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Discrete mapping of brain mu and delta opioid receptors using selective peptides: Quantitative autoradiography, species differences and comparison with kappa receptors
In vitro autoradiographic techniques coupled with computer-assisted image analyses revealed a discrete but differential anatomical localization of mu and delta receptors in the rat and guinea pig brain. Expand
Characterization of the ocular antiallergic and antihistaminic effects of olopatadine (AL-4943A), a novel drug for treating ocular allergic diseases.
A combination of mast cell mediator release inhibition and selective H1 receptor antagonism suggests that olopatadine may be particularly useful in the treatment of ocular allergic diseases. Expand
Immortalized human corneal epithelial cells for ocular toxicity and inflammation studies.
The CEPI-17-CL4 cells are truly immortal and express an extensive array of cytokines, growth factors, and metabolic enzymes that resemble the original tissue that will allow reproducible, mechanistic studies on toxicity, inflammation, and wound healing. Expand
Inhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs.
Select topical ocular drugs with antihistaminic activity may offer therapeutic advantages to patients with allergic conjunctivitis by inhibiting proinflammatory cytokine secretion from human conjunctival epithelial cells by attenuated histamine-stimulated phosphatidylinositol turnover and IL-6 andIL-8 secretion. Expand
AL-8810: A Novel Prostaglandin F2α Analog with Selective Antagonist Effects at the Prostaglandin F2α (FP) Receptor
A novel analog of prostaglandin F 2α [AL-8810; (5 Z , 13E)-(9 S ,11 S ,15 R )-9,15-dihydroxy-11-fluoro-15-(2-indanyl)-16,17,18,19,20-pentanor-5,13-prostadienoic acid] has been discovered withExpand
Pharmacological characterization of [3H]‐prostaglandin E2 binding to the cloned human EP4 prostanoid receptor
Prostaglandin (PG) E2 (PGE2) is a potent prostanoid derived from arachidonic which can interact with EP1, EP2, EP3 and EP4 prostanoid receptor subtypes. Recombinant human EP4 receptors expressed inExpand
Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells.
In conclusion, travoprost acid has the highest affinity, the highest FP-receptor-selectivity, and the highest potency at the FP receptor as compared to the other ocular hypotensive PG analogs known so far, including free acids of latanoprost, bimatobrost, and unoprostone isopropyl ester. Expand
Problems Associated with the Binding of L‐Glutamic Acid to Synaptic Membranes: Methodological Aspects
While binding of [3H]glutamate is almost abolished in frozen or cold‐stored membranes, lyophilisation had a remarkable effect, not only affording protection, but actually enhancing the binding properties of the synaptic membrane preparation. Expand
Comparative effects of topical ocular anti-allergy drugs on human conjunctival mast cells.
Comparing the effects of three new ocular anti-allergic drugs on mediator release from the target human conjunctival mast cell population with those of cromolyn sodium suggests that olopatadine will have efficacy advantages in allergic conjunctivitis patients over the other drugs tested. Expand
Olopatadine (AL-4943A): ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis.
Data have shown AL-4943A to be a high affinity, high potency H1-selective histamine antagonist, and this information, coupled with a long duration of action in an in vivo model of allergic conjunctivitis, suggests that AL- 4943A may be a useful drug to treat various ocular allergic diseases, including allergies to histamine. Expand