Reversible inhibition of sperm receptor synthesis for contraception

Abstract

Methods are disclosed for reversibly inhibiting sperm receptor activity in animals. Nicarbazin, its derivatives and modifications which retain pharmacological activity are shown to inhibit activity of zona pellucida proteins and concomitant synthesis and/or assembly of the sperm receptor on the oocyte surface necessary for fertilization. Nicarbazin is easily administered, for example by simple addition to feed of an animal and is and non-toxic to the animals, providing a safe and efficient means for controlling populations of mammals and avian species.

1 . A method of reversibly inhibiting sperm receptor synthesis and assembly in animals comprising:
 administering to said animals an effective amount of nicarbazin and a carrier,   verifying inhibition of zona pellucida protein C (ZPC) in said animals, and   stopping administration to said animals to reversibly restore ZPC in said animals.   
     
     
         2 . The method of  claim 1  wherein said administration is selected from the group consisting of: intravenously, intradermally, intraarterially, intraperitoneally, intranasally, intravitreally, intravaginally, intrarectally, topically, intramuscularly, intraperitoneally, subcutaneously, mucosally, intrapericardially, orally, topically, locally, inhalation (e.g., aerosol inhalation), injection, infusion, and continuous infusion. 
     
     
         3 . The method of  claim 2  wherein said administration is orally. 
     
     
         4 . The method of  claim 1  wherein said animal is a non-human. 
     
     
         5 . The method of  claim 1  wherein said animal is a mammal. 
     
     
         6 . The method of  claim 1  wherein said animal is a rat. 
     
     
         7 . The method of  claim 1  wherein said animal is a mouse. 
     
     
         8 . The method of  claim 1  wherein said carrier is polyethylene glycol. 
     
     
         9 . The method of  claim 1  further comprising measuring ZPC. 
     
     
         10 . The method of  claim 1  wherein said administration is by combining said nicarbazin with food. 
     
     
         11 . The method of  claim 10  wherein said animal is a rat. 
     
     
         12 . The method of  claim 10  wherein said animal is a mouse. 
     
     
         13 . A method of reversibly inhibiting sperm receptor synthesis and assembly in mammals comprising:
 administering to a mammal in need of contraception an effective amount of nicarbazin and a carrier,   inhibiting zona pellucida protein C (ZPC) in said mammal, and   stopping administration to said mammals to reversibly restore ZPC in said mammals to restore fertility and allow said mammals to produce offspring.   
     
     
         14 . The method of  claim 13  wherein said administration is selected from the group consisting of: intravenously, intradermally, intraarterially, intraperitoneally, intranasally, intravitreally, intravaginally, intrarectally, topically, intramuscularly, intraperitoneally, subcutaneously, mucosally, intrapericardially, orally, topically, locally, inhalation (e.g., aerosol inhalation), injection, infusion, and continuous infusion. 
     
     
         15 . The method of  claim 13  wherein said administration is orally. 
     
     
         16 . The method of  claim 13  wherein said carrier is polyethylene glycol. 
     
     
         17 . The method of  claim 13  wherein said administration is by combining said nicarbazin with food. 
     
     
         18 . The method of  claim 13  wherein said mammal is a non-human. 
     
     
         19 . The method of  claim 13  wherein said mammal is a rat. 
     
     
         20 . The method of  claim 13  wherein said mammal is a mouse. 
     
     
         21 . The method of  claim 13  further comprising measuring ZPC.