piperidines and potassium-hydroxide

piperidines has been researched along with potassium-hydroxide* in 1 studies

Other Studies

1 other study(ies) available for piperidines and potassium-hydroxide

Article	Year
Synthesis and evaluation of optically pure [3H]-(+)-pentazocine, a highly potent and selective radioligand for sigma receptors. FEBS letters, 1989, Jul-17, Volume: 251, Issue:1-2 Tritium-labeled (+)-pentazocine ([3H]-1b) of specific activity 26.6 Ci/mmol was synthesized in 3 steps starting with (+)-normetazocine (2) of defined optical purity. [3H]-1b has been characterized as a highly selective ligand for labeling of sigma receptors. Competition data revealed that [3H]-1b could be displaced from guinea pig brain membrane preparations with a number of commonly used sigma receptor ligands. [3H]-1b exhibited saturable, enantioselective binding with a Kd of 5.13 +/- 0.97 nM and a Bmax of 1146 +/- 122 fmol/mg protein. Phencyclidine (PCP) displaced [3H]-1b with low affinity while MK-801 was inactive, thus indicating insignificant activity at the PCP-binding site; apomorphine failed to displace [3H]-1b indicating lack of dopamine receptor cross-reactivity. Since the affinity of [3H]-1b is about 6 times that of the two commonly employed sigma ligands ((+)-3-[3H]PPP and [3H]DTG) and since it is more selective for sigma receptors than the benzomorphan [3H]SKF-10,047, it represents the first example of a highly selective benzomorphan based sigma receptor ligand. [3H]-1b should prove useful for further study of the structure and function of sigma receptors. Topics: Animals; Apomorphine; Binding, Competitive; Brain; Cell Membrane; Chemical Phenomena; Chemistry; Dopamine Agents; Guanidines; Guinea Pigs; Hydroxides; Molecular Structure; Pentazocine; Phencyclidine; Piperidines; Potassium; Potassium Compounds; Receptors, Dopamine; Receptors, Opioid; Receptors, sigma; Tritium	1989

Article

Year

Synthesis and evaluation of optically pure [3H]-(+)-pentazocine, a highly potent and selective radioligand for sigma receptors.

FEBS letters, 1989, Jul-17, Volume: 251, Issue:1-2

Tritium-labeled (+)-pentazocine ([3H]-1b) of specific activity 26.6 Ci/mmol was synthesized in 3 steps starting with (+)-normetazocine (2) of defined optical purity. [3H]-1b has been characterized as a highly selective ligand for labeling of sigma receptors. Competition data revealed that [3H]-1b could be displaced from guinea pig brain membrane preparations with a number of commonly used sigma receptor ligands. [3H]-1b exhibited saturable, enantioselective binding with a Kd of 5.13 +/- 0.97 nM and a Bmax of 1146 +/- 122 fmol/mg protein. Phencyclidine (PCP) displaced [3H]-1b with low affinity while MK-801 was inactive, thus indicating insignificant activity at the PCP-binding site; apomorphine failed to displace [3H]-1b indicating lack of dopamine receptor cross-reactivity. Since the affinity of [3H]-1b is about 6 times that of the two commonly employed sigma ligands ((+)-3-[3H]PPP and [3H]DTG) and since it is more selective for sigma receptors than the benzomorphan [3H]SKF-10,047, it represents the first example of a highly selective benzomorphan based sigma receptor ligand. [3H]-1b should prove useful for further study of the structure and function of sigma receptors.

Topics: Animals; Apomorphine; Binding, Competitive; Brain; Cell Membrane; Chemical Phenomena; Chemistry; Dopamine Agents; Guanidines; Guinea Pigs; Hydroxides; Molecular Structure; Pentazocine; Phencyclidine; Piperidines; Potassium; Potassium Compounds; Receptors, Dopamine; Receptors, Opioid; Receptors, sigma; Tritium

1989