.delta. Opioid antagonist activity and binding studies of regioisomeric isothiocyanate derivatives of naltrindole: evidence for .delta. receptor subtypes

1992 ◽  
Vol 35 (22) ◽  
pp. 4086-4091 ◽  
Author(s):  
P. S. Portoghese ◽  
M. Sultana ◽  
W. L. Nelson ◽  
P. Klein ◽  
A. E. Takemori
Keyword(s):  
Opioid Antagonist ◽  
Receptor Subtypes ◽  
Binding Studies ◽  
Antagonist Activity ◽  
Delta Receptor ◽  
Derivatives Of

Syntheses and receptor-binding studies of derivatives of the opioid antagonist naltrexone

2004 ◽  
Vol 12 (2) ◽  
pp. 417-421 ◽  
Author(s):  
Koji Uwai ◽  
Hiroko Uchiyama ◽  
Shinobu Sakurada ◽  
Chizuko Kabuto ◽  
Mitsuhiro Takeshita
Keyword(s):  
Receptor Binding ◽  
Opioid Antagonist ◽  
Binding Studies ◽  
Derivatives Of

Bronchospasmolytic and Adenosine Binding Activity of 8- (Proline / Pyrazole)-Substituted Xanthine Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Sneha Singh ◽  
Madhwi Ojha ◽  
Divya Yadav ◽  
Sonja Kachler ◽  
Karl-Norbert Klotz ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Radioligand Binding ◽  
Binding Activity ◽  
Receptor Subtypes ◽  
Significant Protection ◽  
Binding Studies ◽  
Standard Drug ◽  
Xanthine Derivatives ◽  
Radioligand Binding Studies ◽  
Micromolar Range

Background: ABSTRACT: Background: 8-Phenyltheophylline derivatives exhibit prophylactic effects at a specific dose but do not produce the cardiovascular or emetic side effects associated with xanthines, thereby exhibiting unique characteristics of potential therapeutic importance. Methods: Novel series of 8-(proline/pyrazole)-substituted xanthine analogs has been synthesized. The affinity and selectivity of compounds to adenosine receptors have been assessed by radioligand binding studies. The synthesized compounds also showed good bronchospasmolytic properties (increased onset of bronchospasm; decreased duration of jerks) with 100% survival of animals in comparison to the standard drug. Besides, compound 8f & 9f showed good binding affinity in comparison to other synthesized compounds in the micromolar range. Results: The maximum binding affinity of these compounds was observed for A2B receptors, which is ~ 7 or 10 times higher as compared to A1, A2A and A3 receptors. The newly synthesized derivatives 8f, 9a-f, 17g-m, and 18g-m displayed significant protection against histamine aerosol induced bronchospasm in guinea pigs. Conclusion: Newly synthesized proline/pyrazole based xanthines compounds showed a satisfactory binding affinity for adenosine receptor subtypes. Replacement or variation of substituted proline ring with substituted pyrazole scaffold at 8thposition of xanthine moiety resulted in the reduction of adenosine binding affinity and bronchospasmolytic effects.

Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyrido[3,4-b]pyridine

1995 ◽  
Vol 38 (16) ◽  
pp. 3106-3120 ◽  
Author(s):  
Hideaki Natsugari ◽  
Yoshinori Ikeura ◽  
Yutaka Kiyota ◽  
Yuji Ishichi ◽  
Takenori Ishimaru ◽  
...  
Keyword(s):  
Substance P ◽  
Active Substance ◽  
Antagonist Activity ◽  
Substance P Antagonists ◽  
Orally Active ◽  
Derivatives Of

Expression of somatostatin receptor genes and their role in inhibiting Cl- secretion in HT-29cl.19A colonocytes

1995 ◽  
Vol 269 (5) ◽  
pp. G729-G736 ◽  
Author(s):  
G. Warhurst ◽  
G. O. Barbezat ◽  
N. B. Higgs ◽  
F. Reyl-Desmars ◽  
M. J. Lewin ◽  
...  
Keyword(s):  
Somatostatin Receptor ◽  
Secretory Process ◽  
Receptor Subtypes ◽  
Binding Studies ◽  
Activity Maximum ◽  
Cl Secretion ◽  
Maximum Inhibition ◽  
Polymerase Chain ◽  
Somatostatin 14

