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The synthesis of a new type of antagonist is described, capable of inactivating neuroreceptors with heretofore unattainable selectivity and permanence. These antagonists are referred to as mazek agonists (i.e. direct, inhibitory agonists) as they have the high receptor affinity and initial receptor-stimulatory effect of direct agonists and are positively coupled to effector systems. However, like direct antagonists, they have a high receptor affinity and the potential to inhibit or prevent receptor stimulation. The synthesis of the present compounds consisted of the covalent attachment of a tethered dye to three different neurotransmitter analogues, resulting in dye-neuropeptide conjugates with a high affinity for the FMRFa receptor. The dye was prepared from azure B (Az), the neurotransmitter was the neuropeptide FMRFamide (FMRFa), and the dye-neuropeptide conjugates synthesized were Az-CFMRFa; Az-CFMRF and Az-CLRFa. In this procedure, the analogues serve as carrier molecules, bound at one end to the receptor and at the other end to the dye, which is thereby brought into close contact with the receptor. The receptor can then be inactivated by singlet oxygen generated by laser irradiation of the photosensitized receptor.

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A New Method for the Synthesis of 3β-Hydroxy-4α-bromocarane and of cis-3-Carene Epoxide. -3-Carene (I) reacts with bromine and KBr in water to yield the pure trans-3β-hydroxy-4-bromocarane (II) which is converted to the cis-3-carene epoxide (III) upon treatment with sodium methoxide (or phenoxide). -(CHOUBAL, M. D.; BASSETT, J. Y.; Org. Prep. Proced.

Abstract. C16H2404, M r : 280.36, triclinic, P1, a = 6.5675 (8), b = 11.9949 (14), c = 5.1052 (6) ,~, a = 93.418 (4), fl = 100.420 (4), y = 74.612 (6) Two sets of intensity measurements were made using a modified Picker FACS-I diffractometer in the 0-20 scan mode over the range -50 < 20 < 50 °, maximum sin0/A = 0.595 ,~-~. A total of 5448 reflections were encountered between the h, k, l limits of _+ 7, _+ 14 and 0----6, respectively. Five standard reflections (161, 13,~, 312, 132 and 331) measured after every 150 showed less than 2% intensity change so corrections for crystal decay were not applied. Empirical absorption corrections were applied based on intensity variations of three reflections measured at regular intervals in ~o with X--90°. Transmission factors ranged from 1.00 to 0.92. Intensity data were merged for symmetry equivalents to yield 1340 unique reflections (Rint = 0.049) and converted to