receptors (FP receptors) of A7r5 rat thoracic aorta smooth muscle cells and Swiss mouse 3T3 fibroblasts, as assayed by stimulation of phospholipase C...

L-Nicotine stimulates a biphasic release of [H]dopamine from mouse striatal synaptosomes which does not persist after agonist is removed. Approximately 80% of the initial release is transient and disappears with a half-time of less than 1 min; the other 20% persists for several minutes (t1/2, 5–10 min). Both the transient and persistent phases were investigated by 10-min exposures to agonists w...

5-Hydroxytryptamine1A (5-HT1A) receptors have been implicated in the pathophysiology and treatment of anxiety and depression, and are a target for novel drug development. This is the first study examining the human brain in vivo occupancy by a novel, selective, silent 5-HT1A antagonist. 2-[4-[4-(7Chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-diox...

We compared the effects of dopamine and norepinephrine on vasopressin (AVP)-stimulated increases in osmotic water permeability (Pf) and cAMP accumulation in the rat inner medullary collecting duct (IMCD). Both dopamine and norepinephrine inhibited AVP-induced Pf and cAMP accumulation in a concentration-dependent manner; however, norepinephrine was approximately 100-fold more potent than dopamin...

Herkinorin is the first -opioid receptor-selective ligand from the salvinorin A diterpenoid scaffold. Herkinorin has relative binding selectivity, and it can act as an agonist at both and -receptors, in vitro. These studies were the first in vivo evaluation of the effects of herkinorin in nonhuman primates, using prolactin release, a neuroendocrine biomarker assay that is responsive to both and...

The purpose of the present Perspectives is to present a synopsis of the literature on bacterial “quorum sensing” as a background for the proposal that interference with this communication system offers potential targets for the design of novel antibiotic drugs. Quorum sensing is the recently discovered chemical communication system among bacteria (both Grampositive and -negative). It is vital f...

Activation of beta adrenergic receptors in the isolated rabbit heart by catecholamines stimulates prostacyclin (PGI2) synthesis, which is inhibited by adenosine 3959-cyclic monophosphate (cAMP). The purpose of this study was to determine if activation of beta adrenergic receptors in cultured coronary endothelial cells (CEC) of rabbit heart with isoproterenol (ISOP) stimulates PGI2 synthesis and...

The present study was designed to verify our previous hypothesis that carteolol, a 1/ 2-adrenoceptor-blocking agent, is a nonconventional partial agonist of cardiac 1-adrenoceptors. To this purpose, we characterized the effects of carteolol in guinea pig myocardial preparations and measured the affinities of carteolol for highand low-affinity sites of 1-adrenoceptors labeled by CGP12177 [( )4-(...