Recent studies in a cultured model of the intestinal epithelium (HT-29cl.19A) have shown that somatostatin-14 (SS-14) inhibits the Cl- secretory process by acting at multiple G protein-dependent sites. These actions may underlie the antidiarrheal properties of SS peptides. This study has investigated the expression of specific SS receptor subtypes (SSTR) in HT-29cl.19A and examined their role in mediating SS antisecretory actions. Two predominant SSTR, SSTR1 and SSTR2, were identified by reverse transcriptase-polymerase chain reaction (RT-PCR) of mRNA from polarized HT-29cl.19A monolayers. Receptor binding studies showed evidence of two distinct populations of binding sites consistent with the known properties of SSTR1 and SSTR2. The role of SSTR in inhibition of secretion was investigated by comparing the effectiveness of native and synthetic SS peptides on adenosine 3',5'-cyclic monophosphate (cAMP)-dependent Cl- secretion. Secretion stimulated by the receptor-mediated agonist prostaglandin E2 (PGE2) was inhibited > 70% by SS-14 with a 50% effective concentration (EC50) of 32 nM. In contrast, SMS-201-995 (SMS) and RC-160 exhibited little or no antisecretory activity (maximum inhibition of 15 +/- 1.9 and 2.8 +/- 1.9%, respectively, at 100 microM; EC50 > 1.5 microM). Similar effects on PGE2-stimulated cAMP accumulation were also observed. SS-14, but not SMS, also inhibited secretion stimulated by dibutyryl cAMP, which acts independently of changes in cellular cAMP. Pretreatment with pertussis toxin reversed the antisecretory effects of SS peptides.(ABSTRACT TRUNCATED AT 250 WORDS)

Analysis of GPIIb/IIIa receptor number by quantification of 7E3 binding to human platelets

Blood ◽  
1996 ◽  
Vol 88 (3) ◽  
pp. 907-914 ◽  
Author(s):  
CL Wagner ◽  
MA Mascelli ◽  
DS Neblock ◽  
HF Weisman ◽  
BS Coller ◽  
...  
Keyword(s):  
Quantitative Estimation ◽  
Critical Factor ◽  
Human Platelets ◽  
Single Individual ◽  
Binding Studies ◽  
Fab Fragment ◽  
High Affinity ◽  
Fibrinogen Binding ◽  
Receptor Number ◽  
Derivatives Of

Abstract A large number of glycoprotein (GP) IIb/IIIa receptors are present on the surface of platelets. Studies to define precisely the number of GPIIb/IIIa receptors using specific monoclonal antibodies (MoAbs) or fibrinogen binding have, however, yielded varying estimates of receptor number. To refine the quantitative estimation of GPIIb/IIIa receptors on resting platelets, we have used the MoAb 7E3, which has high affinity for GPIIb/IIIa. Quantitative binding studies were performed using radiolabeled conjugates of 7E3 IgG, as well as fragments and derivatives of 7E3. For platelets obtained from any single individual, the numbers of 7E3 F(ab′)2 and IgG molecules bound per platelet were equivalent (approximately 40,000), whereas the number of Fab molecules bound per platelet was consistently approximately twofold higher (approximately 80,000). To investigate the basis of the quantitative disparity in binding of intact 7E3 and 7E3 F(ab′)2 versus 7E3 Fab, we studied the binding of a newly constructed, bispecific (Fab′)2 molecule containing only a single 7E3 combining site. Because this construct bound to the same extent as the Fab species, the larger size of the intact 7E3 and 7E3 F(ab′)2 molecules could not explain the reduced number of molecules that bound per platelet compared to the Fab fragment. Rather, it appears that the valency of the antibody is the critical factor determining the number of antibody molecules bound per platelet. Thus, we conclude that the binding of 7E3 Fab corresponds most closely with surface GPIIb/IIIa number and that the number of GPIIb/IIIa receptors is approximately 80,000 per platelet.

Radioiodinated Azide and Isothiocyanate Derivatives of Cocaine for Irreversible Labeling of Dopamine Transporters:  Synthesis and Covalent Binding Studies

2005 ◽  
Vol 16 (3) ◽  
pp. 644-649 ◽  
Author(s):  
John R. Lever ◽  
Mu-Fa Zou ◽  
M. Laura Parnas ◽  
Romain A. Duval ◽  
Sara E. Wirtz ◽  
...  
Keyword(s):  
Covalent Binding ◽  
Binding Studies ◽  
Dopamine Transporters ◽  
Derivatives Of

ChemInform Abstract: Synthesis of 7-(2-Dimethylaminovinyl) Derivatives of Pyrazolo(1,5-a) pyrimidines, as Precursors of New Tricyclic Series. Binding Studies of BDZ Receptor.

ChemInform ◽  
2010 ◽  
Vol 25 (12) ◽  
pp. no-no
Author(s):  
F. BRUNI ◽  
A. COSTANZO ◽  
S. SELLERI ◽  
G. GUERRINI ◽  
L. GIUSTI ◽  
...  
Keyword(s):  
Binding Studies ◽  
Derivatives Of

scholarly journals Rat brain calcitonin receptor subtypes: binding studies with non-helical analogs

1990 ◽  
Vol 52 ◽  
pp. 120
Author(s):  
Hiromichi Nakamuta ◽  
Masao Koida ◽  
Ronald C. Orlowski ◽  
Richard M. Epand
Keyword(s):  
Rat Brain ◽  
Receptor Subtypes ◽  
Calcitonin Receptor ◽  
Binding Studies
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