Use of &agr;2-adrenergic receptor agonists and adrenergic...

Plant protecting and regulating compositions – Antidotes – Hetero ring containing antidote

Reexamination Certificate

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C504S105000, C504S106000, C504S108000, C504S111000, C504S168000, C504S171000

Reexamination Certificate

active

06544927

ABSTRACT:

BACKGROUND OF THE INVENTION
Abscission is the ability of plants to slough off organs, such as fruit, by an active separation of cells. Abscission occurs in specific areas of organs to be shed called “abscission zones.” Abscission zones contain several layers of starch-filled cells that eventually undergo striking changes such as cell wall digestion that ultimately lead to dropping of the fruit from the stem.
Commercial harvesting of fruit can require deviation from the natural abscission cycle. When harvesting takes place where the abscission layer has not begun to separate, a great deal of force can be required to remove the fruit. The force can damage the fruit or the plant. Presently available abscission agents, such as Ethrel®, can cause unwanted defoliation of a plant or tree. Compositions and methods are needed in the art to reduce the unwanted defoliation of plants and trees, particularly where defoliation is caused by an abscission agent or by an herbicide.
SUMMARY OF THE INVENTION
It is an object of the invention to provide methods and compositions for reducing the defoliation of plants and trees. This and other objects of the invention are provided by one or more of the embodiments described below.
One embodiment of the invention provides a defoliation safener composition. The composition comprises an abscission agent, a thinning agent, or a combination thereof, and an &agr;2-adrenergic receptor agonist, an adrenergic inhibitor, or a combination thereof.
Another embodiment of the invention provides a defoliation safener composition. The composition comprises a plant-compatible surfactant and an &agr;2-adrenergic receptor agonist, an adrenergic inhibitor, or a combination thereof.
Yet another embodiment of the invention provides a defoliation safener composition. The composition comprises a chemical selected from the group consisting of an herbicide, a pesticide, an antimicrobial agent, a fungicide, a fertilizer, and a plant hormone; and an &agr;2-adrenergic receptor agonist, an adrenergic inhibitor, or a combination thereof.
Still another embodiment of the invention provides a method of reducing defoliation of a plant or tree comprising administering an effective amount of an &agr;2-adrenergic receptor agonist, an adrenergic inhibitor, or a combination thereof, to a plant or tree, whereby defoliation is reduced.
Therefore, the invention provides methods and compositions useful in the reduction of defoliation of plants and trees.
DETAILED DESCRIPTION OF THE INVENTION
&agr;2-Adrenergic Receptor Agonists, Adrenergic Inhibitors, and Combinations Thereof
Adrenergic receptors (or adrenoceptors) mediate the central and peripheral actions of the primary sympathetic neurotransmitter, norepinephrine, and the primary adrenal medullary hormone, epinephrine. See, Ruffolo et al.,
Med. Res. Rev.
14:229 (1994). Adrenergic receptors mediate a variety of functions and have affinities for many synthetic drugs.
Adrenergic receptors are divided into two subtypes: &agr;1-adrenergic receptors and &agr;2-adrenergic receptors. &agr;2-adrenergic receptors are located on presynaptic nerve terminals, postsynaptically, and in non-synaptic settings, such as human platelets, adipocytes, and vascular smooth muscle. Agonists of &agr;2-adrenergic receptors are useful in treating a variety of diseases including, for example, hypertension, spasticity (resulting from stroke, cerebral trauma, or multiple sclerosis), short stature (in children with constitutional growth delay), glaucoma, gastric ulcers, pain relief, behavior disorders (e.g., attention-deficit hyperactivity disorder, conduct disorder, oppositional defiant disorder, Tourette's syndrome, Lesch-Nyhan syndrome, and the disinhibitory symptoms accompanying post-traumatic stress disorder and dementia), and diarrhea associated with diabetes. See, e.g., U.S. Pat. No. 6,147,102; U.S. Pat. No. 5,854,290; U.S. Pat. No. 4,312,886.
