Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus.
- K. Berg, S. Maayani, J. Goldfarb, C. Scaramellini, P. Leff, W. Clarke
- Biology, PsychologyMolecular Pharmacology
- 1 July 1998
Concentration-response curves to 5-HT2C agonists were fit well by a three-state model of receptor activation, suggesting that two active receptor states may be sufficient to explain pathway-dependent agonist efficacy.
A Locus of the Gonadotropin-releasing Hormone Receptor That Differentiates Agonist and Antagonist Binding Sites (*)
The results indicate that a charge-strengthened hydrogen bond donor is required at this locus for high affinity agonist binding but not forHigh affinity antagonist binding.
Novel actions of inverse agonists on 5-HT2C receptor systems.
Interestingly, 24-h exposure to inverse agonists acting at 5-HT2C receptors also selectively enhanced IP accumulation, but not AA release, elicited by activation of endogenous purinergic receptors, suggesting that actions of inverse agonist may be mediated through effects on receptor systems that are not direct targets for these drugs.
Signal transduction differences between 5-hydroxytryptamine type 2A and type 2C receptor systems.
- K. Berg, W. Clarke, C. Sailstad, A. Saltzman, S. Maayani
- Biology, ChemistryMolecular Pharmacology
- 1 September 1994
Data provide the first evidence for fundamental differences in the signal transduction systems of these 5-HT2 receptor subtypes.
Pharmacological studies of human erectile tissue: characteristics of spontaneous contractions and alterations in α‐adrenoceptor responsiveness with age and disease in isolated tissues
- G. Christ, S. Maayani, M. Valcic, A. Melman
- Medicine, BiologyBritish Journal of Pharmacology
- 1 October 1990
It is demonstrated that spontaneous contractions in HET are likely to be mediated by the generation and release of a stable cyclo‐oxygenase product, and both agonist and antagonist studies are consistent with the presence of a homogeneous α1‐adrenoceptor population.
Characterization of the 5-hydroxytryptamine1a receptor-mediated inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes.
The concentration-response data show that the inhibition of forskolin-stimulated adenylate cyclase activity in guinea pig and rat hippocampal membranes is mediated by a receptor with the characteristics of the 5-HT1A binding site, and it is proposed that this response is suitable for measuring activities and affinities of drugs acting at 5- HT1A receptors.
Serotonin decreases population spike amplitude in hippocampal cells through a pertussis toxin substrate
A potential 5-HT1A receptor antagonist: p-MPPI.
Modification of sexual behavior of Long–Evans male rats by drugs acting on the 5-HT1A receptor
Pleiotropic Behavior of 5‐HT2A and 5‐HT2C Receptor Agonists
- K. Berg, W. Clarke, S. Maayani, J. Goldfarb
- Biology, PsychologyAnnals of the New York Academy of Sciences
- 1 December 1998
These data strongly support the agonist‐directed trafficking hypothesis and suggest that agonists may be able to selectively activate a subset of multiple signaling pathways coupled to a single receptor subtype.