Airborne gravimetry from a small twin engine aircraft over the Long Island Sound

In January 1990, a test of the feasibility of airborne gravimetry from a small geophysical survey aircraft, a Cessna 404, was conducted over the Long Island Sound using a Bell Aerospace BGM-3 sea gravity meter. Gravity has been measured from large aircraft and specially modified de Havilland Twin Otters but never from small, standard survey aircraft. The gravity field of the Long Island Sound is dominated by an asymmetric positive 30 mGal anomaly which is well constrained by both marine and land gravity measurements. Using a Trimble 4000 GPS receiver to record the aircraft's horizontal position and radar altimeter elevations to recover the vertical accelerations, gravity anomalies along a total of 65 km were successfully measured. The root mean square (rms) difference between the airborne results and marine measurements within 2 km of the flight path was 2.6 mGal for 15 measured values. The anomalies recovered from airborne gravimetry can also be compared with the gridded regional free air gravity field calculated using all available marine and land gravity measurements. The rms difference between 458 airborne gravity measurements and the regional gravity field is 2.7 mGal. This preliminary experiment demonstrates that gravity anomalies, with wavelengths as short as 5 km, can be measured from small aircraft with accuracies of 2.7 mGal or better. The gravity measurements could be improved by higher quality vertical and horizontal positioning and tuning the gravimeter's stabilized platform for aircraft use

Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor

We recently demonstrated that SB269652 (1) engages one protomer of a dopamine D2 receptor (D2R) dimer in a bitopic mode to allosterically inhibit the binding of dopamine at the other protomer. Herein, we investigate structural deter- minants for allostery, focusing on modifications to three moieties within 1. We find that orthosteric “head” groups with small 7-substituents were important to maintain the limited negative cooperativity of analogues of 1, and replacement of the tetrahydroisoquinoline head group with other D2R “privileged structures” generated orthosteric antagonists. Additionally, replacement of the cyclohexylene linker with polymethylene chains conferred linker length dependency in allosteric pharma- cology. We validated the importance of the indolic NH as a hydrogen bond donor moiety for maintaining allostery. Replacement of the indole ring with azaindole conferred a 30-fold increase in affinity while maintaining negative cooperativity. Combined, these results provide novel SAR insight for bitopic ligands that act as negative allosteric modulators of the D2R