Adrenergic inhibitors are also useful in the invention and include, for example, guanethidine, bethanidine, guanadrel, and debrisoquine.
It has now been discovered for the first time that agonists of &agr;2-adrenergic receptors and adrenergic inhibitors and combinations thereof are useful as safeners, which reduce defoliation of plants and trees. In particular, agonists of &agr;2-adrenergic receptors and adrenergic inhibitors are useful in reducing defoliation of plants and trees resulting from the administration of an abscission agent or herbicide to a plant or tree.
Any &agr;2-adrenergic receptor agonist can be used in the invention. Preferably, the &agr;2-adrenergic receptor agonist is clonidine, UK14,304 (Brimonidine), apraclonidine, guanfacine, guanabenz, phenylephrine, methoxamine, metaraminol, ephedrine, oxymetazoline, naphazoline, tetrahydrozoline, or analogues thereof. An analogue is structurally similar to a particular &agr;2-adrenergic receptor agonist and has similar biological activity to the &agr;2-adrenergic receptor agonist. Similar biological activity means having 5%, 10%, or 15% greater or lesser biological activity than the particular &agr;2-adrenergic receptor agonist.
Furthermore, adrenergic inhibitors can be used in the invention. Preferably, the adrenergic inhibitor is guanethidine (Ismelin), bethanidine, guanadrel (Hylorel), debrisoquine, or analogues thereof.
An analogue is structurally similar to a particular &agr;2-adrenergic receptor agonist or adrenergic inhibitor and has similar biological activity to the &agr;2-adrenergic receptor agonist or adrenergic inhibitor. Similar biological activity means having 5%, 10%, or 15% greater or lesser biological activity than the particular &agr;2-adrenergic receptor agonist or adrenergic inhibitor.
&agr;2-adrenergic receptor agonists and adrenergic inhibitors are known in the art and are commercially available from suppliers such as Sigma/Aldrich (St. Louis, Mo.) and Tocris (Ballwin, Mo.).
Compositions of the invention can be applied to a plant or tree in a mixture with a carrier, or optionally, other auxiliary agents from any one of the standard types of preparations commonly used in agriculture, for example, a dry blend, granules, a wettable powder, an emulsion, and an aqueous solution. Suitable carriers for solid formulations include clay, talc, kaolin, bentonite, terra abla, calcium carbonate, diatomaceous earth, silica, synthetic calcium silicate, kieselguhr, dolomite, powdered magnesia, Fuller's earth, gypsum and the like. Solid compositions can be in the form of dispersible powders or grains, comprising, in addition to an &agr;2-adrenergic receptor agonist or adrenergic inhibitor, a surfactant to facilitate the dispersion of the powder or grains in liquid. Granular compositions can be prepared by, for example, impregnating an &agr;2-adrenergic receptor agonist or adrenergic inhibitor onto or into granulated carriers such as attapulgites or vermiculites, or granulated solid fertilizers.
Liquid forms of the compositions of the invention, which are used for example, for spraying on plants or trees as aerosols or mists, are prepared for application by mixing an &agr;2-adrenergic receptor agonist or adrenergic inhibitor, surfactant, if used, and a liquid carrier, such as water or other liquid to form a stable emulsion or suspension. Liquid compositions of the invention include solutions, dispersions, or emulsions containing an &agr;2-adrenergic receptor agonist or adrenergic inhibitor and optionally, one or more surface-active agents such as wetting agents, dispersing agents, emulsifying agents, or suspending agents.
&agr;2-adrenergic receptor agonist and adrenergic inhibitor compositions of the invention are preferably formulated for use in a mixture with a plant-compatible surfactant, to provide solid or liquid (including a suspension of a solid in a liquid phase) formulations. A plant-compatible surfactant causes little or no damage to plants or trees. Surfactants of the invention can be nonionic, anionic, cationic, or zwitterionic surfactants. A surfactant can be present in a composition of the invention as formulated or, alternatively, a s

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